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RO-3306是一種ATP競爭性的選擇性 CDK1 抑制劑,Ki 為20 nM,選擇性是其他各種人類激酶的15倍多。RO-3306可增強p53介導(dǎo)的 Bax 激活和線粒體的凋亡。
Ro-3306 Chemical Structure
CAS: 872573-93-8
細胞系 | 實驗類型 | 給藥濃度 | 孵育時間 | 活性描述 | 文獻信息 |
---|---|---|---|---|---|
human HCT116 cells | Cytotoxic?assay | 5 days | Cytotoxicity against human HCT116 cells after 5 days by MTS assay, IC50=3.2 μM | 22326168 | |
A172 | Growth inhibition assay | Inhibition of human A172 cell growth in a cell viability assay, IC50 = 5.9079 μM. | SANGER | ||
PFSK-1 | Growth inhibition assay | Inhibition of human PFSK-1 cell growth in a cell viability assay, IC50 = 5.86168 μM. | SANGER | ||
GCT | Growth inhibition assay | Inhibition of human GCT cell growth in a cell viability assay, IC50 = 5.85121 μM. | SANGER | ||
HGC-27 | Growth inhibition assay | Inhibition of human HGC-27 cell growth in a cell viability assay, IC50 = 5.73077 μM. | SANGER | ||
KP-4 | Growth inhibition assay | Inhibition of human KP-4 cell growth in a cell viability assay, IC50 = 5.69823 μM. | SANGER | ||
NCI-H1792 | Growth inhibition assay | Inhibition of human NCI-H1792 cell growth in a cell viability assay, IC50 = 5.47954 μM. | SANGER | ||
GAMG | Growth inhibition assay | Inhibition of human GAMG cell growth in a cell viability assay, IC50 = 5.3715 μM. | SANGER | ||
NB13 | Growth inhibition assay | Inhibition of human NB13 cell growth in a cell viability assay, IC50 = 5.32786 μM. | SANGER | ||
SK-MEL-2 | Growth inhibition assay | Inhibition of human SK-MEL-2 cell growth in a cell viability assay, IC50 = 5.09632 μM. | SANGER | ||
YH-13 | Growth inhibition assay | Inhibition of human YH-13 cell growth in a cell viability assay, IC50 = 4.75776 μM. | SANGER | ||
NCI-H2405 | Growth inhibition assay | Inhibition of human NCI-H2405 cell growth in a cell viability assay, IC50 = 4.74493 μM. | SANGER | ||
NEC8 | Growth inhibition assay | Inhibition of human NEC8 cell growth in a cell viability assay, IC50 = 4.47076 μM. | SANGER | ||
MN-60 | Growth inhibition assay | Inhibition of human MN-60 cell growth in a cell viability assay, IC50 = 4.37623 μM. | SANGER | ||
LXF-289 | Growth inhibition assay | Inhibition of human LXF-289 cell growth in a cell viability assay, IC50 = 4.2176 μM. | SANGER | ||
PSN1 | Growth inhibition assay | Inhibition of human PSN1 cell growth in a cell viability assay, IC50 = 4.10805 μM. | SANGER | ||
COR-L88 | Growth inhibition assay | Inhibition of human COR-L88 cell growth in a cell viability assay, IC50 = 3.47583 μM. | SANGER | ||
KOSC-2 | Growth inhibition assay | Inhibition of human KOSC-2 cell growth in a cell viability assay, IC50 = 3.44662 μM. | SANGER | ||
LB1047-RCC | Growth inhibition assay | Inhibition of human LB1047-RCC cell growth in a cell viability assay, IC50 = 3.23501 μM. | SANGER | ||
8-MG-BA | Growth inhibition assay | Inhibition of human 8-MG-BA cell growth in a cell viability assay, IC50 = 3.14049 μM. | SANGER | ||
5637 | Growth inhibition assay | Inhibition of human 5637 cell growth in a cell viability assay, IC50 = 3.08532 μM. | SANGER | ||
BPH-1 | Growth inhibition assay | Inhibition of human BPH-1 cell growth in a cell viability assay, IC50 = 2.97455 μM. | SANGER | ||
UM-UC-3 | Growth inhibition assay | Inhibition of human UM-UC-3 cell growth in a cell viability assay, IC50 = 2.73936 μM. | SANGER | ||
Hs-578-T | Growth inhibition assay | Inhibition of human Hs-578-T cell growth in a cell viability assay, IC50 = 2.27799 μM. | SANGER | ||
639-V | Growth inhibition assay | Inhibition of human 639-V cell growth in a cell viability assay, IC50 = 2.27537 μM. | SANGER | ||
A4-Fuk | Growth inhibition assay | Inhibition of human A4-Fuk cell growth in a cell viability assay, IC50 = 2.05604 μM. | SANGER | ||
SK-N-DZ | Growth inhibition assay | Inhibition of human SK-N-DZ cell growth in a cell viability assay, IC50 = 2.01876 μM. | SANGER | ||
ALL-PO | Growth inhibition assay | Inhibition of human ALL-PO cell growth in a cell viability assay, IC50 = 1.90813 μM. | SANGER | ||
U251 | Growth inhibition assay | Inhibition of human U251 cell growth in a cell viability assay, IC50 = 1.63771 μM. | SANGER | ||
SW1710 | Growth inhibition assay | Inhibition of human SW1710 cell growth in a cell viability assay, IC50 = 1.61408 μM. | SANGER | ||
T98G | Growth inhibition assay | Inhibition of human T98G cell growth in a cell viability assay, IC50 = 1.36812 μM. | SANGER | ||
PA-1 | Growth inhibition assay | Inhibition of human PA-1 cell growth in a cell viability assay, IC50 = 1.22654 μM. | SANGER | ||
H4 | Growth inhibition assay | Inhibition of human H4 cell growth in a cell viability assay, IC50 = 1.15875 μM. | SANGER | ||
NCI-SNU-1 | Growth inhibition assay | Inhibition of human NCI-SNU-1 cell growth in a cell viability assay, IC50 = 0.73095 μM. | SANGER | ||
human SJSA1 cells | Proliferation assay | Antiproliferative activity against human SJSA1 cells, IC50=4.55 μM | 17303421 | ||
human SW480 cells | Proliferation assay | Antiproliferative activity against human SW480 cells, IC50=2.2 μM | 17303421 | ||
human RKO cells | Proliferation assay | Antiproliferative activity against human RKO cells, IC50=2 μM | 17303421 | ||
human HCT116 cells | Proliferation assay | Antiproliferative activity against human HCT116 cells, IC50=1.14 μM | 17303421 | ||
human MDA435 cells | Proliferation assay | Antiproliferative activity against human MDA435 cells, IC50=1.14 μM | 17303421 | ||
human H460a cells | Proliferation assay | Antiproliferative activity against human H460a cells, IC50=1.04 μM | 17303421 | ||
KB-3-1 adenocarcinoma cell line | qHTS assay | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 31515284 | ||
HO-1-N-1 | Growth inhibition assay | Inhibition of human HO-1-N-1 cell growth in a cell viability assay, IC50 = 5.95425 μM. | SANGER | ||
HN | Growth inhibition assay | Inhibition of human HN cell growth in a cell viability assay, IC50 = 5.97097 μM. | SANGER | ||
IST-MES1 | Growth inhibition assay | Inhibition of human IST-MES1 cell growth in a cell viability assay, IC50 = 5.97521 μM. | SANGER | ||
TGW | Growth inhibition assay | Inhibition of human TGW cell growth in a cell viability assay, IC50 = 6.05682 μM. | SANGER | ||
COR-L23 | Growth inhibition assay | Inhibition of human COR-L23 cell growth in a cell viability assay, IC50 = 6.3735 μM. | SANGER | ||
D-566MG | Growth inhibition assay | Inhibition of human D-566MG cell growth in a cell viability assay, IC50 = 6.78873 μM. | SANGER | ||
SKG-IIIa | Growth inhibition assay | Inhibition of human SKG-IIIa cell growth in a cell viability assay, IC50 = 6.85572 μM. | SANGER | ||
NCI-H446 | Growth inhibition assay | Inhibition of human NCI-H446 cell growth in a cell viability assay, IC50 = 7.0181 μM. | SANGER | ||
KYSE-270 | Growth inhibition assay | Inhibition of human KYSE-270 cell growth in a cell viability assay, IC50 = 7.03872 μM. | SANGER | ||
CAL-39 | Growth inhibition assay | Inhibition of human CAL-39 cell growth in a cell viability assay, IC50 = 7.3524 μM. | SANGER | ||
IST-SL1 | Growth inhibition assay | Inhibition of human IST-SL1 cell growth in a cell viability assay, IC50 = 7.43349 μM. | SANGER | ||
SF539 | Growth inhibition assay | Inhibition of human SF539 cell growth in a cell viability assay, IC50 = 7.55197 μM. | SANGER | ||
TE-1 | Growth inhibition assay | Inhibition of human TE-1 cell growth in a cell viability assay, IC50 = 7.89091 μM. | SANGER | ||
NB10 | Growth inhibition assay | Inhibition of human NB10 cell growth in a cell viability assay, IC50 = 7.98758 μM. | SANGER | ||
8505C | Growth inhibition assay | Inhibition of human 8505C cell growth in a cell viability assay, IC50 = 7.99817 μM. | SANGER | ||
DB | Growth inhibition assay | Inhibition of human DB cell growth in a cell viability assay, IC50 = 8.01131 μM. | SANGER | ||
NCI-H28 | Growth inhibition assay | Inhibition of human NCI-H28 cell growth in a cell viability assay, IC50 = 8.59884 μM. | SANGER | ||
LOXIMVI | Growth inhibition assay | Inhibition of human LOXIMVI cell growth in a cell viability assay, IC50 = 8.63701 μM. | SANGER | ||
ME-180 | Growth inhibition assay | Inhibition of human ME-180 cell growth in a cell viability assay, IC50 = 8.80395 μM. | SANGER | ||
ES3 | Growth inhibition assay | Inhibition of human ES3 cell growth in a cell viability assay, IC50 = 9.12794 μM. | SANGER | ||
SK-N-FI | Growth inhibition assay | Inhibition of human SK-N-FI cell growth in a cell viability assay, IC50 = 9.41699 μM. | SANGER | ||
NBsusSR | Growth inhibition assay | Inhibition of human NBsusSR cell growth in a cell viability assay, IC50 = 10.2318 μM. | SANGER | ||
GI-ME-N | Growth inhibition assay | Inhibition of human GI-ME-N cell growth in a cell viability assay, IC50 = 10.2783 μM. | SANGER | ||
A704 | Growth inhibition assay | Inhibition of human A704 cell growth in a cell viability assay, IC50 = 10.3318 μM. | SANGER | ||
HuP-T4 | Growth inhibition assay | Inhibition of human HuP-T4 cell growth in a cell viability assay, IC50 = 10.4271 μM. | SANGER | ||
A101D | Growth inhibition assay | Inhibition of human A101D cell growth in a cell viability assay, IC50 = 11.1574 μM. | SANGER | ||
MCF7 | Growth inhibition assay | Inhibition of human MCF7 cell growth in a cell viability assay, IC50 = 11.1849 μM. | SANGER | ||
A549 | Growth inhibition assay | Inhibition of human A549 cell growth in a cell viability assay, IC50 = 11.206 μM. | SANGER | ||
HD-MY-Z | Growth inhibition assay | Inhibition of human HD-MY-Z cell growth in a cell viability assay, IC50 = 11.206 μM. | SANGER | ||
HCC1395 | Growth inhibition assay | Inhibition of human HCC1395 cell growth in a cell viability assay, IC50 = 11.5596 μM. | SANGER | ||
SK-NEP-1 | Growth inhibition assay | Inhibition of human SK-NEP-1 cell growth in a cell viability assay, IC50 = 11.7332 μM. | SANGER | ||
HSC-2 | Growth inhibition assay | Inhibition of human HSC-2 cell growth in a cell viability assay, IC50 = 11.7842 μM. | SANGER | ||
HCC1937 | Growth inhibition assay | Inhibition of human HCC1937 cell growth in a cell viability assay, IC50 = 11.8473 μM. | SANGER | ||
RS4-11 | Growth inhibition assay | Inhibition of human RS4-11 cell growth in a cell viability assay, IC50 = 11.8836 μM. | SANGER | ||
CAL-27 | Growth inhibition assay | Inhibition of human CAL-27 cell growth in a cell viability assay, IC50 = 12.1637 μM. | SANGER | ||
NCI-H23 | Growth inhibition assay | Inhibition of human NCI-H23 cell growth in a cell viability assay, IC50 = 12.4155 μM. | SANGER | ||
A431 | Growth inhibition assay | Inhibition of human A431 cell growth in a cell viability assay, IC50 = 12.7233 μM. | SANGER | ||
HT-1080 | Growth inhibition assay | Inhibition of human HT-1080 cell growth in a cell viability assay, IC50 = 12.7373 μM. | SANGER | ||
GB-1 | Growth inhibition assay | Inhibition of human GB-1 cell growth in a cell viability assay, IC50 = 12.7716 μM. | SANGER | ||
BFTC-909 | Growth inhibition assay | Inhibition of human BFTC-909 cell growth in a cell viability assay, IC50 = 13.1068 μM. | SANGER | ||
CAL-33 | Growth inhibition assay | Inhibition of human CAL-33 cell growth in a cell viability assay, IC50 = 13.6518 μM. | SANGER | ||
JVM-3 | Growth inhibition assay | Inhibition of human JVM-3 cell growth in a cell viability assay, IC50 = 14.2627 μM. | SANGER | ||
AN3-CA | Growth inhibition assay | Inhibition of human AN3-CA cell growth in a cell viability assay, IC50 = 14.9578 μM. | SANGER | ||
VM-CUB-1 | Growth inhibition assay | Inhibition of human VM-CUB-1 cell growth in a cell viability assay, IC50 = 15.1364 μM. | SANGER | ||
A253 | Growth inhibition assay | Inhibition of human A253 cell growth in a cell viability assay, IC50 = 15.2834 μM. | SANGER | ||
RPMI-7951 | Growth inhibition assay | Inhibition of human RPMI-7951 cell growth in a cell viability assay, IC50 = 16.1981 μM. | SANGER | ||
NCI-H1563 | Growth inhibition assay | Inhibition of human NCI-H1563 cell growth in a cell viability assay, IC50 = 16.8253 μM. | SANGER | ||
LB831-BLC | Growth inhibition assay | Inhibition of human LB831-BLC cell growth in a cell viability assay, IC50 = 17.1929 μM. | SANGER | ||
ES8 | Growth inhibition assay | Inhibition of human ES8 cell growth in a cell viability assay, IC50 = 17.3157 μM. | SANGER | ||
NCI-H292 | Growth inhibition assay | Inhibition of human NCI-H292 cell growth in a cell viability assay, IC50 = 17.4749 μM. | SANGER | ||
OAW-42 | Growth inhibition assay | Inhibition of human OAW-42 cell growth in a cell viability assay, IC50 = 17.8823 μM. | SANGER | ||
RCC10RGB | Growth inhibition assay | Inhibition of human RCC10RGB cell growth in a cell viability assay, IC50 = 17.9578 μM. | SANGER | ||
PC-3 | Growth inhibition assay | Inhibition of human PC-3 cell growth in a cell viability assay, IC50 = 18.0043 μM. | SANGER | ||
HCC38 | Growth inhibition assay | Inhibition of human HCC38 cell growth in a cell viability assay, IC50 = 18.1031 μM. | SANGER | ||
DEL | Growth inhibition assay | Inhibition of human DEL cell growth in a cell viability assay, IC50 = 18.387 μM. | SANGER | ||
ABC-1 | Growth inhibition assay | Inhibition of human ABC-1 cell growth in a cell viability assay, IC50 = 18.5627 μM. | SANGER | ||
SW756 | Growth inhibition assay | Inhibition of human SW756 cell growth in a cell viability assay, IC50 = 19.1351 μM. | SANGER | ||
TE-6 | Growth inhibition assay | Inhibition of human TE-6 cell growth in a cell viability assay, IC50 = 19.2103 μM. | SANGER | ||
H-EMC-SS | Growth inhibition assay | Inhibition of human H-EMC-SS cell growth in a cell viability assay, IC50 = 19.4359 μM. | SANGER | ||
HCT-116 | Growth inhibition assay | Inhibition of human HCT-116 cell growth in a cell viability assay, IC50 = 19.668 μM. | SANGER | ||
CHP-212 | Growth inhibition assay | Inhibition of human CHP-212 cell growth in a cell viability assay, IC50 = 19.7478 μM. | SANGER | ||
SK-LU-1 | Growth inhibition assay | Inhibition of human SK-LU-1 cell growth in a cell viability assay, IC50 = 19.753 μM. | SANGER | ||
HT-3 | Growth inhibition assay | Inhibition of human HT-3 cell growth in a cell viability assay, IC50 = 20.028 μM. | SANGER | ||
KG-1 | Growth inhibition assay | Inhibition of human KG-1 cell growth in a cell viability assay, IC50 = 20.206 μM. | SANGER | ||
ES1 | Growth inhibition assay | Inhibition of human ES1 cell growth in a cell viability assay, IC50 = 21.0048 μM. | SANGER | ||
Ramos-2G6-4C10 | Growth inhibition assay | Inhibition of human Ramos-2G6-4C10 cell growth in a cell viability assay, IC50 = 21.7756 μM. | SANGER | ||
IA-LM | Growth inhibition assay | Inhibition of human IA-LM cell growth in a cell viability assay, IC50 = 21.9694 μM. | SANGER | ||
BHT-101 | Growth inhibition assay | Inhibition of human BHT-101 cell growth in a cell viability assay, IC50 = 22.0629 μM. | SANGER | ||
OVCAR-4 | Growth inhibition assay | Inhibition of human OVCAR-4 cell growth in a cell viability assay, IC50 = 22.47 μM. | SANGER | ||
SW1573 | Growth inhibition assay | Inhibition of human SW1573 cell growth in a cell viability assay, IC50 = 22.7934 μM. | SANGER | ||
CHL-1 | Growth inhibition assay | Inhibition of human CHL-1 cell growth in a cell viability assay, IC50 = 23.2833 μM. | SANGER | ||
BFTC-905 | Growth inhibition assay | Inhibition of human BFTC-905 cell growth in a cell viability assay, IC50 = 23.2892 μM. | SANGER | ||
TE-12 | Growth inhibition assay | Inhibition of human TE-12 cell growth in a cell viability assay, IC50 = 23.5782 μM. | SANGER | ||
NCI-H358 | Growth inhibition assay | Inhibition of human NCI-H358 cell growth in a cell viability assay, IC50 = 23.6477 μM. | SANGER | ||
OVCAR-5 | Growth inhibition assay | Inhibition of human OVCAR-5 cell growth in a cell viability assay, IC50 = 24.104 μM. | SANGER | ||
CGTH-W-1 | Growth inhibition assay | Inhibition of human CGTH-W-1 cell growth in a cell viability assay, IC50 = 25.0804 μM. | SANGER | ||
SNU-423 | Growth inhibition assay | Inhibition of human SNU-423 cell growth in a cell viability assay, IC50 = 25.366 μM. | SANGER | ||
CP50-MEL-B | Growth inhibition assay | Inhibition of human CP50-MEL-B cell growth in a cell viability assay, IC50 = 25.7399 μM. | SANGER | ||
NCI-H2087 | Growth inhibition assay | Inhibition of human NCI-H2087 cell growth in a cell viability assay, IC50 = 25.8655 μM. | SANGER | ||
RMG-I | Growth inhibition assay | Inhibition of human RMG-I cell growth in a cell viability assay, IC50 = 25.9219 μM. | SANGER | ||
KP-N-YS | Growth inhibition assay | Inhibition of human KP-N-YS cell growth in a cell viability assay, IC50 = 26.202 μM. | SANGER | ||
OMC-1 | Growth inhibition assay | Inhibition of human OMC-1 cell growth in a cell viability assay, IC50 = 26.508 μM. | SANGER | ||
DMS-114 | Growth inhibition assay | Inhibition of human DMS-114 cell growth in a cell viability assay, IC50 = 27.3966 μM. | SANGER | ||
SHP-77 | Growth inhibition assay | Inhibition of human SHP-77 cell growth in a cell viability assay, IC50 = 27.488 μM. | SANGER | ||
MPP-89 | Growth inhibition assay | Inhibition of human MPP-89 cell growth in a cell viability assay, IC50 = 27.9438 μM. | SANGER | ||
NCI-H1581 | Growth inhibition assay | Inhibition of human NCI-H1581 cell growth in a cell viability assay, IC50 = 28.4535 μM. | SANGER | ||
D-283MED | Growth inhibition assay | Inhibition of human D-283MED cell growth in a cell viability assay, IC50 = 28.4674 μM. | SANGER | ||
MOLT-4 | Growth inhibition assay | Inhibition of human MOLT-4 cell growth in a cell viability assay, IC50 = 28.9072 μM. | SANGER | ||
ES6 | Growth inhibition assay | Inhibition of human ES6 cell growth in a cell viability assay, IC50 = 29.6436 μM. | SANGER | ||
NB6 | Growth inhibition assay | Inhibition of human NB6 cell growth in a cell viability assay, IC50 = 29.8638 μM. | SANGER | ||
SW954 | Growth inhibition assay | Inhibition of human SW954 cell growth in a cell viability assay, IC50 = 29.9407 μM. | SANGER | ||
A388 | Growth inhibition assay | Inhibition of human A388 cell growth in a cell viability assay, IC50 = 29.9422 μM. | SANGER | ||
OAW-28 | Growth inhibition assay | Inhibition of human OAW-28 cell growth in a cell viability assay, IC50 = 30.2278 μM. | SANGER | ||
SK-MES-1 | Growth inhibition assay | Inhibition of human SK-MES-1 cell growth in a cell viability assay, IC50 = 31.2208 μM. | SANGER | ||
NCI-H441 | Growth inhibition assay | Inhibition of human NCI-H441 cell growth in a cell viability assay, IC50 = 31.9868 μM. | SANGER | ||
HOP-92 | Growth inhibition assay | Inhibition of human HOP-92 cell growth in a cell viability assay, IC50 = 32.2356 μM. | SANGER | ||
NB14 | Growth inhibition assay | Inhibition of human NB14 cell growth in a cell viability assay, IC50 = 32.7251 μM. | SANGER | ||
MS-1 | Growth inhibition assay | Inhibition of human MS-1 cell growth in a cell viability assay, IC50 = 32.7604 μM. | SANGER | ||
YKG-1 | Growth inhibition assay | Inhibition of human YKG-1 cell growth in a cell viability assay, IC50 = 32.8336 μM. | SANGER | ||
SiHa | Growth inhibition assay | Inhibition of human SiHa cell growth in a cell viability assay, IC50 = 33.3829 μM. | SANGER | ||
HAL-01 | Growth inhibition assay | Inhibition of human HAL-01 cell growth in a cell viability assay, IC50 = 34.2376 μM. | SANGER | ||
Ca-Ski | Growth inhibition assay | Inhibition of human Ca-Ski cell growth in a cell viability assay, IC50 = 34.7669 μM. | SANGER | ||
NCI-H747 | Growth inhibition assay | Inhibition of human NCI-H747 cell growth in a cell viability assay, IC50 = 34.9875 μM. | SANGER | ||
KYSE-510 | Growth inhibition assay | Inhibition of human KYSE-510 cell growth in a cell viability assay, IC50 = 35.6485 μM. | SANGER | ||
A204 | Growth inhibition assay | Inhibition of human A204 cell growth in a cell viability assay, IC50 = 35.7209 μM. | SANGER | ||
HSC-3 | Growth inhibition assay | Inhibition of human HSC-3 cell growth in a cell viability assay, IC50 = 36.0086 μM. | SANGER | ||
HuP-T3 | Growth inhibition assay | Inhibition of human HuP-T3 cell growth in a cell viability assay, IC50 = 36.4832 μM. | SANGER | ||
RPMI-8226 | Growth inhibition assay | Inhibition of human RPMI-8226 cell growth in a cell viability assay, IC50 = 36.6208 μM. | SANGER | ||
QIMR-WIL | Growth inhibition assay | Inhibition of human QIMR-WIL cell growth in a cell viability assay, IC50 = 36.644 μM. | SANGER | ||
HuH-7 | Growth inhibition assay | Inhibition of human HuH-7 cell growth in a cell viability assay, IC50 = 38.6184 μM. | SANGER | ||
CAL-12T | Growth inhibition assay | Inhibition of human CAL-12T cell growth in a cell viability assay, IC50 = 38.9416 μM. | SANGER | ||
GT3TKB | Growth inhibition assay | Inhibition of human GT3TKB cell growth in a cell viability assay, IC50 = 39.1921 μM. | SANGER | ||
OC-314 | Growth inhibition assay | Inhibition of human OC-314 cell growth in a cell viability assay, IC50 = 39.7125 μM. | SANGER | ||
NCI-H2228 | Growth inhibition assay | Inhibition of human NCI-H2228 cell growth in a cell viability assay, IC50 = 40.1403 μM. | SANGER | ||
NCI-H727 | Growth inhibition assay | Inhibition of human NCI-H727 cell growth in a cell viability assay, IC50 = 40.2531 μM. | SANGER | ||
NTERA-S-cl-D1 | Growth inhibition assay | Inhibition of human NTERA-S-cl-D1 cell growth in a cell viability assay, IC50 = 40.4706 μM. | SANGER | ||
MMAC-SF | Growth inhibition assay | Inhibition of human MMAC-SF cell growth in a cell viability assay, IC50 = 40.9235 μM. | SANGER | ||
HTC-C3 | Growth inhibition assay | Inhibition of human HTC-C3 cell growth in a cell viability assay, IC50 = 41.4169 μM. | SANGER | ||
SF295 | Growth inhibition assay | Inhibition of human SF295 cell growth in a cell viability assay, IC50 = 41.5379 μM. | SANGER | ||
U-2-OS | Growth inhibition assay | Inhibition of human U-2-OS cell growth in a cell viability assay, IC50 = 41.8567 μM. | SANGER | ||
HPAF-II | Growth inhibition assay | Inhibition of human HPAF-II cell growth in a cell viability assay, IC50 = 41.9382 μM. | SANGER | ||
KYSE-450 | Growth inhibition assay | Inhibition of human KYSE-450 cell growth in a cell viability assay, IC50 = 42.4707 μM. | SANGER | ||
DMS-273 | Growth inhibition assay | Inhibition of human DMS-273 cell growth in a cell viability assay, IC50 = 43.2836 μM. | SANGER | ||
HT-1376 | Growth inhibition assay | Inhibition of human HT-1376 cell growth in a cell viability assay, IC50 = 43.3156 μM. | SANGER | ||
786-0 | Growth inhibition assay | Inhibition of human 786-0 cell growth in a cell viability assay, IC50 = 43.6261 μM. | SANGER | ||
NCI-H810 | Growth inhibition assay | Inhibition of human NCI-H810 cell growth in a cell viability assay, IC50 = 44.0136 μM. | SANGER | ||
8305C | Growth inhibition assay | Inhibition of human 8305C cell growth in a cell viability assay, IC50 = 44.645 μM. | SANGER | ||
DSH1 | Growth inhibition assay | Inhibition of human DSH1 cell growth in a cell viability assay, IC50 = 45.7042 μM. | SANGER | ||
KYSE-520 | Growth inhibition assay | Inhibition of human KYSE-520 cell growth in a cell viability assay, IC50 = 46.5721 μM. | SANGER | ||
TYK-nu | Growth inhibition assay | Inhibition of human TYK-nu cell growth in a cell viability assay, IC50 = 46.7092 μM. | SANGER | ||
EPLC-272H | Growth inhibition assay | Inhibition of human EPLC-272H cell growth in a cell viability assay, IC50 = 46.7283 μM. | SANGER | ||
T-24 | Growth inhibition assay | Inhibition of human T-24 cell growth in a cell viability assay, IC50 = 47.9292 μM. | SANGER | ||
BHY | Growth inhibition assay | Inhibition of human BHY cell growth in a cell viability assay, IC50 = 47.999 μM. | SANGER | ||
NCI-H82 | Growth inhibition assay | Inhibition of human NCI-H82 cell growth in a cell viability assay, IC50 = 48.217 μM. | SANGER | ||
SF268 | Growth inhibition assay | Inhibition of human SF268 cell growth in a cell viability assay, IC50 = 48.6189 μM. | SANGER | ||
C-33-A | Growth inhibition assay | Inhibition of human C-33-A cell growth in a cell viability assay, IC50 = 48.7554 μM. | SANGER | ||
MIA-PaCa-2 | Growth inhibition assay | Inhibition of human MIA-PaCa-2 cell growth in a cell viability assay, IC50 = 48.8388 μM. | SANGER | ||
HCC1954 | Growth inhibition assay | Inhibition of human HCC1954 cell growth in a cell viability assay, IC50 = 49.0871 μM. | SANGER | ||
NCI-H1666 | Growth inhibition assay | Inhibition of human NCI-H1666 cell growth in a cell viability assay, IC50 = 49.3642 μM. | SANGER | ||
GR-ST | Growth inhibition assay | Inhibition of human GR-ST cell growth in a cell viability assay, IC50 = 49.3695 μM. | SANGER | ||
Ca9-22 | Growth inhibition assay | Inhibition of human Ca9-22 cell growth in a cell viability assay, IC50 = 49.4013 μM. | SANGER | ||
D-502MG | Growth inhibition assay | Inhibition of human D-502MG cell growth in a cell viability assay, IC50 = 49.417 μM. | SANGER | ||
SCC-4 | Growth inhibition assay | Inhibition of human SCC-4 cell growth in a cell viability assay, IC50 = 49.5602 μM. | SANGER | ||
RKO | Growth inhibition assay | Inhibition of human RKO cell growth in a cell viability assay, IC50 = 49.8356 μM. | SANGER | ||
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產(chǎn)品描述 | RO-3306是一種ATP競爭性的選擇性 CDK1 抑制劑,Ki 為20 nM,選擇性是其他各種人類激酶的15倍多。RO-3306可增強p53介導(dǎo)的 Bax 激活和線粒體的凋亡。 | ||||||||
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靶點 |
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體外研究(In Vitro) | ||||
體外研究活性 | RO-3306抑制CDK1/cyclin B1,CDK1/cyclin A,CDK2/cyclin E,和CDK4/cyclin D活性,Ki分別為35 nM,110 nM,340 nM,和>2000 nM。HCT116,SW480,和HeLa細胞用RO-3306處理20小時導(dǎo)致細胞周期完全阻滯在G2/M期。HCT116和SW480的增殖被RO-3306有效阻斷。RO-3306似乎在癌細胞(HCT116和SW480)中比在非致瘤性細胞(MCF 10A和MCF 12A)中具有更強的促凋亡作用。[1] 10 μM 濃度的RO-3306有效阻止卵母細胞成熟。[2] |
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激酶實驗 | CDK試驗 | |||
CDK1 cyclin B1,CDK1 cyclin A,CDK2 cyclin E,和CDK4 cyclin D通過均相時間分辨熒光法在96孔格式中測量。實驗緩沖液包含25 mM Hepes,6.25 mM MgCl2,0.003% Tween 20,0.3 mg/mL BSA,1.5 mM DTT,和如下含量的ATP: 162 μM (CDK1),90 mM (CDK2),或135 μM (CDK4)。CDK1和CDK2緩沖液包含10 mM MgCl2。測試化合物在20 μL實驗緩沖液中稀釋為它們終濃度的3倍,反應(yīng)通過加入40 μL包含pRB底物(0.185μM)的試驗緩沖液起始。板在37°C下連續(xù)攪拌培養(yǎng)30分鐘,反應(yīng)通過加入15 μL 含1.6μM 抗磷酸pRB抗體(Ser-780)的25 mM Hepes,24 mM EDTA,和0.2 mg/mL BSA終止。再振蕩培育30分鐘后,加入15μL 包含3nM Lance-Eu-W1024-labeledanti-rabbitIgG和60 nM Alophycocyanin共軛的抗-His-6 抗體的25 mM Hepes,以及0.5 mg/mL BSA,培育1小時。板在Victor-V多標(biāo)閱讀器上以340 nm激發(fā)波長和615 nm與665 nm發(fā)射波長讀取數(shù)據(jù)。IC50值根據(jù)665 nm下的讀數(shù)值進行計算,并歸一化為615 nm下銪的讀數(shù)值。Ki值根據(jù)公式Ki= IC50/(1 + S/Km )計算,其中S是試驗中ATP濃度,Km是相對ATP的Michaelis-Menten常數(shù)。對激酶組的抑制活性通過IMAP測定技術(shù)確定。 | ||||
細胞實驗 | 細胞系 | MDA-MB-231 細胞系 | ||
濃度 | 20 μM | |||
孵育時間 | 72 h | |||
方法 | 對數(shù)生長期細胞(25,000)接種于96孔板,在37℃培養(yǎng)箱中與CO2一起培養(yǎng),24小時后,給予不同濃度RO-3306以測定達到50%生長抑制(IC50)的藥物濃度。MTT (20 μL,包含5mg/mL儲備溶液的生理鹽水)加入每孔中,細胞培養(yǎng)4小時。移除上清液,來自活細胞的甲瓚晶體溶解在200 μL無水DMSO中。吸光度使用550模式酶標(biāo)儀在565 nm波長下檢測。 |
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實驗圖片 | 檢測方法 | 檢測指標(biāo) | 實驗圖片 | PMID |
Western blot | p-Cdk1 / Cdk1 / Cleaved PARP / Cleaved caspase-3 / p-p38 / Bad / Apaf1-1 / p-H2Ax / Bim / Bad | 27385216 | ||
Immunofluorescence | PARP1 / Plk1 | 28069876 | ||
Growth inhibition assay | Cell viability | 27385216 |
分子量 | 351.45 | 分子式 | C18H13N3OS2 |
CAS號 | 872573-93-8 | SDF | Download Ro-3306 SDF |
Smiles | C1=CC2=C(C=CC(=C2)C=C3C(=O)NC(=NCC4=CC=CS4)S3)N=C1 | ||
儲存條件(自收到貨起) | |||
體外溶解度 |
DMSO : 70 mg/mL ( (199.17 mM) ;DMSO吸濕會降低化合物溶解度,請使用新開封DMSO) Water : Insoluble Ethanol : Insoluble |
摩爾濃度計算器 |
體內(nèi)溶解度 現(xiàn)配現(xiàn)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(nèi)配方計算器 |
動物體內(nèi)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)
第二步:請輸入動物體內(nèi)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(lián)系Selleck為您提供正確的澄清溶液配方)
計算結(jié)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(lián)系Selleck);
體內(nèi)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(nèi)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。
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