Palbociclib Isethionate
別名: PD0332991 Isethionate
Palbociclib Isethionate是一種高度選擇性的CDK4/6抑制劑，無細胞試驗中IC50為11 nM/16 nM，對CDK1/2/5，EGFR，FGFR，PDGFR， InsR等沒有抑制活性。Phase 3。
Palbociclib Isethionate Chemical Structure
CAS: 827022-33-3
產品質控
批次：
純度：
99.99%
99.99
Palbociclib Isethionate相關產品
相關信號通路圖
細胞實驗數據示例
| 細胞系 | 實驗類型 | 給藥濃度 | 孵育時間 | 活性描述 | 文獻信息 |
|---|---|---|---|---|---|
| U-CH6 | Growth Inhibition Assay | 0-1 μM | 72 h | IC50=90 nM | 26183925 |
| U-CH3 | Growth Inhibition Assay | 0-1 μM | 72 h | IC50=52 nM | 26183925 |
| U-CH2 | Growth Inhibition Assay | 0-1 μM | 72 h | IC50=50.2 nM | 26183925 |
| IMR-32 | Fuction Assay | 0-1 μM | 24 h | reduces the expression of?TOP2A,?CCNE2, and?TK1?in a dose-dependent manner | 26225123 |
| NGP | Fuction Assay | 0-1 μM | 24 h | reduces the expression of?TOP2A,?CCNE2, and?TK1?in a dose-dependent manner | 26225123 |
| SH-EP | Growth Inhibition Assay | 1 μM | 24 h | induces G1 arrest | 26225123 |
| NGP | Growth Inhibition Assay | 1 μM | 24 h | induces G1 arrest | 26225123 |
| SH-SY5Y | Growth Inhibition Assay | 1 μM | 24 h | induces G1 arrest | 26225123 |
| IMR-32 | Growth Inhibition Assay | 1 μM | 24 h | induces G1 arrest | 26225123 |
| H596 | Growth Inhibition Assay | 0-100 μM | 72 h | IC50=12 μM | 26390342 |
| H520 | Growth Inhibition Assay | 0-100 μM | 72 h | IC50=0.73 μM | 26390342 |
| H2170 | Growth Inhibition Assay | 0-100 μM | 72 h | IC50=5 μM | 26390342 |
| H157 | Growth Inhibition Assay | 0-100 μM | 72 h | IC50=9 μM | 26390342 |
| U-CH7 | Growth Inhibition Assay | 0-1 μM | 72 h | IC50=98 nM | 26183925 |
| U-CH11 | Growth Inhibition Assay | 0-1 μM | 72 h | IC50=340 nM | 26183925 |
| MCF7 | Fuction Assay | 2.5-250 nM | 24 h | reduces Rb phosphorylation | 25991817 |
| MV4-11 | Apoptosis Assay | 0.5 μM | 24 h | enhances apoptosis induced by sorafenib and AC220 | 25487917 |
| MOLM13 | Apoptosis Assay | 0.5 μM | 24 h | enhances apoptosis induced by sorafenib and AC220 | 25487917 |
| MCF7 | Antitumor assay | 100 mg/kg/day | 14 days | Antitumor activity against human estrogen-independent human MCF7 cells xenografted in RNU rat assessed as tumor growth inhibition at 100 mg/kg/day, ig administered for 14 days measured on day 15 | 27448913 |
| MDA-MB-231 | Cell cycle arrest assay | 0.5 to 1 uM | 24 hrs | Cell cycle arrest in human MDA-MB-231 cells assessed as accumulation at G1 phase at 0.5 to 1 uM after 24 hrs by propidium iodide staining-based flow cytometric analysis | 24417566 |
| MCF7 | Cell cycle arrest assay | 0.5 to 1 uM | 24 hrs | Cell cycle arrest in human MCF7 cells assessed as accumulation at G1 phase at 0.5 to 1 uM after 24 hrs by propidium iodide staining-based flow cytometric analysis | 24417566 |
| MDA-MB-231 | Function assay | 0.5 to 5 uM | 24 hrs | Inhibition of recombinant CDK4/cyclinD1 in human MDA-MB-231 cells assessed as inhibition of retinoblastoma phosphorylation at Ser780 at 0.5 to 5 uM after 24 hrs by Western blotting analysis | 24417566 |
| MDA-MB-231 | Function assay | 0.5 to 5 uM | 24 hrs | Inhibition of recombinant CDK4/cyclinD1 in human MDA-MB-231 cells assessed as inhibition of retinoblastoma phosphorylation at Ser780 at 0.5 to 5 uM after 24 hrs by Western blotting analysis | 24417566 |
| MCF7 | Function assay | 0.5 to 5 uM | 24 hrs | Inhibition of recombinant CDK4/cyclinD1 in human MCF7 cells assessed as inhibition of retinoblastoma phosphorylation at Ser780 at 0.5 to 5 uM after 24 hrs by Western blotting analysis | 24417566 |
| MCF7 | Function assay | 0.5 to 5 uM | 24 hrs | Inhibition of recombinant CDK4/cyclinD1 in human MCF7 cells assessed as inhibition of retinoblastoma phosphorylation at Ser780 at 0.5 to 5 uM after 24 hrs by Western blotting analysis | 24417566 |
| SH-EP | Growth Inhibition Assay | 48?h | IC50=2.211 μM | 26225123 | |
| NGP | Growth Inhibition Assay | 48?h | IC50=2.077 μM | 26225123 | |
| SH-SY5Y | Growth Inhibition Assay | 48?h | IC50=676 nM | 26225123 | |
| IMR-32 | Growth Inhibition Assay | 48?h | IC50=261 nM | 26225123 | |
| MOLM13 | Function assay | 24 hrs | Inhibition of CDK4 in human MOLM13 cells assessed as inhibition of Rb phosphorylation at Ser780 after 24 hrs, IC50 = 0.011 μM. | 24641103 | |
| COLO205 | Antiproliferative assay | 72 hrs | Antiproliferative activity against Rb-positive human COLO205 cells assessed as incorporation of [3H]thymidine into DNA after 72 hrs by beta-plate counting analysis, IC50 = 0.036 μM. | 24641103 | |
| MOLM13 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MOLM13 cells harboring FLT3 ITD mutant assessed as incorporation of [3H]thymidine into DNA after 72 hrs by beta-plate counting analysis, IC50 = 0.096 μM. | 24641103 | |
| MOLM13 | Antiproliferative assay | 72 hrs | Antiproliferative activity against sorafenib-resistant human MOLM13 cells assessed as incorporation of [3H]thymidine into DNA after 72 hrs by beta-plate counting analysis, IC50 = 0.096 μM. | 24641103 | |
| U937 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human U937 cells assessed as incorporation of [3H]thymidine into DNA after 72 hrs by beta-plate counting analysis, IC50 = 0.14 μM. | 24641103 | |
| insect cell | Function assay | 2 mins | Inhibition of CDK6/cyclin D2 (unknown origin) expressed in baculovirus infected insect cells using GST-fused pRb (792 to 928) as substrate preincubated for 2 mins followed by [gamma-32P]-ATP addition measured after 15 mins by beta plate counting analysis, IC50 = 0.009 μM. | 26115571 | |
| insect cell | Function assay | 2 mins | Inhibition of CDK6/cyclin D2 (unknown origin) expressed in baculovirus infected insect cells using GST-fused pRb (792 to 928) as substrate preincubated for 2 mins followed by [gamma-32P]-ATP addition measured after 15 mins by beta plate counting analysis, IC50 = 0.009 μM. | 26115571 | |
| insect cell | Function assay | 2 mins | Inhibition of CDK4/cyclin D1 (unknown origin) expressed in baculovirus infected insect cells using GST-fused pRb (792 to 928) as substrate preincubated for 2 mins followed by [gamma-32P]-ATP addition measured after 15 mins by beta plate counting analysis, IC50 = 0.011 μM. | 26115571 | |
| insect cell | Function assay | 2 mins | Inhibition of CDK4/cyclin D1 (unknown origin) expressed in baculovirus infected insect cells using GST-fused pRb (792 to 928) as substrate preincubated for 2 mins followed by [gamma-32P]-ATP addition measured after 15 mins by beta plate counting analysis, IC50 = 0.011 μM. | 26115571 | |
| MDA-MB-435 | Antiproliferative assay | 24 hrs | Antiproliferative activity against Rb-positive human MDA-MB-435 cells assessed as inhibition of [14C]-thymidine incorporation into DNA preincubated for 24 hrs followed by [14C]-thymidine addition measured after 72 hrs by beta plate counting analysis, IC50 = 0.16 μM. | 26115571 | |
| insect cell | Function assay | 2 mins | Inhibition of CDK4/cyclin D1 (unknown origin) expressed in baculovirus infected insect cells using GST-tagged pRB (792 to 928 residues) as substrate preincubated for 2 mins followed by [gamma32P]ATP addition measured after 15 mins by beta counting method, IC50 = 0.011 μM. | 27171036 | |
| insect cell | Function assay | 2 mins | Inhibition of CDK4/cyclin D1 (unknown origin) expressed in baculovirus infected insect cells using GST-tagged pRB (792 to 928 residues) as substrate preincubated for 2 mins followed by [gamma32P]ATP addition measured after 15 mins by beta counting method, IC50 = 0.011 μM. | 27171036 | |
| insect cell | Function assay | 2 mins | Inhibition of CDK6/cyclin D2 (unknown origin) expressed in baculovirus infected insect cells using GST-tagged pRB (792 to 928 residues) as substrate preincubated for 2 mins followed by [gamma32P]ATP addition measured after 15 mins by beta counting method, IC50 = 0.015 μM. | 27171036 | |
| insect cell | Function assay | 2 mins | Inhibition of CDK6/cyclin D2 (unknown origin) expressed in baculovirus infected insect cells using GST-tagged pRB (792 to 928 residues) as substrate preincubated for 2 mins followed by [gamma32P]ATP addition measured after 15 mins by beta counting method, IC50 = 0.015 μM. | 27171036 | |
| MDA-MB-453 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human MDA-MB-453 cells assessed as reduction in cell viability after 48 hrs by CCK8 assay, IC50 = 0.137 μM. | 27448913 | |
| MCF7 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 48 hrs by CCK8 assay, IC50 = 0.24 μM. | 27448913 | |
| MDA-MB-231 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 48 hrs by CCK8 assay, IC50 = 0.58 μM. | 27448913 | |
| A2780 | Growth inhibition assay | 72 hrs | Growth inhibition of human A2780 cells after 72 hrs by resazurin or MTT assay, GI50 = 0.032 μM. | 28156111 | |
| MV4-11 | Growth inhibition assay | 72 hrs | Growth inhibition of human MV4-11 cells after 72 hrs by resazurin assay, GI50 = 0.05 μM. | 28156111 | |
| MOLM13 | Growth inhibition assay | 72 hrs | Growth inhibition of human MOLM13 cells after 72 hrs by resazurin or MTT assay, GI50 = 0.062 μM. | 28156111 | |
| NB4 | Growth inhibition assay | 72 hrs | Growth inhibition of human NB4 cells after 72 hrs by resazurin or MTT assay, GI50 = 0.066 μM. | 28156111 | |
| PC3 | Growth inhibition assay | 72 hrs | Growth inhibition of human PC3 cells after 72 hrs by resazurin or MTT assay, GI50 = 0.071 μM. | 28156111 | |
| MDA-MB-453 | Growth inhibition assay | 72 hrs | Growth inhibition of human MDA-MB-453 cells after 72 hrs by MTT assay, GI50 = 0.326 μM. | 28156111 | |
| MCF7 | Growth inhibition assay | 72 hrs | Growth inhibition of human MCF7 cells after 72 hrs by resazurin or MTT assay, GI50 = 0.557 μM. | 28156111 | |
| M229 | Growth inhibition assay | 72 hrs | Growth inhibition of human M229 cells after 72 hrs by resazurin or MTT assay, GI50 = 1.22 μM. | 28156111 | |
| M238 | Growth inhibition assay | 72 hrs | Growth inhibition of human M238 cells after 72 hrs by resazurin or MTT assay, GI50 = 1.97 μM. | 28156111 | |
| M249 | Growth inhibition assay | 72 hrs | Growth inhibition of human M249 cells after 72 hrs by resazurin or MTT assay, GI50 = 1.99 μM. | 28156111 | |
| M249R | Growth inhibition assay | 72 hrs | Growth inhibition of human M249R cells after 72 hrs by resazurin or MTT assay, GI50 = 2.96 μM. | 28156111 | |
| C4-2B | Growth inhibition assay | 72 hrs | Growth inhibition of human C4-2B cells after 72 hrs by resazurin or MTT assay, GI50 = 4.15 μM. | 28156111 | |
| DU145 | Growth inhibition assay | 72 hrs | Growth inhibition of human DU145 cells after 72 hrs by resazurin or MTT assay, GI50 = 5.792 μM. | 28156111 | |
| MDA-MB-468 | Growth inhibition assay | 72 hrs | Growth inhibition of human MDA-MB-468 cells after 72 hrs by resazurin or MTT assay, GI50 = 5.96 μM. | 28156111 | |
| BPH1 | Growth inhibition assay | 72 hrs | Growth inhibition of nontransformed human BPH1 cells after 72 hrs by resazurin or MTT assay, GI50 = 7.442 μM. | 28156111 | |
| K562 | Cytotoxicity assay | 96 hrs | Cytotoxicity against human K562 cells after 96 hrs by Cell-Titer Blue assay, IC50 = 2 μM. | 24417566 | |
| DU145 | Cytotoxicity assay | 96 hrs | Cytotoxicity against human DU145 cells after 96 hrs by Cell-Titer Blue assay, IC50 = 7.5 μM. | 24417566 | |
| MV4-11 | Function assay | 12 to 24 hrs | Inhibition of CDK4/6 in human MV4-11 cells assessed as reduction in Rb phosphorylation at Ser780 at GI50 after 12 to 24 hrs by Western blot analysis | 28156111 | |
| MV4-11 | Function assay | 12 to 24 hrs | Inhibition of CDK4/6 in human MV4-11 cells assessed as reduction in Rb phosphorylation at Ser780 at GI50 after 12 to 24 hrs by Western blot analysis | 28156111 | |
| MOLM13-ITD alone | Growth Inhibition Assay | IC50=0.089 ± 0.009 μM | 25487917 | ||
| MV4-11-ITD alone | Growth Inhibition Assay | IC50=0.092 ± 0.008 μM | 25487917 | ||
| MOLM13-ITD/D835Y | Growth Inhibition Assay | IC50=0.114 ± 0.011 μM | 25487917 | ||
| MV4-11-ITD/D835V | Growth Inhibition Assay | IC50=0.116 ± 0.011 μM | 25487917 | ||
| MV4-11-ITD/D835V | Growth Inhibition Assay | IC50=0.102 ± 0.006 μM | 25487917 | ||
| MV4-11-ITD/F691L | Growth Inhibition Assay | IC50=0.112 ± 0.015 μM | 25487917 | ||
| MV4-11-ITD/N841K | Growth Inhibition Assay | IC50=0.113 ± 0.002 μM | 25487917 | ||
| U937-FLT3 WT | Growth Inhibition Assay | IC50=0.102 ± 0.013 μM | 25487917 | ||
| P12-ICHIKAWA | Growth Inhibition assay | IC50 = 0.09604 μM | SANGER | ||
| 697 | Growth Inhibition assay | IC50 = 0.14838 μM | SANGER | ||
| NB69 | Growth Inhibition assay | IC50 = 0.1618 μM | SANGER | ||
| EoL-1-cell | Growth Inhibition assay | IC50 = 0.18726 μM | SANGER | ||
| BHT-101 | Growth Inhibition assay | IC50 = 0.19825 μM | SANGER | ||
| SK-NEP-1 | Growth Inhibition assay | IC50 = 0.22002 μM | SANGER | ||
| MHH-NB-11 | Growth Inhibition assay | IC50 = 0.22019 μM | SANGER | ||
| AsPC-1 | Growth Inhibition assay | IC50 = 0.25253 μM | SANGER | ||
| ES1 | Growth Inhibition assay | IC50 = 0.25625 μM | SANGER | ||
| LAMA-84 | Growth Inhibition assay | IC50 = 0.25819 μM | SANGER | ||
| MOLT-16 | Growth Inhibition assay | IC50 = 0.25849 μM | SANGER | ||
| ES7 | Growth Inhibition assay | IC50 = 0.27309 μM | SANGER | ||
| KY821 | Growth Inhibition assay | IC50 = 0.3141 μM | SANGER | ||
| RT-112 | Growth Inhibition assay | IC50 = 0.32105 μM | SANGER | ||
| HL-60 | Growth Inhibition assay | IC50 = 0.34066 μM | SANGER | ||
| MOLT-4 | Growth Inhibition assay | IC50 = 0.34513 μM | SANGER | ||
| KARPAS-45 | Growth Inhibition assay | IC50 = 0.37616 μM | SANGER | ||
| SK-N-AS | Growth Inhibition assay | IC50 = 0.38783 μM | SANGER | ||
| CTB-1 | Growth Inhibition assay | IC50 = 0.40502 μM | SANGER | ||
| NKM-1 | Growth Inhibition assay | IC50 = 0.41189 μM | SANGER | ||
| HTC-C3 | Growth Inhibition assay | IC50 = 0.43295 μM | SANGER | ||
| BE-13 | Growth Inhibition assay | IC50 = 0.44427 μM | SANGER | ||
| KOSC-2 | Growth Inhibition assay | IC50 = 0.4669 μM | SANGER | ||
| NB14 | Growth Inhibition assay | IC50 = 0.48358 μM | SANGER | ||
| CAL-27 | Growth Inhibition assay | IC50 = 0.49459 μM | SANGER | ||
| H9 | Growth Inhibition assay | IC50 = 0.49543 μM | SANGER | ||
| RS4-11 | Growth Inhibition assay | IC50 = 0.50473 μM | SANGER | ||
| PA-1 | Growth Inhibition assay | IC50 = 0.50986 μM | SANGER | ||
| MV-4-11 | Growth Inhibition assay | IC50 = 0.51385 μM | SANGER | ||
| OS-RC-2 | Growth Inhibition assay | IC50 = 0.52162 μM | SANGER | ||
| RPMI-8226 | Growth Inhibition assay | IC50 = 0.52686 μM | SANGER | ||
| HGC-27 | Growth Inhibition assay | IC50 = 0.56499 μM | SANGER | ||
| CHP-212 | Growth Inhibition assay | IC50 = 0.59359 μM | SANGER | ||
| NB10 | Growth Inhibition assay | IC50 = 0.59918 μM | SANGER | ||
| HH | Growth Inhibition assay | IC50 = 0.59943 μM | SANGER | ||
| EW-16 | Growth Inhibition assay | IC50 = 0.60352 μM | SANGER | ||
| ES8 | Growth Inhibition assay | IC50 = 0.60521 μM | SANGER | ||
| HAL-01 | Growth Inhibition assay | IC50 = 0.60567 μM | SANGER | ||
| A204 | Growth Inhibition assay | IC50 = 0.63391 μM | SANGER | ||
| MHH-PREB-1 | Growth Inhibition assay | IC50 = 0.63699 μM | SANGER | ||
| EM-2 | Growth Inhibition assay | IC50 = 0.65064 μM | SANGER | ||
| BV-173 | Growth Inhibition assay | IC50 = 0.65248 μM | SANGER | ||
| ONS-76 | Growth Inhibition assay | IC50 = 0.67782 μM | SANGER | ||
| KM-H2 | Growth Inhibition assay | IC50 = 0.69554 μM | SANGER | ||
| D-263MG | Growth Inhibition assay | IC50 = 0.71712 μM | SANGER | ||
| ES3 | Growth Inhibition assay | IC50 = 0.72893 μM | SANGER | ||
| VA-ES-BJ | Growth Inhibition assay | IC50 = 0.73227 μM | SANGER | ||
| NBsusSR | Growth Inhibition assay | IC50 = 0.74299 μM | SANGER | ||
| NCI-H520 | Growth Inhibition assay | IC50 = 0.74652 μM | SANGER | ||
| ES5 | Growth Inhibition assay | IC50 = 0.7528 μM | SANGER | ||
| T-24 | Growth Inhibition assay | IC50 = 0.77871 μM | SANGER | ||
| SW962 | Growth Inhibition assay | IC50 = 0.80863 μM | SANGER | ||
| EW-3 | Growth Inhibition assay | IC50 = 0.80876 μM | SANGER | ||
| RXF393 | Growth Inhibition assay | IC50 = 0.81279 μM | SANGER | ||
| U251 | Growth Inhibition assay | IC50 = 0.81388 μM | SANGER | ||
| CAMA-1 | Growth Inhibition assay | IC50 = 0.83394 μM | SANGER | ||
| JVM-3 | Growth Inhibition assay | IC50 = 0.85178 μM | SANGER | ||
| COLO-800 | Growth Inhibition assay | IC50 = 0.89778 μM | SANGER | ||
| OVCAR-5 | Growth Inhibition assay | IC50 = 0.9001 μM | SANGER | ||
| LB1047-RCC | Growth Inhibition assay | IC50 = 0.92756 μM | SANGER | ||
| SW954 | Growth Inhibition assay | IC50 = 0.92941 μM | SANGER | ||
| J-RT3-T3-5 | Growth Inhibition assay | IC50 = 0.93606 μM | SANGER | ||
| Mewo | Growth Inhibition assay | IC50 = 0.9366 μM | SANGER | ||
| NCI-H1770 | Growth Inhibition assay | IC50 = 0.94055 μM | SANGER | ||
| HO-1-N-1 | Growth Inhibition assay | IC50 = 0.96281 μM | SANGER | ||
| HSC-3 | Growth Inhibition assay | IC50 = 0.96648 μM | SANGER | ||
| TYK-nu | Growth Inhibition assay | IC50 = 0.99825 μM | SANGER | ||
| KYSE-150 | Growth Inhibition assay | IC50 = 1.00076 μM | SANGER | ||
| SN12C | Growth Inhibition assay | IC50 = 1.00875 μM | SANGER | ||
| MOLT-13 | Growth Inhibition assay | IC50 = 1.01421 μM | SANGER | ||
| TE-11 | Growth Inhibition assay | IC50 = 1.04812 μM | SANGER | ||
| DB | Growth Inhibition assay | IC50 = 1.07273 μM | SANGER | ||
| CAL-39 | Growth Inhibition assay | IC50 = 1.07522 μM | SANGER | ||
| A3-KAW | Growth Inhibition assay | IC50 = 1.08408 μM | SANGER | ||
| CHP-134 | Growth Inhibition assay | IC50 = 1.11807 μM | SANGER | ||
| TGW | Growth Inhibition assay | IC50 = 1.12395 μM | SANGER | ||
| QIMR-WIL | Growth Inhibition assay | IC50 = 1.13134 μM | SANGER | ||
| NCI-SNU-1 | Growth Inhibition assay | IC50 = 1.16354 μM | SANGER | ||
| CGTH-W-1 | Growth Inhibition assay | IC50 = 1.17186 μM | SANGER | ||
| MHH-ES-1 | Growth Inhibition assay | IC50 = 1.17986 μM | SANGER | ||
| LB2241-RCC | Growth Inhibition assay | IC50 = 1.1862 μM | SANGER | ||
| ML-2 | Growth Inhibition assay | IC50 = 1.20734 μM | SANGER | ||
| COR-L23 | Growth Inhibition assay | IC50 = 1.22933 μM | SANGER | ||
| BFTC-905 | Growth Inhibition assay | IC50 = 1.24267 μM | SANGER | ||
| Hs-578-T | Growth Inhibition assay | IC50 = 1.25817 μM | SANGER | ||
| KG-1 | Growth Inhibition assay | IC50 = 1.26686 μM | SANGER | ||
| HEL | Growth Inhibition assay | IC50 = 1.29338 μM | SANGER | ||
| A549 | Growth Inhibition assay | IC50 = 1.29399 μM | SANGER | ||
| COLO-741 | Growth Inhibition assay | IC50 = 1.32089 μM | SANGER | ||
| PC-3 | Growth Inhibition assay | IC50 = 1.35221 μM | SANGER | ||
| HOS | Growth Inhibition assay | IC50 = 1.35296 μM | SANGER | ||
| HT-1080 | Growth Inhibition assay | IC50 = 1.37519 μM | SANGER | ||
| TE-8 | Growth Inhibition assay | IC50 = 1.41774 μM | SANGER | ||
| BHY | Growth Inhibition assay | IC50 = 1.46923 μM | SANGER | ||
| BB65-RCC | Growth Inhibition assay | IC50 = 1.50528 μM | SANGER | ||
| HN | Growth Inhibition assay | IC50 = 1.54071 μM | SANGER | ||
| NCI-H441 | Growth Inhibition assay | IC50 = 1.54907 μM | SANGER | ||
| RPMI-8866 | Growth Inhibition assay | IC50 = 1.58507 μM | SANGER | ||
| CAL-62 | Growth Inhibition assay | IC50 = 1.60862 μM | SANGER | ||
| MG-63 | Growth Inhibition assay | IC50 = 1.61813 μM | SANGER | ||
| SK-LU-1 | Growth Inhibition assay | IC50 = 1.62152 μM | SANGER | ||
| BCPAP | Growth Inhibition assay | IC50 = 1.66457 μM | SANGER | ||
| 22RV1 | Growth Inhibition assay | IC50 = 1.67843 μM | SANGER | ||
| T47D | Growth Inhibition assay | IC50 = 1.68061 μM | SANGER | ||
| MSTO-211H | Growth Inhibition assay | IC50 = 1.69603 μM | SANGER | ||
| DEL | Growth Inhibition assay | IC50 = 1.70273 μM | SANGER | ||
| H4 | Growth Inhibition assay | IC50 = 1.73212 μM | SANGER | ||
| CAL-51 | Growth Inhibition assay | IC50 = 1.74855 μM | SANGER | ||
| ABC-1 | Growth Inhibition assay | IC50 = 1.78582 μM | SANGER | ||
| MZ2-MEL | Growth Inhibition assay | IC50 = 1.79542 μM | SANGER | ||
| YKG-1 | Growth Inhibition assay | IC50 = 1.81061 μM | SANGER | ||
| KM12 | Growth Inhibition assay | IC50 = 1.81602 μM | SANGER | ||
| L-363 | Growth Inhibition assay | IC50 = 1.87412 μM | SANGER | ||
| KU812 | Growth Inhibition assay | IC50 = 1.89282 μM | SANGER | ||
| LOXIMVI | Growth Inhibition assay | IC50 = 1.91228 μM | SANGER | ||
| G-401 | Growth Inhibition assay | IC50 = 1.92428 μM | SANGER | ||
| SW780 | Growth Inhibition assay | IC50 = 1.96246 μM | SANGER | ||
| SW872 | Growth Inhibition assay | IC50 = 1.9833 μM | SANGER | ||
| NB7 | Growth Inhibition assay | IC50 = 1.99323 μM | SANGER | ||
| T98G | Growth Inhibition assay | IC50 = 2.00666 μM | SANGER | ||
| SW1710 | Growth Inhibition assay | IC50 = 2.06945 μM | SANGER | ||
| NCI-H1573 | Growth Inhibition assay | IC50 = 2.07298 μM | SANGER | ||
| KE-37 | Growth Inhibition assay | IC50 = 2.08951 μM | SANGER | ||
| 786-0 | Growth Inhibition assay | IC50 = 2.15439 μM | SANGER | ||
| SAS | Growth Inhibition assay | IC50 = 2.20374 μM | SANGER | ||
| CAL-54 | Growth Inhibition assay | IC50 = 2.20413 μM | SANGER | ||
| SF268 | Growth Inhibition assay | IC50 = 2.23122 μM | SANGER | ||
| SW620 | Growth Inhibition assay | IC50 = 2.26169 μM | SANGER | ||
| MN-60 | Growth Inhibition assay | IC50 = 2.3106 μM | SANGER | ||
| EFO-27 | Growth Inhibition assay | IC50 = 2.32058 μM | SANGER | ||
| NCI-H747 | Growth Inhibition assay | IC50 = 2.32199 μM | SANGER | ||
| HCC2218 | Growth Inhibition assay | IC50 = 2.35374 μM | SANGER | ||
| MIA-PaCa-2 | Growth Inhibition assay | IC50 = 2.36437 μM | SANGER | ||
| SJSA-1 | Growth Inhibition assay | IC50 = 2.37796 μM | SANGER | ||
| RKO | Growth Inhibition assay | IC50 = 2.38496 μM | SANGER | ||
| NB6 | Growth Inhibition assay | IC50 = 2.40374 μM | SANGER | ||
| ES4 | Growth Inhibition assay | IC50 = 2.45422 μM | SANGER | ||
| EGI-1 | Growth Inhibition assay | IC50 = 2.46883 μM | SANGER | ||
| CTV-1 | Growth Inhibition assay | IC50 = 2.52773 μM | SANGER | ||
| NCI-H1355 | Growth Inhibition assay | IC50 = 2.55951 μM | SANGER | ||
| GT3TKB | Growth Inhibition assay | IC50 = 2.59199 μM | SANGER | ||
| SK-HEP-1 | Growth Inhibition assay | IC50 = 2.59266 μM | SANGER | ||
| GAMG | Growth Inhibition assay | IC50 = 2.59394 μM | SANGER | ||
| SK-MES-1 | Growth Inhibition assay | IC50 = 2.61803 μM | SANGER | ||
| RO82-W-1 | Growth Inhibition assay | IC50 = 2.62057 μM | SANGER | ||
| ECC10 | Growth Inhibition assay | IC50 = 2.70206 μM | SANGER | ||
| MCF7 | Growth Inhibition assay | IC50 = 2.71464 μM | SANGER | ||
| D-283MED | Growth Inhibition assay | IC50 = 2.7243 μM | SANGER | ||
| RPMI-7951 | Growth Inhibition assay | IC50 = 2.75694 μM | SANGER | ||
| Ramos-2G6-4C10 | Growth Inhibition assay | IC50 = 2.77099 μM | SANGER | ||
| KGN | Growth Inhibition assay | IC50 = 2.81884 μM | SANGER | ||
| NUGC-3 | Growth Inhibition assay | IC50 = 2.82505 μM | SANGER | ||
| NCI-H292 | Growth Inhibition assay | IC50 = 2.85053 μM | SANGER | ||
| Becker | Growth Inhibition assay | IC50 = 2.95832 μM | SANGER | ||
| NCI-H1299 | Growth Inhibition assay | IC50 = 3.05263 μM | SANGER | ||
| ETK-1 | Growth Inhibition assay | IC50 = 3.0543 μM | SANGER | ||
| TK10 | Growth Inhibition assay | IC50 = 3.20165 μM | SANGER | ||
| VMRC-RCZ | Growth Inhibition assay | IC50 = 3.36488 μM | SANGER | ||
| YH-13 | Growth Inhibition assay | IC50 = 3.44079 μM | SANGER | ||
| DU-145 | Growth Inhibition assay | IC50 = 3.46269 μM | SANGER | ||
| SW1088 | Growth Inhibition assay | IC50 = 3.4747 μM | SANGER | ||
| HOP-92 | Growth Inhibition assay | IC50 = 3.50342 μM | SANGER | ||
| KP-N-YS | Growth Inhibition assay | IC50 = 3.62139 μM | SANGER | ||
| NCI-H460 | Growth Inhibition assay | IC50 = 3.6673 μM | SANGER | ||
| U-2-OS | Growth Inhibition assay | IC50 = 3.72535 μM | SANGER | ||
| A101D | Growth Inhibition assay | IC50 = 3.76936 μM | SANGER | ||
| MDA-MB-231 | Growth Inhibition assay | IC50 = 3.81951 μM | SANGER | ||
| IST-MES1 | Growth Inhibition assay | IC50 = 3.832 μM | SANGER | ||
| COR-L105 | Growth Inhibition assay | IC50 = 4.018 μM | SANGER | ||
| NCI-H1437 | Growth Inhibition assay | IC50 = 4.02302 μM | SANGER | ||
| CAL-85-1 | Growth Inhibition assay | IC50 = 4.02461 μM | SANGER | ||
| MZ1-PC | Growth Inhibition assay | IC50 = 4.18556 μM | SANGER | ||
| VM-CUB-1 | Growth Inhibition assay | IC50 = 4.31284 μM | SANGER | ||
| CHL-1 | Growth Inhibition assay | IC50 = 4.32169 μM | SANGER | ||
| MDA-MB-361 | Growth Inhibition assay | IC50 = 4.33153 μM | SANGER | ||
| NCI-H661 | Growth Inhibition assay | IC50 = 4.50092 μM | SANGER | ||
| EW-11 | Growth Inhibition assay | IC50 = 4.52231 μM | SANGER | ||
| BEN | Growth Inhibition assay | IC50 = 4.52815 μM | SANGER | ||
| BFTC-909 | Growth Inhibition assay | IC50 = 4.56275 μM | SANGER | ||
| NCI-H2087 | Growth Inhibition assay | IC50 = 4.58164 μM | SANGER | ||
| RVH-421 | Growth Inhibition assay | IC50 = 4.6669 μM | SANGER | ||
| P30-OHK | Growth Inhibition assay | IC50 = 4.68008 μM | SANGER | ||
| NCI-H28 | Growth Inhibition assay | IC50 = 4.81661 μM | SANGER | ||
| ES6 | Growth Inhibition assay | IC50 = 4.83016 μM | SANGER | ||
| 769-P | Growth Inhibition assay | IC50 = 4.85926 μM | SANGER | ||
| OE33 | Growth Inhibition assay | IC50 = 4.88161 μM | SANGER | ||
| SW982 | Growth Inhibition assay | IC50 = 4.95061 μM | SANGER | ||
| A388 | Growth Inhibition assay | IC50 = 5.02983 μM | SANGER | ||
| TI-73 | Growth Inhibition assay | IC50 = 5.06194 μM | SANGER | ||
| HCT-116 | Growth Inhibition assay | IC50 = 5.09889 μM | SANGER | ||
| HuP-T3 | Growth Inhibition assay | IC50 = 5.18709 μM | SANGER | ||
| G-402 | Growth Inhibition assay | IC50 = 5.19416 μM | SANGER | ||
| NCI-H1792 | Growth Inhibition assay | IC50 = 5.24622 μM | SANGER | ||
| NCI-H209 | Growth Inhibition assay | IC50 = 5.25942 μM | SANGER | ||
| NCI-H1650 | Growth Inhibition assay | IC50 = 5.30634 μM | SANGER | ||
| LCLC-97TM1 | Growth Inhibition assay | IC50 = 5.31808 μM | SANGER | ||
| S-117 | Growth Inhibition assay | IC50 = 5.36976 μM | SANGER | ||
| GI-ME-N | Growth Inhibition assay | IC50 = 5.39681 μM | SANGER | ||
| NCI-H2122 | Growth Inhibition assay | IC50 = 5.49397 μM | SANGER | ||
| NCI-H1793 | Growth Inhibition assay | IC50 = 5.67593 μM | SANGER | ||
| C2BBe1 | Growth Inhibition assay | IC50 = 5.70088 μM | SANGER | ||
| TE-12 | Growth Inhibition assay | IC50 = 5.80556 μM | SANGER | ||
| LCLC-103H | Growth Inhibition assay | IC50 = 5.917 μM | SANGER | ||
| A673 | Growth Inhibition assay | IC50 = 5.91932 μM | SANGER | ||
| BB30-HNC | Growth Inhibition assay | IC50 = 5.9836 μM | SANGER | ||
| SF295 | Growth Inhibition assay | IC50 = 6.00422 μM | SANGER | ||
| KU-19-19 | Growth Inhibition assay | IC50 = 6.01731 μM | SANGER | ||
| CFPAC-1 | Growth Inhibition assay | IC50 = 6.04443 μM | SANGER | ||
| LoVo | Growth Inhibition assay | IC50 = 6.05063 μM | SANGER | ||
| 8505C | Growth Inhibition assay | IC50 = 6.07573 μM | SANGER | ||
| GMS-10 | Growth Inhibition assay | IC50 = 6.15002 μM | SANGER | ||
| Ca9-22 | Growth Inhibition assay | IC50 = 6.1671 μM | SANGER | ||
| DOK | Growth Inhibition assay | IC50 = 6.22072 μM | SANGER | ||
| FADU | Growth Inhibition assay | IC50 = 6.26039 μM | SANGER | ||
| BxPC-3 | Growth Inhibition assay | IC50 = 6.2732 μM | SANGER | ||
| CAL-33 | Growth Inhibition assay | IC50 = 6.29201 μM | SANGER | ||
| SHP-77 | Growth Inhibition assay | IC50 = 6.31512 μM | SANGER | ||
| LXF-289 | Growth Inhibition assay | IC50 = 6.33455 μM | SANGER | ||
| GB-1 | Growth Inhibition assay | IC50 = 6.382 μM | SANGER | ||
| KS-1 | Growth Inhibition assay | IC50 = 6.38447 μM | SANGER | ||
| D-502MG | Growth Inhibition assay | IC50 = 6.42376 μM | SANGER | ||
| LAN-6 | Growth Inhibition assay | IC50 = 6.51023 μM | SANGER | ||
| H-EMC-SS | Growth Inhibition assay | IC50 = 6.56147 μM | SANGER | ||
| LC-2-ad | Growth Inhibition assay | IC50 = 6.60076 μM | SANGER | ||
| NCI-H1693 | Growth Inhibition assay | IC50 = 6.62215 μM | SANGER | ||
| SK-N-FI | Growth Inhibition assay | IC50 = 6.75044 μM | SANGER | ||
| D-423MG | Growth Inhibition assay | IC50 = 6.76117 μM | SANGER | ||
| KNS-42 | Growth Inhibition assay | IC50 = 6.78197 μM | SANGER | ||
| GCT | Growth Inhibition assay | IC50 = 6.938 μM | SANGER | ||
| DSH1 | Growth Inhibition assay | IC50 = 7.0633 μM | SANGER | ||
| D-247MG | Growth Inhibition assay | IC50 = 7.07881 μM | SANGER | ||
| NCI-SNU-5 | Growth Inhibition assay | IC50 = 7.18371 μM | SANGER | ||
| TE-6 | Growth Inhibition assay | IC50 = 7.20601 μM | SANGER | ||
| NOMO-1 | Growth Inhibition assay | IC50 = 7.22127 μM | SANGER | ||
| NB17 | Growth Inhibition assay | IC50 = 7.30309 μM | SANGER | ||
| EW-22 | Growth Inhibition assay | IC50 = 7.34348 μM | SANGER | ||
| EW-13 | Growth Inhibition assay | IC50 = 7.35162 μM | SANGER | ||
| DOHH-2 | Growth Inhibition assay | IC50 = 7.4402 μM | SANGER | ||
| TGBC1TKB | Growth Inhibition assay | IC50 = 7.49899 μM | SANGER | ||
| GR-ST | Growth Inhibition assay | IC50 = 7.52594 μM | SANGER | ||
| KYSE-520 | Growth Inhibition assay | IC50 = 7.55515 μM | SANGER | ||
| CAPAN-1 | Growth Inhibition assay | IC50 = 7.5951 μM | SANGER | ||
| HCE-4 | Growth Inhibition assay | IC50 = 7.62279 μM | SANGER | ||
| MLMA | Growth Inhibition assay | IC50 = 7.62957 μM | SANGER | ||
| HT-144 | Growth Inhibition assay | IC50 = 7.65368 μM | SANGER | ||
| KYSE-180 | Growth Inhibition assay | IC50 = 7.71169 μM | SANGER | ||
| TE-5 | Growth Inhibition assay | IC50 = 7.95971 μM | SANGER | ||
| IGROV-1 | Growth Inhibition assay | IC50 = 7.98551 μM | SANGER | ||
| NCI-H1581 | Growth Inhibition assay | IC50 = 8.012 μM | SANGER | ||
| SW1990 | Growth Inhibition assay | IC50 = 8.04659 μM | SANGER | ||
| EFM-19 | Growth Inhibition assay | IC50 = 8.08545 μM | SANGER | ||
| IGR-1 | Growth Inhibition assay | IC50 = 8.43023 μM | SANGER | ||
| U-118-MG | Growth Inhibition assay | IC50 = 8.43463 μM | SANGER | ||
| SK-OV-3 | Growth Inhibition assay | IC50 = 8.46765 μM | SANGER | ||
| KNS-62 | Growth Inhibition assay | IC50 = 8.51761 μM | SANGER | ||
| GOTO | Growth Inhibition assay | IC50 = 8.57635 μM | SANGER | ||
| 8305C | Growth Inhibition assay | IC50 = 8.70484 μM | SANGER | ||
| RPMI-2650 | Growth Inhibition assay | IC50 = 8.71955 μM | SANGER | ||
| NEC8 | Growth Inhibition assay | IC50 = 8.74307 μM | SANGER | ||
| KYSE-450 | Growth Inhibition assay | IC50 = 8.86548 μM | SANGER | ||
| RMG-I | Growth Inhibition assay | IC50 = 9.14058 μM | SANGER | ||
| CAKI-1 | Growth Inhibition assay | IC50 = 9.31979 μM | SANGER | ||
| KYSE-510 | Growth Inhibition assay | IC50 = 9.35778 μM | SANGER | ||
| A4-Fuk | Growth Inhibition assay | IC50 = 9.36701 μM | SANGER | ||
| AN3-CA | Growth Inhibition assay | IC50 = 9.45444 μM | SANGER | ||
| SK-N-DZ | Growth Inhibition assay | IC50 = 9.72849 μM | SANGER | ||
| HSC-2 | Growth Inhibition assay | IC50 = 9.76629 μM | SANGER | ||
| EW-1 | Growth Inhibition assay | IC50 = 9.79369 μM | SANGER | ||
| D-566MG | Growth Inhibition assay | IC50 = 9.83664 μM | SANGER | ||
| COLO-792 | Growth Inhibition assay | IC50 = 9.98746 μM | SANGER | ||
| TE-10 | Growth Inhibition assay | IC50 = 10.0396 μM | SANGER | ||
| NCI-H650 | Growth Inhibition assay | IC50 = 10.4286 μM | SANGER | ||
| U-266 | Growth Inhibition assay | IC50 = 10.455 μM | SANGER | ||
| Detroit562 | Growth Inhibition assay | IC50 = 11.0515 μM | SANGER | ||
| NH-12 | Growth Inhibition assay | IC50 = 11.1446 μM | SANGER | ||
| OC-314 | Growth Inhibition assay | IC50 = 11.2842 μM | SANGER | ||
| IST-MEL1 | Growth Inhibition assay | IC50 = 11.5323 μM | SANGER | ||
| KNS-81-FD | Growth Inhibition assay | IC50 = 11.5527 μM | SANGER | ||
| SW1463 | Growth Inhibition assay | IC50 = 11.5989 μM | SANGER | ||
| NCI-H23 | Growth Inhibition assay | IC50 = 11.6553 μM | SANGER | ||
| SK-MEL-2 | Growth Inhibition assay | IC50 = 11.7197 μM | SANGER | ||
| NB13 | Growth Inhibition assay | IC50 = 12.1495 μM | SANGER | ||
| Daoy | Growth Inhibition assay | IC50 = 12.2855 μM | SANGER | ||
| NCI-H1623 | Growth Inhibition assay | IC50 = 12.3801 μM | SANGER | ||
| NMC-G1 | Growth Inhibition assay | IC50 = 12.717 μM | SANGER | ||
| DK-MG | Growth Inhibition assay | IC50 = 12.9482 μM | SANGER | ||
| TCCSUP | Growth Inhibition assay | IC50 = 13.1284 μM | SANGER | ||
| SCC-15 | Growth Inhibition assay | IC50 = 13.2651 μM | SANGER | ||
| NOS-1 | Growth Inhibition assay | IC50 = 13.2893 μM | SANGER | ||
| RH-1 | Growth Inhibition assay | IC50 = 13.3037 μM | SANGER | ||
| SK-MEL-3 | Growth Inhibition assay | IC50 = 13.3728 μM | SANGER | ||
| NB5 | Growth Inhibition assay | IC50 = 13.4067 μM | SANGER | ||
| SNU-387 | Growth Inhibition assay | IC50 = 13.5072 μM | SANGER | ||
| CAL-120 | Growth Inhibition assay | IC50 = 13.6718 μM | SANGER | ||
| LNCaP-Clone-FGC | Growth Inhibition assay | IC50 = 13.7991 μM | SANGER | ||
| ACN | Growth Inhibition assay | IC50 = 14.0288 μM | SANGER | ||
| SK-MEL-30 | Growth Inhibition assay | IC50 = 14.063 μM | SANGER | ||
| COLO-678 | Growth Inhibition assay | IC50 = 14.0822 μM | SANGER | ||
| SCC-9 | Growth Inhibition assay | IC50 = 14.1021 μM | SANGER | ||
| KINGS-1 | Growth Inhibition assay | IC50 = 14.1402 μM | SANGER | ||
| LS-513 | Growth Inhibition assay | IC50 = 14.187 μM | SANGER | ||
| HLE | Growth Inhibition assay | IC50 = 14.3852 μM | SANGER | ||
| SW1573 | Growth Inhibition assay | IC50 = 14.4435 μM | SANGER | ||
| KYSE-140 | Growth Inhibition assay | IC50 = 14.6327 μM | SANGER | ||
| SK-PN-DW | Growth Inhibition assay | IC50 = 14.8001 μM | SANGER | ||
| A253 | Growth Inhibition assay | IC50 = 15.0625 μM | SANGER | ||
| CAL-12T | Growth Inhibition assay | IC50 = 15.4662 μM | SANGER | ||
| COLO-679 | Growth Inhibition assay | IC50 = 15.7683 μM | SANGER | ||
| UACC-257 | Growth Inhibition assay | IC50 = 16.1201 μM | SANGER | ||
| U-87-MG | Growth Inhibition assay | IC50 = 16.3523 μM | SANGER | ||
| HCC1806 | Growth Inhibition assay | IC50 = 16.7071 μM | SANGER | ||
| NCI-H2170 | Growth Inhibition assay | IC50 = 17.2448 μM | SANGER | ||
| AGS | Growth Inhibition assay | IC50 = 17.3808 μM | SANGER | ||
| MEL-HO | Growth Inhibition assay | IC50 = 17.7503 μM | SANGER | ||
| SW48 | Growth Inhibition assay | IC50 = 17.7716 μM | SANGER | ||
| HuP-T4 | Growth Inhibition assay | IC50 = 18.0206 μM | SANGER | ||
| NCI-H720 | Growth Inhibition assay | IC50 = 18.1402 μM | SANGER | ||
| RCC10RGB | Growth Inhibition assay | IC50 = 18.1697 μM | SANGER | ||
| HD-MY-Z | Growth Inhibition assay | IC50 = 18.2254 μM | SANGER | ||
| A427 | Growth Inhibition assay | IC50 = 18.5094 μM | SANGER | ||
| HCC2998 | Growth Inhibition assay | IC50 = 18.6051 μM | SANGER | ||
| EPLC-272H | Growth Inhibition assay | IC50 = 19.0434 μM | SANGER | ||
| C32 | Growth Inhibition assay | IC50 = 19.045 μM | SANGER | ||
| UMC-11 | Growth Inhibition assay | IC50 = 19.2123 μM | SANGER | ||
| CaR-1 | Growth Inhibition assay | IC50 = 19.6804 μM | SANGER | ||
| KYSE-410 | Growth Inhibition assay | IC50 = 19.9139 μM | SANGER | ||
| HuCCT1 | Growth Inhibition assay | IC50 = 20.6293 μM | SANGER | ||
| LB996-RCC | Growth Inhibition assay | IC50 = 20.7168 μM | SANGER | ||
| KYSE-70 | Growth Inhibition assay | IC50 = 20.8059 μM | SANGER | ||
| CAL-72 | Growth Inhibition assay | IC50 = 20.915 μM | SANGER | ||
| Capan-2 | Growth Inhibition assay | IC50 = 21.0413 μM | SANGER | ||
| PANC-08-13 | Growth Inhibition assay | IC50 = 21.2515 μM | SANGER | ||
| SBC-1 | Growth Inhibition assay | IC50 = 21.3081 μM | SANGER | ||
| MFM-223 | Growth Inhibition assay | IC50 = 21.3342 μM | SANGER | ||
| BB49-HNC | Growth Inhibition assay | IC50 = 21.5716 μM | SANGER | ||
| SH-4 | Growth Inhibition assay | IC50 = 21.6618 μM | SANGER | ||
| HuO9 | Growth Inhibition assay | IC50 = 21.9825 μM | SANGER | ||
| AM-38 | Growth Inhibition assay | IC50 = 22.0485 μM | SANGER | ||
| A431 | Growth Inhibition assay | IC50 = 23.2119 μM | SANGER | ||
| YAPC | Growth Inhibition assay | IC50 = 23.2651 μM | SANGER | ||
| LU-139 | Growth Inhibition assay | IC50 = 23.4809 μM | SANGER | ||
| HEC-1 | Growth Inhibition assay | IC50 = 23.4937 μM | SANGER | ||
| SCC-25 | Growth Inhibition assay | IC50 = 24.3006 μM | SANGER | ||
| HT-29 | Growth Inhibition assay | IC50 = 24.3823 μM | SANGER | ||
| PC-14 | Growth Inhibition assay | IC50 = 24.6571 μM | SANGER | ||
| Calu-6 | Growth Inhibition assay | IC50 = 25.5071 μM | SANGER | ||
| SJRH30 | Growth Inhibition assay | IC50 = 25.6496 μM | SANGER | ||
| ChaGo-K-1 | Growth Inhibition assay | IC50 = 26.1629 μM | SANGER | ||
| IA-LM | Growth Inhibition assay | IC50 = 26.3645 μM | SANGER | ||
| GP5d | Growth Inhibition assay | IC50 = 26.4491 μM | SANGER | ||
| NCI-H2291 | Growth Inhibition assay | IC50 = 26.6541 μM | SANGER | ||
| BALL-1 | Growth Inhibition assay | IC50 = 26.9397 μM | SANGER | ||
| HCC1954 | Growth Inhibition assay | IC50 = 26.9808 μM | SANGER | ||
| NCI-H2452 | Growth Inhibition assay | IC50 = 27.4163 μM | SANGER | ||
| LU-99A | Growth Inhibition assay | IC50 = 27.5582 μM | SANGER | ||
| NTERA-S-cl-D1 | Growth Inhibition assay | IC50 = 27.7299 μM | SANGER | ||
| PANC-10-05 | Growth Inhibition assay | IC50 = 27.7775 μM | SANGER | ||
| NCI-H2405 | Growth Inhibition assay | IC50 = 27.9387 μM | SANGER | ||
| MDA-MB-415 | Growth Inhibition assay | IC50 = 28.4137 μM | SANGER | ||
| NCI-H2342 | Growth Inhibition assay | IC50 = 28.5281 μM | SANGER | ||
| TGBC24TKB | Growth Inhibition assay | IC50 = 28.7117 μM | SANGER | ||
| LU-134-A | Growth Inhibition assay | IC50 = 28.9261 μM | SANGER | ||
| SCC-4 | Growth Inhibition assay | IC50 = 31.0495 μM | SANGER | ||
| Saos-2 | Growth Inhibition assay | IC50 = 31.9306 μM | SANGER | ||
| RERF-LC-MS | Growth Inhibition assay | IC50 = 32.8231 μM | SANGER | ||
| M14 | Growth Inhibition assay | IC50 = 32.9764 μM | SANGER | ||
| HPAF-II | Growth Inhibition assay | IC50 = 33.5011 μM | SANGER | ||
| NCI-H1755 | Growth Inhibition assay | IC50 = 34.3305 μM | SANGER | ||
| D-392MG | Growth Inhibition assay | IC50 = 35.8674 μM | SANGER | ||
| A704 | Growth Inhibition assay | IC50 = 36.0427 μM | SANGER | ||
| CP50-MEL-B | Growth Inhibition assay | IC50 = 36.1911 μM | SANGER | ||
| EW-18 | Growth Inhibition assay | IC50 = 36.452 μM | SANGER | ||
| WM-115 | Growth Inhibition assay | IC50 = 36.8099 μM | SANGER | ||
| LU-65 | Growth Inhibition assay | IC50 = 37.1417 μM | SANGER | ||
| NCI-H1563 | Growth Inhibition assay | IC50 = 37.2484 μM | SANGER | ||
| DBTRG-05MG | Growth Inhibition assay | IC50 = 38.0691 μM | SANGER | ||
| NCI-H630 | Growth Inhibition assay | IC50 = 38.4714 μM | SANGER | ||
| NCI-H1155 | Growth Inhibition assay | IC50 = 39.242 μM | SANGER | ||
| OVCAR-3 | Growth Inhibition assay | IC50 = 39.9195 μM | SANGER | ||
| OAW-42 | Growth Inhibition assay | IC50 = 40.4258 μM | SANGER | ||
| JVM-2 | Growth Inhibition assay | IC50 = 41.2415 μM | SANGER | ||
| C3A | Growth Inhibition assay | IC50 = 41.3447 μM | SANGER | ||
| HT55 | Growth Inhibition assay | IC50 = 42.2841 μM | SANGER | ||
| OVCAR-4 | Growth Inhibition assay | IC50 = 42.2974 μM | SANGER | ||
| MEG-01 | Growth Inhibition assay | IC50 = 42.4616 μM | SANGER | ||
| NCI-H82 | Growth Inhibition assay | IC50 = 43.9892 μM | SANGER | ||
| JEG-3 | Growth Inhibition assay | IC50 = 44.947 μM | SANGER | ||
| BPH-1 | Growth Inhibition assay | IC50 = 46.3998 μM | SANGER | ||
| MPP-89 | Growth Inhibition assay | IC50 = 47.2898 μM | SANGER | ||
| ALL-PO | Growth Inhibition assay | IC50 = 47.4188 μM | SANGER | ||
| HT | Growth Inhibition assay | IC50 = 47.492 μM | SANGER | ||
| NCI-H2347 | Growth Inhibition assay | IC50 = 48.0715 μM | SANGER | ||
| A2780 | Growth Inhibition assay | IC50 = 49.4228 μM | SANGER | ||
| KARPAS-299 | Growth Inhibition assay | IC50 = 49.5119 μM | SANGER | ||
| NCI-H1651 | Growth Inhibition assay | IC50 = 49.8821 μM | SANGER | ||
| OCI-AML2 | Growth Inhibition assay | IC50 = 50.2084 μM | SANGER | ||
| OCUB-M | Growth Inhibition assay | IC50 = 50.3047 μM | SANGER | ||
| HuH-7 | Growth Inhibition assay | IC50 = 50.5943 μM | SANGER | ||
| RCM-1 | Growth Inhibition assay | IC50 = 50.9133 μM | SANGER | ||
| FTC-133 | Growth Inhibition assay | IC50 = 51.322 μM | SANGER | ||
| PSN1 | Growth Inhibition assay | IC50 = 51.4335 μM | SANGER | ||
| A498 | Growth Inhibition assay | IC50 = 52.0995 μM | SANGER | ||
| SF126 | Growth Inhibition assay | IC50 = 52.6568 μM | SANGER | ||
| UACC-62 | Growth Inhibition assay | IC50 = 55.2224 μM | SANGER | ||
| PANC-03-27 | Growth Inhibition assay | IC50 = 56.6788 μM | SANGER | ||
| NCI-H727 | Growth Inhibition assay | IC50 = 56.8127 μM | SANGER | ||
| SNU-423 | Growth Inhibition assay | IC50 = 57.2859 μM | SANGER | ||
| LB771-HNC | Growth Inhibition assay | IC50 = 57.8405 μM | SANGER | ||
| HCC1395 | Growth Inhibition assay | IC50 = 58.0464 μM | SANGER | ||
| OAW-28 | Growth Inhibition assay | IC50 = 58.2785 μM | SANGER | ||
| NB12 | Growth Inhibition assay | IC50 = 60.6696 μM | SANGER | ||
| DJM-1 | Growth Inhibition assay | IC50 = 60.7331 μM | SANGER | ||
| MDA-MB-157 | Growth Inhibition assay | IC50 = 61.1649 μM | SANGER | ||
| DU-4475 | Growth Inhibition assay | IC50 = 62.5495 μM | SANGER | ||
| RD | Growth Inhibition assay | IC50 = 62.7387 μM | SANGER | ||
| LS-123 | Growth Inhibition assay | IC50 = 63.2618 μM | SANGER | ||
| NCI-H226 | Growth Inhibition assay | IC50 = 64.22 μM | SANGER | ||
| MS-1 | Growth Inhibition assay | IC50 = 64.8358 μM | SANGER | ||
| no-10 | Growth Inhibition assay | IC50 = 65.7473 μM | SANGER | ||
| SW626 | Growth Inhibition assay | IC50 = 65.7579 μM | SANGER | ||
| DMS-273 | Growth Inhibition assay | IC50 = 66.2296 μM | SANGER | ||
| ESS-1 | Growth Inhibition assay | IC50 = 66.5096 μM | SANGER | ||
| TE-9 | Growth Inhibition assay | IC50 = 66.6316 μM | SANGER | ||
| CAS-1 | Growth Inhibition assay | IC50 = 67.7954 μM | SANGER | ||
| 639-V | Growth Inhibition assay | IC50 = 69.4198 μM | SANGER | ||
| GAK | Growth Inhibition assay | IC50 = 70.2031 μM | SANGER | ||
| NCI-H526 | Growth Inhibition assay | IC50 = 71.0913 μM | SANGER | ||
| DoTc2-4510 | Growth Inhibition assay | IC50 = 71.443 μM | SANGER | ||
| 647-V | Growth Inhibition assay | IC50 = 73.2118 μM | SANGER | ||
| OVCAR-8 | Growth Inhibition assay | IC50 = 73.2367 μM | SANGER | ||
| COLO-680N | Growth Inhibition assay | IC50 = 75.2497 μM | SANGER | ||
| HDLM-2 | Growth Inhibition assay | IC50 = 75.7806 μM | SANGER | ||
| TGBC11TKB | Growth Inhibition assay | IC50 = 79.0192 μM | SANGER | ||
| DMS-114 | Growth Inhibition assay | IC50 = 81.9577 μM | SANGER | ||
| CW-2 | Growth Inhibition assay | IC50 = 82.6818 μM | SANGER | ||
| MDA-MB-175-VII | Growth Inhibition assay | IC50 = 85.3135 μM | SANGER | ||
| HT-1376 | Growth Inhibition assay | IC50 = 85.846 μM | SANGER | ||
| SW1417 | Growth Inhibition assay | IC50 = 88.2906 μM | SANGER | ||
| HCE-T | Growth Inhibition assay | IC50 = 91.7205 μM | SANGER | ||
| OE19 | Growth Inhibition assay | IC50 = 92.7944 μM | SANGER | ||
| NCI-N87 | Growth Inhibition assay | IC50 = 92.8881 μM | SANGER | ||
| SNU-449 | Growth Inhibition assay | IC50 = 93.584 μM | SANGER | ||
| NCI-H1092 | Growth Inhibition assay | IC50 = 96.5851 μM | SANGER | ||
| COLO-684 | Growth Inhibition assay | IC50 = 99.0686 μM | SANGER | ||
| HCC1937 | Growth Inhibition assay | IC50 = 99.9315 μM | SANGER | ||
| EFO-21 | Growth Inhibition assay | IC50 = 110.988 μM | SANGER | ||
| ZR-75-30 | Growth Inhibition assay | IC50 = 114.117 μM | SANGER | ||
| HCC1187 | Growth Inhibition assay | IC50 = 114.179 μM | SANGER | ||
| SW684 | Growth Inhibition assay | IC50 = 114.655 μM | SANGER | ||
| AU565 | Growth Inhibition assay | IC50 = 115.892 μM | SANGER | ||
| HCC38 | Growth Inhibition assay | IC50 = 116.559 μM | SANGER | ||
| LK-2 | Growth Inhibition assay | IC50 = 119.652 μM | SANGER | ||
| LB2518-MEL | Growth Inhibition assay | IC50 = 122.428 μM | SANGER | ||
| COLO-320-HSR | Growth Inhibition assay | IC50 = 126.212 μM | SANGER | ||
| HCC1419 | Growth Inhibition assay | IC50 = 129.227 μM | SANGER | ||
| NCI-H2228 | Growth Inhibition assay | IC50 = 129.321 μM | SANGER | ||
| NCI-H2052 | Growth Inhibition assay | IC50 = 130.358 μM | SANGER | ||
| HCC2157 | Growth Inhibition assay | IC50 = 133.973 μM | SANGER | ||
| HCC1569 | Growth Inhibition assay | IC50 = 135.05 μM | SANGER | ||
| HuO-3N1 | Growth Inhibition assay | IC50 = 135.366 μM | SANGER | ||
| MZ7-mel | Growth Inhibition assay | IC50 = 145.604 μM | SANGER | ||
| SW756 | Growth Inhibition assay | IC50 = 147.143 μM | SANGER | ||
| NCI-H1304 | Growth Inhibition assay | IC50 = 149.222 μM | SANGER | ||
| LN-405 | Growth Inhibition assay | IC50 = 149.732 μM | SANGER | ||
| BT-474 | Growth Inhibition assay | IC50 = 150.969 μM | SANGER | ||
| LS-411N | Growth Inhibition assay | IC50 = 152.319 μM | SANGER | ||
| ATN-1 | Growth Inhibition assay | IC50 = 152.458 μM | SANGER | ||
| SNU-C2B | Growth Inhibition assay | IC50 = 153.444 μM | SANGER | ||
| KYSE-270 | Growth Inhibition assay | IC50 = 155.75 μM | SANGER | ||
| NCI-H1395 | Growth Inhibition assay | IC50 = 156.493 μM | SANGER | ||
| EKVX | Growth Inhibition assay | IC50 = 156.981 μM | SANGER | ||
| HCC70 | Growth Inhibition assay | IC50 = 157.989 μM | SANGER | ||
| NCI-H522 | Growth Inhibition assay | IC50 = 161.368 μM | SANGER | ||
| Ca-Ski | Growth Inhibition assay | IC50 = 161.86 μM | SANGER | ||
| SW1116 | Growth Inhibition assay | IC50 = 163.382 μM | SANGER | ||
| 8-MG-BA | Growth Inhibition assay | IC50 = 165.797 μM | SANGER | ||
| NCI-H1048 | Growth Inhibition assay | IC50 = 172.374 μM | SANGER | ||
| RH-18 | Growth Inhibition assay | IC50 = 172.601 μM | SANGER | ||
| LU-135 | Growth Inhibition assay | IC50 = 173.259 μM | SANGER | ||
| SW948 | Growth Inhibition assay | IC50 = 174.6 μM | SANGER | ||
| LS-1034 | Growth Inhibition assay | IC50 = 183.742 μM | SANGER | ||
| SCH | Growth Inhibition assay | IC50 = 187.022 μM | SANGER | ||
| KP-N-YN | Growth Inhibition assay | IC50 = 192.971 μM | SANGER | ||
| NCI-H69 | Growth Inhibition assay | IC50 = 210.925 μM | SANGER | ||
| SBC-5 | Growth Inhibition assay | IC50 = 211.162 μM | SANGER | ||
| MFE-280 | Growth Inhibition assay | IC50 = 212.067 μM | SANGER | ||
| MC116 | Growth Inhibition assay | IC50 = 212.736 μM | SANGER | ||
| BT-20 | Growth Inhibition assay | IC50 = 216.38 μM | SANGER | ||
| NCI-H1993 | Growth Inhibition assay | IC50 = 217.295 μM | SANGER | ||
| Calu-3 | Growth Inhibition assay | IC50 = 217.37 μM | SANGER | ||
| GCIY | Growth Inhibition assay | IC50 = 221.332 μM | SANGER | ||
| HT-3 | Growth Inhibition assay | IC50 = 222.173 μM | SANGER | ||
| MC-IXC | Growth Inhibition assay | IC50 = 227.215 μM | SANGER | ||
| COR-L88 | Growth Inhibition assay | IC50 = 234.259 μM | SANGER | ||
| SK-MEL-1 | Growth Inhibition assay | IC50 = 235.59 μM | SANGER | ||
| MDA-MB-453 | Growth Inhibition assay | IC50 = 236.33 μM | SANGER | ||
| SiHa | Growth Inhibition assay | IC50 = 247.22 μM | SANGER | ||
| C8166 | Growth Inhibition assay | IC50 = 251.341 μM | SANGER | ||
| SKG-IIIa | Growth Inhibition assay | IC50 = 251.504 μM | SANGER | ||
| HT-1197 | Growth Inhibition assay | IC50 = 268.492 μM | SANGER | ||
| no-11 | Growth Inhibition assay | IC50 = 291.357 μM | SANGER | ||
| ME-180 | Growth Inhibition assay | IC50 = 296.912 μM | SANGER | ||
| NY | Growth Inhibition assay | IC50 = 320.632 μM | SANGER | ||
| C-33-A | Growth Inhibition assay | IC50 = 325.06 μM | SANGER | ||
| NCI-H2029 | Growth Inhibition assay | IC50 = 338.305 μM | SANGER | ||
| IST-SL1 | Growth Inhibition assay | IC50 = 342.105 μM | SANGER | ||
| KLE | Growth Inhibition assay | IC50 = 347.29 μM | SANGER | ||
| SF539 | Growth Inhibition assay | IC50 = 348.01 μM | SANGER | ||
| 5637 | Growth Inhibition assay | IC50 = 360.37 μM | SANGER | ||
| COLO-824 | Growth Inhibition assay | IC50 = 363.58 μM | SANGER | ||
| NCI-H810 | Growth Inhibition assay | IC50 = 363.938 μM | SANGER | ||
| JAR | Growth Inhibition assay | IC50 = 365.01 μM | SANGER | ||
| L-428 | Growth Inhibition assay | IC50 = 369.277 μM | SANGER | ||
| COLO-668 | Growth Inhibition assay | IC50 = 387.033 μM | SANGER | ||
| GI-1 | Growth Inhibition assay | IC50 = 398.59 μM | SANGER | ||
| NCI-H446 | Growth Inhibition assay | IC50 = 399.497 μM | SANGER | ||
| CCRF-CEM | Growth Inhibition assay | IC50 = 403.587 μM | SANGER | ||
| T84 | Growth Inhibition assay | IC50 = 403.686 μM | SANGER | ||
| K-562 | Growth Inhibition assay | IC50 = 432.947 μM | SANGER | ||
| OMC-1 | Growth Inhibition assay | IC50 = 433.814 μM | SANGER | ||
| LB831-BLC | Growth Inhibition assay | IC50 = 434.556 μM | SANGER | ||
| BT-549 | Growth Inhibition assay | IC50 = 435.102 μM | SANGER | ||
| MKN7 | Growth Inhibition assay | IC50 = 439.822 μM | SANGER | ||
| SW1783 | Growth Inhibition assay | IC50 = 449.251 μM | SANGER | ||
| SNB75 | Growth Inhibition assay | IC50 = 486.478 μM | SANGER | ||
| M059J | Growth Inhibition assay | IC50 = 492.923 μM | SANGER | ||
| KURAMOCHI | Growth Inhibition assay | IC50 = 498.612 μM | SANGER | ||
| TE-1 | Growth Inhibition assay | IC50 = 502.729 μM | SANGER | ||
| NCI-H596 | Growth Inhibition assay | IC50 = 530.805 μM | SANGER | ||
| PFSK-1 | Growth Inhibition assay | IC50 = 532.941 μM | SANGER | ||
| sf9 | Function assay | Inhibition of CDK2/Cyclin E (unknown origin) expressed in sf9 cells using histone H1 as substrate in presence of [gamma33P]-ATP, IC50 = 9.2 μM. | 26851505 | ||
| sf9 | Function assay | Inhibition of CDK2/Cyclin E (unknown origin) expressed in sf9 cells using histone H1 as substrate in presence of [gamma33P]-ATP, IC50 = 9.2 μM. | 26851505 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 29435139 | ||
| Saos-2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 29435139 | ||
| BT-37 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 29435139 | ||
| RD | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 29435139 | ||
| SK-N-SH | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 29435139 | ||
| NB1643 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 29435139 | ||
| OHS-50 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 29435139 | ||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 29435139 | ||
| NB-EBc1 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 29435139 | ||
| LAN-5 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 29435139 | ||
| Rh18 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 29435139 | ||
| 點擊查看更多細胞系數據 | |||||
生物活性
| 產品描述 | Palbociclib Isethionate是一種高度選擇性的CDK4/6抑制劑，無細胞試驗中IC50為11 nM/16 nM，對CDK1/2/5，EGFR，FGFR，PDGFR， InsR等沒有抑制活性。Phase 3。 | ||||||
|---|---|---|---|---|---|---|---|
| 特性 | PD 0332991治療多種癌癥，特異性抑制CDK4/6，是第一種有前途的抑制劑。 | ||||||
| 靶點 |
|
| 體外研究(In Vitro) | ||||
| 體外研究活性 | PD 0332991對CDK4/6具有絕對選擇性，對其他CDKs幾乎沒有抑制活性。PD 0332991作用于MDA-MB-435乳腺癌細胞，有效降低Rb在Ser780 和 Ser795位點磷酸化，IC50分別為66 nM和63 nM。PD 0332991通過抑制細胞進入S期，有效抑制細胞生長，抑制 DNA復制。PD 0332991抑制胸苷滲透進Rb陽性人類乳腺癌(如MDA-MB-435, MCF-7), 結腸癌 (H1299), 和肺癌(Colo-205) 及白血病(CRRF-CEM和K562)的DNA中，IC50值為0.04-0.17 μM。PD 0332991顯著增強MDA-MB-453在G1期的百分比。[1]PD 0332991作用于CD138+原發(fā)性骨髓瘤細胞，初級非轉化的B細胞，MM1.S和CAG HMCLs細胞系，抑制Rb磷酸化，IC50分別為 <0.1 μM, 0.05 μM, 和 60-70 nM。PD 0332991作用于CD138+原發(fā)性骨髓瘤細胞和初級非轉化的B細胞，誘導細胞停滯在G1期。PD 0332991誘導MM1.S細胞停滯在G1期，IC50為~0.05 μM。[2]PD 0332991優(yōu)先抑制Luminal雌激素受體陽性(包括HER2陽性)人類乳腺癌細胞系。PD 0332991作用于大部分敏感的細胞系，促進pRb和cyclin D1基因表達，且降低CDKN2A(p16)基因表達。PD 0332991作用于條件性抗ER抑制的細胞系，增強對Tamoxifen的敏感性。[3] | |||
|---|---|---|---|---|
| 激酶實驗 | CDK活性實驗 | |||
| 在96孔過濾板中進行動力學測評，測定CDK實驗的IC50值。所有的CDK-cyclin激酶復合物在昆蟲細胞中通過桿狀病毒感染而表達，并進行純化。實驗底物是與GST(GST?RB-Cterm)融合的pRb組分(792–928位氨基酸)?？偡磻w積為0.1 mL，包含終濃度20 mM Tris-HCl,pH 7.4, 50 mM NaCl,1 mM 二硫蘇糖醇,10 mM MgCl2，含0.25 μCi[γ-32P]ATP的25 μM ATP(作用于 CDK4-cyclin D1, CDK6-cyclin D2, 和 CDK6-cyclin D3), 20 ng 酶, 1 μg GST?RB-Cterm, 及適度稀釋的抑制劑。每孔加入全部組分，除了[γ-32P]ATP，置于混合器中2分鐘。加入[γ-32P]ATP開始反應,在25°C下溫育15分鐘。加入0.1 mL 20% 三氯乙酸終止反應, 實驗板置于4°C至少1小時，使底物沉淀。每孔使用 0.2 mL 10%三氯乙酸洗滌 五次，使用β計數器測定滲透的放射性。 | ||||
| 細胞實驗 | 細胞系 | 人類乳腺癌細胞MDA-MB-435 | ||
| 濃度 | 2 μM | |||
| 孵育時間 | 6 天 | |||
| 方法 | 細胞按一式兩份每孔5,000 到10,000個細胞接種在24孔板中，接種后，加入不同濃度的PD 0332991。對照組不加入藥物。溫育末期，細胞胰蛋白酶化，并置于等滲溶液中，并立即使用Coulter Z2粒子計數器計數。 | |||
| 實驗圖片 | 檢測方法 | 檢測指標 | 實驗圖片 | PMID |
| Western blot | RB1 (pT821) / RB1 (pS780) pAMPKα(T172) / AMPKα pULK1(S317) / ULK1 c-Jun / p-c-Jun / NFκB(p50) p38 / p-P38 / JNK / p-JNK |
|
30300583 | |
| Growth inhibition assay | Cell viability IC50 |
|
28453226 | |
| Immunofluorescence | γH2AX(Ser139) LC3B |
|
29669860 | |
| ELISA | PGE2 |
|
26540629 | |
| 體內研究(In Vivo) | ||
| 體內研究活性 | PD 0332991(150 mg/kg)作用于Colo-205結腸癌移植瘤，誘導腫瘤快速衰退，腫瘤生長相應延遲。PD 0332991(150 mg/kg)作用于MDA-MB-435乳腺癌，誘導全部腫瘤停滯和殺死細胞。PD 0332991(150 mg/kg)處理攜帶SF-295膠質母細胞瘤，和ZR-75-1乳腺癌和PC-3前列腺腫瘤模型(完全抑制腫瘤生長)的小鼠，顯著誘導腫瘤衰退。PD 0332991 (150 mg/kg)處理 MDA-MB-435乳腺癌超過24小時，抑制Rb在Ser780位點磷酸化。PD 0332991(150 mg/kg)處理Colo-205 移植瘤，下調四種E2F調節(jié)的基因CDC2, CCNE2, TK1, 和 TOP2A表達。[1]PD 0332991也快速抑制骨髓瘤生長。[2] | |
|---|---|---|
| 動物實驗 | Animal Models | 人類結腸癌移植瘤Colo-205 |
| Dosages | 150 mg/kg | |
| Administration | 每天口服處理 | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT05665361 | Recruiting | Advanced Clear Cell Renal Carcinoma (Ccrcc)|Papillary Renal Cell Carcinoma (Prcc) |
National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) |
April 24 2024 | Phase 1|Phase 2 |
| NCT06307457 | Completed | Breast Cancer |
Pfizer |
March 11 2024 | -- |
| NCT05709158 | Not yet recruiting | Breast Cancer |
Pfizer |
March 1 2024 | -- |
| NCT05912933 | Not yet recruiting | Breast Cancer |
Pfizer |
March 1 2024 | -- |
化學信息&溶解度
| 分子量 | 573.66 | 分子式 | C24H29N7O2.C2H6O4S |
| CAS號 | 827022-33-3 | SDF | Download Palbociclib Isethionate SDF |
| Smiles | CC1=C(C(=O)N(C2=NC(=NC=C12)NC3=NC=C(C=C3)N4CCNCC4)C5CCCC5)C(=O)C.C(CS(=O)(=O)O)O | ||
| 儲存條件(自收到貨起) | |||
|
體外溶解度 |
Water : 100 mg/mL (174.31 mM) DMSO : Insoluble ( ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO) Ethanol : Insoluble |
摩爾濃度計算器 |
|
體內溶解度 現配現用，請按從左到右的順序依次添加，澄清后再加入下一溶劑 |
動物體內配方計算器 | ||||
實驗計算
動物體內配方計算器（澄清溶液）
第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）
mg/kg
g
μL
只
第二步：請輸入動物體內配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯系Selleck為您提供正確的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計算結果：
工作液濃度： mg/ml；
DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯系Selleck）；
體內配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。
體內配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。
注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。
技術支持
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如果有其他問題，請給我們留言。
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常見問題及建議解決方法
問題 1:
What is the best vehicle for palbociclib for in vitro and in vivo?
回答：
You can use water for vitro use and Saline for vivo use.
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