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Bortezomib

別名: LDP-341, MLM341, NSC 681239,PS-341 中文名稱：硼替佐米

此產(chǎn)品請避光密封保存。

Bortezomib是有效的蛋白酶抑制劑，Ki為0.6 nM。它對腫瘤細(xì)胞表現(xiàn)出良好的選擇性。Bortezomib可抑制 NF-κB 并誘導(dǎo) ERK 的磷酸化從而抑制cathepsin B并在卵巢癌和其他固體腫瘤中抑制自噬的催化過程。

Bortezomib Chemical Structure

Bortezomib Chemical Structure

CAS: 179324-69-7

規(guī)格 價格 庫存 購買數(shù)量
10mM (1mL in DMSO) 749.39 現(xiàn)貨
5mg 571.94 現(xiàn)貨
25mg 1613.43 現(xiàn)貨
100mg 4316.13 現(xiàn)貨
1g 7944.3 現(xiàn)貨
更大包裝 有超大折扣

400-668-6834

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Bortezomib相關(guān)產(chǎn)品

相關(guān)信號通路圖

Proteasome Signaling Pathways

Proteasome信號通路圖

細(xì)胞實驗數(shù)據(jù)示例

細(xì)胞系 實驗類型 給藥濃度 孵育時間 活性描述 文獻(xiàn)信息
human PBMC Function Assay 100 nM 24 h Induces IL-8 release 25791477
U937 Function Assay 100 nM 6 h Induces IL-8 expression in LPS-stimulated U937 macrophages 25791477
HH Migration Assay 100 nM 24 h Reduces cell migration by 80–91% 25681335
Hut-78 Migration Assay 100 nM 24 h Reduces cell migration by 80–90% 25681335
HH Function Assay 100 nM 24 h downregulates TGF-β1 and IL-12 expression 25681335
H9 Function Assay 100 nM 24 h Downregulates TGF-β1 and IL-11 expression 25681335
Hut-78 Function Assay 100 nM 24 h Downregulates TGF-β1 and IL-10 expression 25681335
H1299 Apoptosis Assay 80 nM 24 h Sensitizes NSCLC cells to MSC-derived iC9-induced apoptosis 25323693
BLM Autophagy Assay 10 nM 12 h Induces formation of autophagosomes 23079083
A375 Autophagy Assay 10 nM 12 h Induces formation of autophagosomes 23079083
BLM Apoptosis Assay 10 nM 24 h Induces cell apoptosis 23079083
A375 Apoptosis Assay 10 nM 24 h Induces cell apoptosis 23079083
RAW 264.7 Growth Inhibition Assay 100 nM 48 h Reduces cell viability? 22427154
SNK-6 Antiviral Assay 1 μM 24 h Induces lytic infection of EBV 21170988
KAI-3 Antiviral Assay 1 μM 24 h Induces lytic infection of EBV 21170988
SNT-16 Antiviral Assay 1 μM 24 h Induces lytic infection of EBV 21170988
SNT-13 Antiviral Assay 1 μM 24 h Induces lytic infection of EBV 21170988
KHYG-1 Apoptosis Assay 1 μM 6 h Induces cell apoptosis 21170988
KAI-3 Apoptosis Assay 1 μM 6 h Induces cell apoptosis 21170988
Jurkat Apoptosis Assay 1 μM 6 h Induces cell apoptosis 21170988
SNT-16 Apoptosis Assay 1 μM 6 h Induces cell apoptosis 21170988
KHYG-1 Growth Inhibition Assay 1 μM 24 h Reduces cell viability? 21170988
SNK-6 Growth Inhibition Assay 1 μM 24 h Reduces cell viability? 21170988
KAI-3 Growth Inhibition Assay 1 μM 24 h Reduces cell viability? 21170988
Jurkat Growth Inhibition Assay 1 μM 24 h Reduces cell viability? 21170988
SNT-16 Growth Inhibition Assay 1 μM 24 h Reduces cell viability? 21170988
SNT-13 Growth Inhibition Assay 1 μM 24 h Reduces cell viability? 21170988
BJAB Growth Inhibition Assay 1 μM 24 h Reduces cell viability? 21170988
LCL-2 Growth Inhibition Assay 1 μM 24 h Reduces cell viability? 21170988
LCL-1 Growth Inhibition Assay 1 μM 24 h Reduces cell viability? 21170988
Raji Growth Inhibition Assay 1 μM 24 h Reduces cell viability? 21170988
BaF/3-p210 Function Assay 6 nM 24 h Reduces the phosphorylation and the activity of Rb 20305692
BaF/3-p210 Function Assay 6 nM 48 h Induces a slight G1 cell-cycle arrest 20305692
BaF/3 Function Assay 6 nM 48 h Induces a great G1 cell-cycle arrest 20305692
TCC-S Growth Inhibition Assay 100 nM 48 h IC50=2.8 nM 20305692
BaF/3-p210 Growth Inhibition Assay 100 nM 48 h IC50=4.7 nM 20305692
BaF/3 Growth Inhibition Assay 100 nM 48 h IC50=6.2 nM 20305692
RPMI 8226 Function Assay 20 nM 8 h Induces DNA synthesis 19436050
OPM2 Function Assay 20 nM 8 h Significantly enhances NF-κB activity 19436050
INA6 Function Assay 20 nM 8 h Significantly enhances NF-κB activity 19436050
OPM1 Function Assay 20 nM 8 h Significantly enhances NF-κB activity 19436050
U266 Function Assay 20 nM 8 h Significantly enhances NF-κB activity 19436050
MM.1S Function Assay 20 nM 8 h Significantly enhances NF-κB activity 19436050
RPMI 8226 Function Assay 20 nM 8 h Significantly enhances NF-κB activity 19436050
CHLA-255 Function Assay 10 nM 24 h Modestly reduces cells in the G0/G1 phase 17689684
NB-1691 Function Assay 10 nM 24 h Significantly reduces cells in the G0/G1 phase 17689684
SK-N-AS Growth Inhibition Assay 1 μM 72 h Inhibits cell proliferation to 10% 17689684
CHLA-255 Growth Inhibition Assay 1 μM 72 h Inhibits cell proliferation to 2% 17689684
NB-1691 Growth Inhibition Assay 1 μM 72 h Inhibits cell proliferation to 5% 17689684
HKe-3 Apoptosis Assay 50 nM 48 h Induces cell apoptosis 16778179
HCT116 Apoptosis Assay 50 nM 48 h Induces cell apoptosis 16778179
T29Kt1 Apoptosis Assay 50 nM 48 h Induces cell apoptosis 16778179
T29 Apoptosis Assay 50 nM 48 h Induces cell apoptosis 16778179
LNCap-Pro5 Function Assay 1 μM 4 h Stabilizes p53 14612532
H460 Function Assay 100 nM 24 h Induces G2-M-phase arrest and tubulin assembly-disassembly 12631620
H322 Growth Inhibition Assay 10 μM 72 h IC50=620 nM 12631620
H358 Growth Inhibition Assay 10 μM 72 h IC50=70 nM 12631620
H460 Growth Inhibition Assay 10 μM 72 h IC50=100 nM 12631620
RPMI8226/LR5 Growth Inhibition Assay 500 ng/ml 48 h Inhibits cell growth 12631619
U266/dox4 Growth Inhibition Assay 500 ng/ml 48 h Inhibits cell growth 12631619
U266/LR7 Growth Inhibition Assay 500 ng/ml 48 h Inhibits cell growth 12631619
WAD-1 Growth Inhibition Assay 500 ng/ml 48 h Inhibits cell growth 12631619
ARH77 Growth Inhibition Assay 500 ng/ml 48 h Inhibits cell growth 12631619
U266 Growth Inhibition Assay 500 ng/ml 48 h Inhibits cell growth 12631619
H460 Function Assay 10 μM 24 h Induces Bcl-2 phosphorylation and cleavage correlated with G2-M phase arrest 12492117
UM-SCC-11B Growth Inhibition Assay 100 nM 72 h Inhibits cell viability 11350913
UM-SCC-9 Growth Inhibition Assay 100 nM 72 h Inhibits cell viability 11350913
B7E3 Growth Inhibition Assay 100 nM 72 h Inhibits cell viability 11350913
B4B8 Growth Inhibition Assay 100 nM 72 h Inhibits cell viability 11350913
PAM-LY2 Growth Inhibition Assay 100 nM 72 h Inhibits cell viability 11350913
PAM 212 Growth Inhibition Assay 100 nM 72 h Inhibits cell viability 11350913
PAM-LY2 Function Assay 100 nM 12 h Inhibits NF-κB activation 11350913
Hs Sultan Growth Inhibition Assay 100 nM 48 h IC50=20 nM 11306489
IM-9 Growth Inhibition Assay 100 nM 48 h IC50=6 nM 11306489
U266 Growth Inhibition Assay 100 nM 48 h IC50=3 nM 11306489
LR5 Growth Inhibition Assay 100 nM 48 h IC50=20 nM 11306489
MR20 Growth Inhibition Assay 100 nM 48 h IC50=20 nM 11306489
Dox40 Growth Inhibition Assay 100 nM 48 h IC50=40 nM 11306489
RPMI8226 Growth Inhibition Assay 100 nM 48 h IC50=30 nM 11306489
OVCA 429 Function Assay 300 nM 48 h Disrupts intact multicellular tumor spheroids 10999766
MCF-7 Cytotoxic Assay 50 μM 48 h Kills cells by more than 99% 10499643
HeLa Function assay 5 nM 8 hrs Inhibition of proteasome activity in human HeLa cells assessed as induction of ubiquitinG76V-FL reporter level at 5 nM after 8 hrs by luciferase assay 21186794
HeLa Function assay 1 uM 8 hrs Inhibition of proteasome activity in human HeLa cells assessed as induction of ubiquitinG76V-FL reporter level at 1 uM after 8 hrs by luciferase assay 21186794
LN229 Function assay 100 nM 1 hr Inhibition of HIF1alpha expression in human LN229 cells assessed as reduction of HIF-1alpha accumulation at 100 nM preincubated for 1 hr under normoxia condition followed by 24 hrs incubation under hypoxia condition by Western blotting 21831638
LN229 Function assay 20 uM 1 hr Inhibition of hypoxia-induced HIF1alpha accumulation in human LN229 cells at 20 uM after 1 hr preincubation measured after 24 hrs by Western blot analysis 22032632
U1 Function assay 10 uM 24 hr Inhibition of NF-kappaB-mediated viral replication in Homo sapiens (human) U1 cells infected with X4 tropic HIV1 NL4-3 at 10 uM after 24 hr by RT-PCR analysis in presence of TNF-alpha 23290051
Calu6 Function assay 10 uM 18 hrs Inhibition of His-tagged Frataxin (unknown origin)/Ubiquitin interaction expressed in human Calu6 cells assessed as increase in frataxin (1-210) precursor level at 10 uM after 18 hrs by Western blotting analysis 23506486
HEK293 Cytotoxicity assay 0.0001 uM to 100 uM 48 hrs Cytotoxicity against human HEK293 cells expressing murine FAP at 0.0001 uM to 100 uM after 48 hrs by CellTiter-Blue assay 23594271
A549 Function assay 0.025 to 0.5 uM 24 hrs Induction of cell death in human A549 cells assessed as accumulation of poly-ubiquitinated proteins at 0.025 to 0.5 uM after 24 hrs by immunoblot assay 25639862
A549 Function assay 0.025 to 0.5 uM 24 hrs Induction of cell death in human A549 cells assessed as stabilization of p53 at 0.025 to 0.5 uM after 24 hrs by immunoblot assay 25639862
A549 Function assay 0.025 to 0.1 uM 24 hrs Induction of cell death in human A549 cells assessed as accumulation of Noxa at 0.025 to 0.1 uM after 24 hrs by immunoblot assay 25639862
MCF7 Function assay 35 nM 4 hrs Inhibition of 26S proteasome in human MCF7 cells assessed as accumulation of high molecular weight polyubiquitin-conjugated proteins at 35 nM after 4 hrs by Western blot analysis 27994734
MDA-MB-468 Function assay 35 nM 4 hrs Inhibition of 26S proteasome in human MDA-MB-468 cells assessed as accumulation of high molecular weight polyubiquitin-conjugated proteins at 35 nM after 4 hrs by Western blot analysis 27994734
SK-N-SH Cytotoxicity assay 0.1 to 1 uM 24 hrs Cytotoxicity against human SK-N-SH cells assessed as reduction in cell viability at 0.1 to 1 uM after 24 hrs by MTT assay 29269255
MYCN2 Cytotoxicity assay 0.1 to 1 uM 24 hrs Cytotoxicity against human MYCN2 cells assessed as reduction in cell viability at 0.1 to 1 uM after 24 hrs by MTT assay 29269255
U266 Apoptosis assay 2.5 nM 24 hrs Induction of apoptosis in human U266 cells at 2.5 nM after 24 hrs by Annexin V/propidium iodide staining based flow cytometry 29304284
RPMI8226 Apoptosis assay 2.5 nM 24 hrs Induction of apoptosis in human RPMI8226 cells at 2.5 nM after 24 hrs by Annexin V/propidium iodide staining based flow cytometry 29304284
NCI-H929 Apoptosis assay 2.5 nM 24 hrs Induction of apoptosis in human NCI-H929 cells at 2.5 nM after 24 hrs by Annexin V/propidium iodide staining based flow cytometry 29304284
HL60 Function assay 1 to 100 nM 24 hrs Inhibition of proteasome in human HL60 cells assessed as increase in cleaved PARP expression at 1 to 100 nM after 24 hrs by immunoblot assay 30365892
SUP-B15 Function assay 1 to 100 nM 24 hrs Inhibition of proteasome in imatinib-resistant human SUP-B15 cells assessed as increase in cleaved PARP expression at 1 to 100 nM after 24 hrs by immunoblot assay 30365892
SEM Function assay 1 to 100 nM 24 hrs Inhibition of proteasome in human SEM cells assessed as increase in cleaved PARP expression at 1 to 100 nM after 24 hrs by immunoblot assay 30365892
SEM Function assay 10 nM 18 hrs Inhibition of proteasome in human SEM cells assessed as increase in aggresome accumulation at 10 nM after 18 hrs by by FACS analysis 30365892
SEM Function assay 10 nM 18 hrs Inhibition of proteasome in human SEM cells assessed as increase in aggresome accumulation at 10 nM after 18 hrs by fluorescence microscopic method 30365892
HL60 Function assay 100 nM Inhibition of chymotrypsin-like activity of proteasome in human HL60 cells at 100 nM 19655762
AMO1 Antitumor assay 1 mg/kg Antitumor activity against human AMO1 cells xenografted in nude SCID beige mouse assessed as tumor growth inhibition at 1 mg/kg, iv administered twice per week 26565666
MDA-MB-231 Function assay 1 uM Inhibition of trypsin like activity of 26S proteasome derived from human MDA-MB-231 cells at 1 uM 28291344
MDA-MB-231 Function assay 1 uM Inhibition of caspase like activity of 26S proteasome derived from human MDA-MB-231 cells at 1 uM 28291344
MDA-MB-231 Function assay 1 uM Inhibition of chymotrypsin like activity of 26S proteasome derived from human MDA-MB-231 cells at 1 uM 28291344
FSCLL Cytotoxicity assay 24 hrs CC50 = 0.004 μM 21634429
HEK293 Cytotoxicity assay 24 hrs CC50 = 0.347 μM 21634429
Glioma (HF2303) Cytotoxicity assay 72 hrs EC50 = 0.0007 μM 26288699
Glioma (HF2476) Cytotoxicity assay 72 hrs EC50 = 0.0007 μM 26288699
Glioma (HF2876) Cytotoxicity assay 72 hrs EC50 = 0.0007 μM 26288699
Glioma (HF2885) Cytotoxicity assay 72 hrs EC50 = 0.0007 μM 26288699
Glioma (HF3013) Cytotoxicity assay 72 hrs EC50 = 0.0007 μM 26288699
Glioma (HF2381) Cytotoxicity assay 72 hrs EC50 = 0.0007 μM 26288699
Glioma (HF2790) Cytotoxicity assay 72 hrs EC50 = 0.0007 μM 26288699
HepG2 Cytotoxicity assay 48 hrs EC50 = 0.01 μM 29800827
HL60 Function assay 10 mins ED50 = 0.0025 μM 19422206
HL60 Function assay 10 mins ED50 = 0.0025 μM 21973101
CEM Antiproliferative assay 72 hrs GI50 = 0.001 μM 28441582
U266 Antiproliferative assay 72 hrs GI50 = 0.001 μM 28441582
K562 Antiproliferative assay 72 hrs GI50 = 0.007 μM 28441582
DLD1 Function assay 6 hrs IC50 = 0.0002 μM 22206869
DLD1 Function assay 6 hrs IC50 = 0.0009 μM 22206869
HCT116 Cytotoxicity assay 72 hrs IC50 = 0.001 μM 28634039
HCT116 Antiproliferative assay 72 hrs IC50 = 0.0014 μM 27769033
HepG2 Antiproliferative assay 72 hrs IC50 = 0.00161 μM 27769033
SKOV3 Antiproliferative assay 72 hrs IC50 = 0.00162 μM 27769033
DOGUM Cytotoxicity assay 72 hrs IC50 = 0.002 μM 23031590
U266 Cytotoxicity assay 72 hrs IC50 = 0.00245 μM 19537716
A549 Antiproliferative assay 72 hrs IC50 = 0.0025 μM 28182990
HL60 Antiproliferative assay 72 hrs IC50 = 0.0032 μM 28182990
RPMI18226 Cytotoxicity assay 72 hrs IC50 = 0.0035 μM 21077681
HL60 Cytotoxicity assay 72 hrs IC50 = 0.0035 μM 21077681
RPMI8226 Cytotoxicity assay 72 hrs IC50 = 0.00388 μM 26965867
HL60 Function assay 2 hrs IC50 = 0.004 μM 27769033
U266 Function assay 1 hr IC50 = 0.004 μM 28441582
HL60 Function assay 2 hrs IC50 = 0.004 μM 28634039
SEM Function assay 2 hrs IC50 = 0.00443 μM 30365892
HL60 Cytotoxicity assay 72 hrs IC50 = 0.0055 μM 19537716
U266 Cytotoxicity assay 72 hrs IC50 = 0.00573 μM 26965867
MGC803 Antiproliferative assay 72 hrs IC50 = 0.005782 μM 27769033
GUMBUS Cytotoxicity assay 72 hrs IC50 = 0.006 μM 23031590
ARH77 Cytotoxicity assay 72 hrs IC50 = 0.00607 μM 26965867
SW480 Cytotoxicity assay 72 hrs IC50 = 0.0061 μM 20158184
MDA-MB-231 Antiproliferative assay 72 hrs IC50 = 0.0065 μM 28182990
HL60 Function assay 2 hrs IC50 = 0.00667 μM 30365892
A549 Cytotoxicity assay 72 hrs IC50 = 0.0067 μM 20158184
RPMI8226 Antiproliferative assay 72 hrs IC50 = 0.0067 μM 28182990
5TGM1 Cytotoxicity assay 48 to 72 hrs IC50 = 0.00678 μM 24119559
HL60 Cytotoxicity assay 72 hrs IC50 = 0.0069 μM 19747832
PC3 Cytotoxicity assay 72 hrs IC50 = 0.007 μM 20158184
DOGUM Cytotoxicity assay 72 hrs IC50 = 0.007 μM 23031590
HL60 Cytotoxicity assay 72 hrs IC50 = 0.0071 μM 20158184
MKN45 Antiproliferative assay 72 hrs IC50 = 0.00715 μM 27769033
HepG2 Cytotoxicity assay 72 hrs IC50 = 0.0075 μM 20158184
HL60 Antiproliferative assay 72 hrs IC50 = 0.0076 μM 27769033
RPMI8226 Cytotoxic activity against human 72 hrs IC50 = 0.00796 μM 24767818
HL60 Cytotoxicity assay 72 hrs IC50 = 0.008 μM 28634039
MGC803 Cytotoxicity assay 72 hrs IC50 = 0.008 μM 28634039
SKOV3/TR Function assay 4 days IC50 = 0.008 μM 29767973
PC3 Cytotoxicity assay 72 hrs IC50 = 0.0083 μM 21077681
U266 Cytotoxicity assay 72 hrs IC50 = 0.0088 μM 20158184
RPMI8226 Cytotoxicity assay 48 to 72 hrs IC50 = 0.0095 μM 24119559
ARH77 Cytotoxicity assay 72 hrs IC50 = 0.00957 μM 29934218
HEK293 Function assay 3 hrs IC50 = 0.01 μM 20875739
HCT116 Cytotoxicity assay 72 hrs IC50 = 0.01 μM 23547757
NCI-H929 Cytotoxicity assay 72 hrs IC50 = 0.01085 μM 24767818
CCRF-CEM Antiproliferative assay 72 hrs IC50 = 0.011 μM 26231162
RPMI8226 Cytotoxicity assay 72 hrs IC50 = 0.0112 μM 29934218
U266B1 Cytotoxicity assay 72 hrs IC50 = 0.01163 μM 29934218
BxPC3 Cytotoxicity assay 72 hrs IC50 = 0.0118 μM 19747832
293T Antiproliferative assay 72 hrs IC50 = 0.012 μM 28191850
U266 Cytotoxicity assay 72 hrs IC50 = 0.0122 μM 19747832
SW480 Cytotoxicity assay 72 hrs IC50 = 0.0123 μM 21077681
SKOV3 Cytotoxicity assay 4 days IC50 = 0.0129 μM 29767973
A549 Cytotoxicity assay 72 hrs IC50 = 0.0139 μM 21077681
HEK293 Function assay 30 mins IC50 = 0.014 μM 21044847
RPMI8266 Antiproliferative assay 72 hrs IC50 = 0.0144 μM 26231162
BxPC3 Cytotoxicity assay 72 hrs IC50 = 0.0162 μM 20158184
MDA-MB-231 Antiproliferative assay 72 hrs IC50 = 0.01665 μM 27769033
TOV21G Antiproliferative assay 72 hrs IC50 = 0.0167 μM 26231162
MDA-MB-231 Cytotoxicity assay 72 hrs IC50 = 0.017 μM 28634039
BxPC3 Cytotoxicity assay 72 hrs IC50 = 0.0194 μM 21077681
HeLa Growth inhibition assay 72 hrs IC50 = 0.02 μM 19428245
RKO Antiproliferative assay 72 hrs IC50 = 0.0208 μM 26231162
MCF7 Antiproliferative assay 3 days IC50 = 0.025 μM 28557430
Bel7404 Antiproliferative assay 72 hrs IC50 = 0.02504 μM 27769033
HepG2 Cytotoxicity assay 72 hrs IC50 = 0.0252 μM 21077681
HEK293 Function assay 24 hrs IC50 = 0.027 μM 21634429
HCT116 Antiproliferative assay 72 hrs IC50 = 0.027 μM 26231162
SUP-B15 Function assay 2 hrs IC50 = 0.02809 μM 30365892
A431 Antiproliferative assay 72 hrs IC50 = 0.0282 μM 26231162
A2780 Antiproliferative assay 72 hrs IC50 = 0.0289 μM 28182990
HL60 Function assay 2 hrs IC50 = 0.03 μM 27769033
HL60 Function assay 2 hrs IC50 = 0.03 μM 28634039
HEK293 Function assay 6 hrs IC50 = 0.03 μM 28919340
WM266.4 Cytotoxicity assay 72 hrs IC50 = 0.035 μM 22206869
GUMBUS Cytotoxicity assay 72 hrs IC50 = 0.035 μM 23031590
HepG2 Cytotoxicity assay 72 hrs IC50 = 0.0375 μM 19537716
95-D Cytotoxicity assay 72 hrs IC50 = 0.038 μM 28634039
95-D Antiproliferative assay 72 hrs IC50 = 0.03818 μM 27769033
SW480 Cytotoxicity assay 72 hrs IC50 = 0.05 μM 19537716
KB Cytotoxicity assay 72 hrs IC50 = 0.0595 μM 19537716
SKOV3 Cytotoxicity assay 72 hrs IC50 = 0.0668 μM 21077681
SW1990 Antiproliferative assay 72 hrs IC50 = 0.07906 μM 27769033
HeLa Cytotoxicity assay 72 hrs IC50 = 0.092 μM 19537716
A549 Antiproliferative assay 72 hrs IC50 = 0.092 μM 28191850
H460 Cytotoxicity assay 72 hrs IC50 = 0.115 μM 19537716
SKOV3 Cytotoxicity assay 72 hrs IC50 = 0.13 μM 19537716
SKOV3 Cytotoxicity assay 72 hrs IC50 = 0.151 μM 20158184
A549 Cytotoxicity assay 72 hrs IC50 = 0.255 μM 19537716
HL60 Function assay 2 hrs IC50 = 0.44 μM 27769033
HL60 Function assay 2 hrs IC50 = 0.44 μM 28634039
H460 Cytotoxicity assay 72 hrs IC50 = 0.78 μM 20158184
BGC823 Cytotoxicity assay 72 hrs IC50 = 0.88 μM 19537716
MCF7 Antiproliferative assay 72 hrs IC50 = 18.37 μM 29426629
A549 Antiproliferative assay 72 hrs IC50 = 2.13573 μM 27769033
A549 Cytotoxicity assay 72 hrs IC50 = 2.14 μM 28634039
BGC823 Cytotoxicity assay 72 hrs IC50 = 2.89 μM 19747832
MDA-MB-231 Antiproliferative assay 72 hrs IC50 = 3.125 μM 29426629
BCG823 Cytotoxicity assay 72 hrs IC50 = 3.29 μM 20158184
A549 Antiproliferative assay 72 hrs IC50 = 9.318 μM 29426629
Calu6 Cytotoxicity assay 72 hrs LC50 = 0.0061 μM 20875739
HEK293T Antiproliferative assay 48 hrs LC50 = 0.016 μM 29843100
LO2 Antiproliferative assay 48 hrs LC50 = 0.398 μM 29843100
NCI-H929 Cytotoxicity assay 48 hrs LD50 = 0.0066 μM 27994734
U266 Cytotoxicity assay 48 hrs LD50 = 0.018 μM 27994734
LCL Cytotoxicity assay 48 hrs LD50 = 0.02 μM 27994734
MDA-MB-468 Cytotoxicity assay 48 hrs LD50 = 0.037 μM 27994734
RD-ES Cytotoxicity assay 48 hrs LD50 = 0.04 μM 27994734
WE68 Cytotoxicity assay 48 hrs LD50 = 0.1 μM 27994734
IMR90 Cytotoxicity assay 48 hrs LD50 = 0.13 μM 27994734
KGN Cytotoxicity assay 48 hrs LD50 = 0.18 μM 27994734
HNDF Cytotoxicity assay 48 hrs LD50 = 0.48 μM 27994734
MCF10A Cytotoxicity assay 48 hrs LD50 = 1.5 μM 27994734
SKOV3 Cytotoxicity assay 48 hrs LD50 = 1.6 μM 27994734
MCF7 Cytotoxicity assay 48 hrs LD50 = 9.8 μM 27994734
HCT116 Cell cycle assay 24 hrs Cell cycle arrest in human HCT116 cells assessed as accumulation at G2/M phase after 24 hrs by propidium iodide staining-based flow cytometric analysis 23547757
K-562 Growth Inhibition Assay IC50=4.12 nM SANGER
NCI-H1648 Growth Inhibition Assay IC50=4.13 nM SANGER
OMC-1 Growth Inhibition Assay IC50=4.18 nM SANGER
LB647-SCLC Growth Inhibition Assay IC50=4.22 nM SANGER
TE-12 Growth Inhibition Assay IC50=4.25 nM SANGER
NOMO-1 Growth Inhibition Assay IC50=4.33 nM SANGER
Raji Growth Inhibition Assay IC50=4.46 nM SANGER
NALM-6 Growth Inhibition Assay IC50=4.49 nM SANGER
HL-60 Growth Inhibition Assay IC50=4.67 nM SANGER
IST-SL1 Growth Inhibition Assay IC50=4.68 nM SANGER
MHH-PREB-1 Growth Inhibition Assay IC50=4.86 nM SANGER
MHH-NB-11 Growth Inhibition Assay IC50=4.91 nM SANGER
JiyoyeP-2003 Growth Inhibition Assay IC50=5 nM SANGER
SBC-1 Growth Inhibition Assay IC50=5.01 nM SANGER
CHP-126 Growth Inhibition Assay IC50=5.06 nM SANGER
LU-139 Growth Inhibition Assay IC50=5.13 nM SANGER
NCI-SNU-5 Growth Inhibition Assay IC50=5.17 nM SANGER
SW962 Growth Inhibition Assay IC50=5.21 nM SANGER
EW-1 Growth Inhibition Assay IC50=5.31 nM SANGER
NCI-H1417 Growth Inhibition Assay IC50=5.51 nM SANGER
LU-65 Growth Inhibition Assay IC50=5.84 nM SANGER
D-502MG Growth Inhibition Assay IC50=6.37 nM SANGER
BC-3 Growth Inhibition Assay IC50=6.61 nM SANGER
GDM-1 Growth Inhibition Assay IC50=6.77 nM SANGER
NCI-H2196 Growth Inhibition Assay IC50=6.8 nM SANGER
NB1 Growth Inhibition Assay IC50=6.88 nM SANGER
NCI-H345 Growth Inhibition Assay IC50=7.2 nM SANGER
SU-DHL-1 Growth Inhibition Assay IC50=7.24 nM SANGER
JVM-2 Growth Inhibition Assay IC50=7.28 nM SANGER
LU-134-A Growth Inhibition Assay IC50=7.39 nM SANGER
NCI-H1694 Growth Inhibition Assay IC50=7.58 nM SANGER
NCI-SNU-16 Growth Inhibition Assay IC50=7.65 nM SANGER
L-363 Growth Inhibition Assay IC50=7.7 nM SANGER
KG-1 Growth Inhibition Assay IC50=7.94 nM SANGER
MN-60 Growth Inhibition Assay IC50=8.14 nM SANGER
NB6 Growth Inhibition Assay IC50=8.48 nM SANGER
MLMA Growth Inhibition Assay IC50=8.85 nM SANGER
ATN-1 Growth Inhibition Assay IC50=8.89 nM SANGER
SK-NEP-1 Growth Inhibition Assay IC50=9.01 nM SANGER
DMS-114 Growth Inhibition Assay IC50=9.62 nM SANGER
CTB-1 Growth Inhibition Assay IC50=9.67 nM SANGER
NCI-H2081 Growth Inhibition Assay IC50=10.09 nM SANGER
ES5 Growth Inhibition Assay IC50=10.38 nM SANGER
HCC1599 Growth Inhibition Assay IC50=11.91 nM SANGER
NCI-H23 Growth Inhibition Assay IC50=12.12 nM SANGER
NCI-H1581 Growth Inhibition Assay IC50=12.28 nM SANGER
JVM-3 Growth Inhibition Assay IC50=12.99 nM SANGER
NCI-SNU-1 Growth Inhibition Assay IC50=13.19 nM SANGER
NB7 Growth Inhibition Assay IC50=15.92 nM SANGER
JAR Growth Inhibition Assay IC50=16.13 nM SANGER
TGW Growth Inhibition Assay IC50=16.48 nM SANGER
U-87-MG Growth Inhibition Assay IC50=16.76 nM SANGER
NCI-H1436 Growth Inhibition Assay IC50=17.01 nM SANGER
GOTO Growth Inhibition Assay IC50=17.06 nM SANGER
COLO-800 Growth Inhibition Assay IC50=17.64 nM SANGER
MFM-223 Growth Inhibition Assay IC50=17.91 nM SANGER
EW-18 Growth Inhibition Assay IC50=17.96 nM SANGER
NB14 Growth Inhibition Assay IC50=17.98 nM SANGER
EB2 Growth Inhibition Assay IC50=18.08 nM SANGER
EoL-1- Growth Inhibition Assay IC50=18.31 nM SANGER
NCCIT Growth Inhibition Assay IC50=18.36 nM SANGER
DG-75 Growth Inhibition Assay IC50=18.61 nM SANGER
HCC2218 Growth Inhibition Assay IC50=19.5 nM SANGER
TE-6 Growth Inhibition Assay IC50=20.08 nM SANGER
SF539 Growth Inhibition Assay IC50=20.67 nM SANGER
NCI-H446 Growth Inhibition Assay IC50=21.18 nM SANGER
IST-MES1 Growth Inhibition Assay IC50=22.77 nM SANGER
NCI-H82 Growth Inhibition Assay IC50=23.02 nM SANGER
HCC2157 Growth Inhibition Assay IC50=23.13 nM SANGER
EW-12 Growth Inhibition Assay IC50=23.17 nM SANGER
SIMA Growth Inhibition Assay IC50=23.38 nM SANGER
DOHH-2 Growth Inhibition Assay IC50=23.45 nM SANGER
IM-9 Growth Inhibition Assay IC50=23.54 nM SANGER
EC-GI-10 Growth Inhibition Assay IC50=24.23 nM SANGER
HDLM-2 Growth Inhibition Assay IC50=24.54 nM SANGER
LS-1034 Growth Inhibition Assay IC50=25.75 nM SANGER
REH Growth Inhibition Assay IC50=26.41 nM SANGER
LU-165 Growth Inhibition Assay IC50=26.72 nM SANGER
NH-12 Growth Inhibition Assay IC50=27.67 nM SANGER
WSU-NHL Growth Inhibition Assay IC50=28.39 nM SANGER
ECC4 Growth Inhibition Assay IC50=28.79 nM SANGER
OCI-AML2 Growth Inhibition Assay IC50=29.69 nM SANGER
EW-3 Growth Inhibition Assay IC50=30.59 nM SANGER
NCI-H526 Growth Inhibition Assay IC50=32.54 nM SANGER
NCI-H719 Growth Inhibition Assay IC50=34.31 nM SANGER
KARPAS-422 Growth Inhibition Assay IC50=35.04 nM SANGER
SK-MEL-1 Growth Inhibition Assay IC50=35.17 nM SANGER
ES3 Growth Inhibition Assay IC50=35.19 nM SANGER
UACC-812 Growth Inhibition Assay IC50=35.44 nM SANGER
C8166 Growth Inhibition Assay IC50=35.7 nM SANGER
MDA-MB-134-VI Growth Inhibition Assay IC50=35.87 nM SANGER
D-283MED Growth Inhibition Assay IC50=37.79 nM SANGER
SHP-77 Growth Inhibition Assay IC50=38.03 nM SANGER
NCI-H2227 Growth Inhibition Assay IC50=40.49 nM SANGER
SKM-1 Growth Inhibition Assay IC50=42.63 nM SANGER
L-428 Growth Inhibition Assay IC50=43.86 nM SANGER
RPMI-6666 Growth Inhibition Assay IC50=45.89 nM SANGER
NCI-H716 Growth Inhibition Assay IC50=48.81 nM SANGER
DMS-79 Growth Inhibition Assay IC50=50.71 nM SANGER
RS4-11 Growth Inhibition Assay IC50=50.88 nM SANGER
NCI-H720 Growth Inhibition Assay IC50=51.11 nM SANGER
MC-CAR Growth Inhibition Assay IC50=51.52 nM SANGER
TALL-1 Growth Inhibition Assay IC50=53.91 nM SANGER
NCI-N87 Growth Inhibition Assay IC50=54.18 nM SANGER
P30-OHK Growth Inhibition Assay IC50=54.61 nM SANGER
LP-1 Growth Inhibition Assay IC50=61.28 nM SANGER
YT Growth Inhibition Assay IC50=61.8 nM SANGER
MRK-nu-1 Growth Inhibition Assay IC50=61.82 nM SANGER
BT-474 Growth Inhibition Assay IC50=65 nM SANGER
NCI-H322M Growth Inhibition Assay IC50=66.11 nM SANGER
NCI-H128 Growth Inhibition Assay IC50=74.77 nM SANGER
KMS-12-PE Growth Inhibition Assay IC50=76.24 nM SANGER
KP-N-YS Growth Inhibition Assay IC50=76.74 nM SANGER
ALL-PO Growth Inhibition Assay IC50=77.66 nM SANGER
EW-13 Growth Inhibition Assay IC50=77.76 nM SANGER
EW-11 Growth Inhibition Assay IC50=78.52 nM SANGER
SK-N-FI Growth Inhibition Assay IC50=80.2 nM SANGER
CAL-148 Growth Inhibition Assay IC50=81.84 nM SANGER
RL Growth Inhibition Assay IC50=86.09 nM SANGER
AM-38 Growth Inhibition Assay IC50=88.08 nM SANGER
RH-1 Growth Inhibition Assay IC50=99.85 nM SANGER
NCI-H1770 Growth Inhibition Assay IC50=102.49 nM SANGER
SIG-M5 Growth Inhibition Assay IC50=105.06 nM SANGER
GR-ST Growth Inhibition Assay IC50=113.34 nM SANGER
ST486 Growth Inhibition Assay IC50=114.06 nM SANGER
NCI-H1650 Growth Inhibition Assay IC50=115.29 nM SANGER
MHH-CALL-2 Growth Inhibition Assay IC50=115.7 nM SANGER
BV-173 Growth Inhibition Assay IC50=122.71 nM SANGER
MC116 Growth Inhibition Assay IC50=148.85 nM SANGER
NCI-H524 Growth Inhibition Assay IC50=159.1 nM SANGER
SCLC-21H Growth Inhibition Assay IC50=159.41 nM SANGER
NCI-H1304 Growth Inhibition Assay IC50=169.21 nM SANGER
NCI-H510A Growth Inhibition Assay IC50=185.37 nM SANGER
NCI-H209 Growth Inhibition Assay IC50=196.52 nM SANGER
KM-H2 Growth Inhibition Assay IC50=197.05 nM SANGER
NCI-H1395 Growth Inhibition Assay IC50=210.13 nM SANGER
NCI-H1155 Growth Inhibition Assay IC50=230.32 nM SANGER
COR-L279 Growth Inhibition Assay IC50=252.17 nM SANGER
NCI-H1299 Growth Inhibition Assay IC50=261.71 nM SANGER
EW-22 Growth Inhibition Assay IC50=263.75 nM SANGER
SK-MEL-2 Growth Inhibition Assay IC50=281.9 nM SANGER
KASUMI-1 Growth Inhibition Assay IC50=283.05 nM SANGER
NCI-H187 Growth Inhibition Assay IC50=287.08 nM SANGER
NCI-H2171 Growth Inhibition Assay IC50=288.92 nM SANGER
LNCaP-Clone-FGC Growth Inhibition Assay IC50=295.26 nM SANGER
NCI-H1522 Growth Inhibition Assay IC50=307.05 nM SANGER
SCH Growth Inhibition Assay IC50=322.22 nM SANGER
THP-1 Growth Inhibition Assay IC50=322.6 nM SANGER
SNU-C1 Growth Inhibition Assay IC50=362.09 nM SANGER
CA46 Growth Inhibition Assay IC50=373.63 nM SANGER
NCI-H1963 Growth Inhibition Assay IC50=386.19 nM SANGER
DEL Growth Inhibition Assay IC50=391.27 nM SANGER
TUR Growth Inhibition Assay IC50=396.61 nM SANGER
NCI-H226 Growth Inhibition Assay IC50=403.23 nM SANGER
COLO-668 Growth Inhibition Assay IC50=403.57 nM SANGER
CPC-N Growth Inhibition Assay IC50=403.77 nM SANGER
NCI-H889 Growth Inhibition Assay IC50=461.92 nM SANGER
J-RT3-T3-5 Growth Inhibition Assay IC50=532.57 nM SANGER
MSTO-211H Growth Inhibition Assay IC50=574.26 nM SANGER
SCC-15 Growth Inhibition Assay IC50=667.47 nM SANGER
SUP-T1 Growth Inhibition Assay IC50=686.04 nM SANGER
DMS-153 Growth Inhibition Assay IC50=746.83 nM SANGER
MS-1 Growth Inhibition Assay IC50=759.42 nM SANGER
TC-YIK Growth Inhibition Assay IC50=781.01 nM SANGER
RPMI-8866 Growth Inhibition Assay IC50=1006.28 μM SANGER
KY821 Growth Inhibition Assay IC50=1036.04 μM SANGER
P31-FUJ Growth Inhibition Assay IC50=1112.75 μM SANGER
COLO-824 Growth Inhibition Assay IC50=1261.78 μM SANGER
U-698-M Growth Inhibition Assay IC50=2262.15 μM SANGER
TE-441-T Growth Inhibition Assay IC50=2521.7 μM SANGER
IMR-5 Growth Inhibition Assay IC50=3409.62 μM SANGER
NCI-H1838 Growth Inhibition Assay IC50=4186.32 μM SANGER
NCI-H2141 Growth Inhibition Assay IC50=4.05 nM SANGER
HD-MY-Z Growth Inhibition Assay IC50=3.93 nM SANGER
RCC10RGB Growth Inhibition Assay IC50=3.93 nM SANGER
COLO-320-HSR Growth Inhibition Assay IC50=3.92 nM SANGER
RL95-2 Growth Inhibition Assay IC50=3.79 nM SANGER
LC-1F Growth Inhibition Assay IC50=3.74 nM SANGER
NMC-G1 Growth Inhibition Assay IC50=3.68 nM SANGER
COLO-684 Growth Inhibition Assay IC50=3.66 nM SANGER
DJM-1 Growth Inhibition Assay IC50=3.63 nM SANGER
EVSA-T Growth Inhibition Assay IC50=3.6 nM SANGER
no-11 Growth Inhibition Assay IC50=3.55 nM SANGER
MZ1-PC Growth Inhibition Assay IC50=3.54 nM SANGER
HCC1187 Growth Inhibition Assay IC50=3.54 nM SANGER
KARPAS-45 Growth Inhibition Assay IC50=3.54 nM SANGER
RPMI-8402 Growth Inhibition Assay IC50=3.5 nM SANGER
LOXIMVI Growth Inhibition Assay IC50=3.5 nM SANGER
MEG-01 Growth Inhibition Assay IC50=3.49 nM SANGER
LAMA-84 Growth Inhibition Assay IC50=3.49 nM SANGER
COR-L88 Growth Inhibition Assay IC50=3.47 nM SANGER
TE-15 Growth Inhibition Assay IC50=3.43 nM SANGER
DB Growth Inhibition Assay IC50=3.41 nM SANGER
LB996-RCC Growth Inhibition Assay IC50=3.4 nM SANGER
NEC8 Growth Inhibition Assay IC50=3.35 nM SANGER
SK-N-DZ Growth Inhibition Assay IC50=3.26 nM SANGER
CW-2 Growth Inhibition Assay IC50=3.21 nM SANGER
SK-PN-DW Growth Inhibition Assay IC50=3.14 nM SANGER
CGTH-W-1 Growth Inhibition Assay IC50=3.1 nM SANGER
MONO-MAC-6 Growth Inhibition Assay IC50=3.1 nM SANGER
KARPAS-299 Growth Inhibition Assay IC50=3.06 nM SANGER
HT Growth Inhibition Assay IC50=3.02 nM SANGER
SW954 Growth Inhibition Assay IC50=2.9 nM SANGER
MOLT-16 Growth Inhibition Assay IC50=2.89 nM SANGER
C2BBe1 Growth Inhibition Assay IC50=2.89 nM SANGER
ETK-1 Growth Inhibition Assay IC50=2.84 nM SANGER
CTV-1 Growth Inhibition Assay IC50=2.8 nM SANGER
EW-16 Growth Inhibition Assay IC50=2.75 nM SANGER
Mo-T Growth Inhibition Assay IC50=2.74 nM SANGER
EB-3 Growth Inhibition Assay IC50=2.66 nM SANGER
LB1047-RCC Growth Inhibition Assay IC50=2.57 nM SANGER
KNS-81-FD Growth Inhibition Assay IC50=2.48 nM SANGER
NB69 Growth Inhibition Assay IC50=2.46 nM SANGER
NCI-H64 Growth Inhibition Assay IC50=2.44 nM SANGER
KU812 Growth Inhibition Assay IC50=2.42 nM SANGER
NCI-H748 Growth Inhibition Assay IC50=2.39 nM SANGER
ARH-77 Growth Inhibition Assay IC50=2.38 nM SANGER
SCC-3 Growth Inhibition Assay IC50=2.37 nM SANGER
RPMI-8226 Growth Inhibition Assay IC50=2.35 nM SANGER
NB10 Growth Inhibition Assay IC50=2.32 nM SANGER
BC-1 Growth Inhibition Assay IC50=2.31 nM SANGER
NB5 Growth Inhibition Assay IC50=2.27 nM SANGER
KMOE-2 Growth Inhibition Assay IC50=2.23 nM SANGER
SJSA-1 Growth Inhibition Assay IC50=2.21 nM SANGER
ES4 Growth Inhibition Assay IC50=2.16 nM SANGER
KGN Growth Inhibition Assay IC50=2.15 nM SANGER
EKVX Growth Inhibition Assay IC50=2.14 nM SANGER
MOLT-4 Growth Inhibition Assay IC50=2.13 nM SANGER
KE-37 Growth Inhibition Assay IC50=2.13 nM SANGER
HH Growth Inhibition Assay IC50=2.13 nM SANGER
GT3TKB Growth Inhibition Assay IC50=2.12 nM SANGER
BL-70 Growth Inhibition Assay IC50=2.12 nM SANGER
NOS-1 Growth Inhibition Assay IC50=2.11 nM SANGER
EW-24 Growth Inhibition Assay IC50=2.08 nM SANGER
LAN-6 Growth Inhibition Assay IC50=2.05 nM SANGER
NB17 Growth Inhibition Assay IC50=2.04 nM SANGER
LS-123 Growth Inhibition Assay IC50=2.02 nM SANGER
NB13 Growth Inhibition Assay IC50=2 nM SANGER
NKM-1 Growth Inhibition Assay IC50=2 nM SANGER
697 Growth Inhibition Assay IC50=1.99 nM SANGER
BE-13 Growth Inhibition Assay IC50=1.93 nM SANGER
MPP-89 Growth Inhibition Assay IC50=1.89 nM SANGER
Becker Growth Inhibition Assay IC50=1.83 nM SANGER
MV-4-11 Growth Inhibition Assay IC50=1.82 nM SANGER
GB-1 Growth Inhibition Assay IC50=1.81 nM SANGER
NCI-H1092 Growth Inhibition Assay IC50=1.8 nM SANGER
NCI-H2126 Growth Inhibition Assay IC50=1.8 nM SANGER
LC4-1 Growth Inhibition Assay IC50=1.79 nM SANGER
U-266 Growth Inhibition Assay IC50=1.76 nM SANGER
KURAMOCHI Growth Inhibition Assay IC50=1.72 nM SANGER
TGBC1TKB Growth Inhibition Assay IC50=1.71 nM SANGER
EHEB Growth Inhibition Assay IC50=1.67 nM SANGER
GCIY Growth Inhibition Assay IC50=1.62 nM SANGER
HEL Growth Inhibition Assay IC50=1.61 nM SANGER
NB12 Growth Inhibition Assay IC50=1.56 nM SANGER
NCI-H69 Growth Inhibition Assay IC50=1.54 nM SANGER
LS-411N Growth Inhibition Assay IC50=1.53 nM SANGER
PF-382 Growth Inhibition Assay IC50=1.47 nM SANGER
CAS-1 Growth Inhibition Assay IC50=1.37 nM SANGER
L-540 Growth Inhibition Assay IC50=1.37 nM SANGER
ECC12 Growth Inhibition Assay IC50=1.37 nM SANGER
DU-4475 Growth Inhibition Assay IC50=1.36 nM SANGER
OPM-2 Growth Inhibition Assay IC50=1.33 nM SANGER
IST-SL2 Growth Inhibition Assay IC50=1.31 nM SANGER
Calu-6 Growth Inhibition Assay IC50=1.29 nM SANGER
CMK Growth Inhibition Assay IC50=1.29 nM SANGER
A3-KAW Growth Inhibition Assay IC50=1.28 nM SANGER
K5 Growth Inhibition Assay IC50=1.28 nM SANGER
KM12 Growth Inhibition Assay IC50=1.27 nM SANGER
SR Growth Inhibition Assay IC50=1.25 nM SANGER
BL-41 Growth Inhibition Assay IC50=1.25 nM SANGER
Daudi Growth Inhibition Assay IC50=1.22 nM SANGER
NCI-H1882 Growth Inhibition Assay IC50=1.2 nM SANGER
TE-8 Growth Inhibition Assay IC50=1.19 nM SANGER
HAL-01 Growth Inhibition Assay IC50=1.18 nM SANGER
EM-2 Growth Inhibition Assay IC50=1.16 nM SANGER
CCRF-CEM Growth Inhibition Assay IC50=1.13 nM SANGER
D-392MG Growth Inhibition Assay IC50=1.1 nM SANGER
MZ7-mel Growth Inhibition Assay IC50=1.09 nM SANGER
VA-ES-BJ Growth Inhibition Assay IC50=1.09 nM SANGER
SK-MM-2 Growth Inhibition Assay IC50=1.09 nM SANGER
LC-2-ad Growth Inhibition Assay IC50=1.08 nM SANGER
RKO Growth Inhibition Assay IC50=1.06 nM SANGER
TE-10 Growth Inhibition Assay IC50=1.03 nM SANGER
TE-1 Growth Inhibition Assay IC50=1.03 nM SANGER
PSN1 Growth Inhibition Assay IC50=1.01 nM SANGER
SW872 Growth Inhibition Assay IC50=0.996 nM SANGER
HC-1 Growth Inhibition Assay IC50=0.975 nM SANGER
KALS-1 Growth Inhibition Assay IC50=0.925 nM SANGER
SF268 Growth Inhibition Assay IC50=0.923 nM SANGER
IST-MEL1 Growth Inhibition Assay IC50=0.917 nM SANGER
RXF393 Growth Inhibition Assay IC50=0.914 nM SANGER
SNB75 Growth Inhibition Assay IC50=0.912 nM SANGER
NCI-H1355 Growth Inhibition Assay IC50=0.895 nM SANGER
TE-5 Growth Inhibition Assay IC50=0.865 nM SANGER
QIMR-WIL Growth Inhibition Assay IC50=0.889 nM SANGER
SK-LMS-1 Growth Inhibition Assay IC50=0.854 nM SANGER
SW684 Growth Inhibition Assay IC50=0.821 nM SANGER
ML-2 Growth Inhibition Assay IC50=0.821 nM SANGER
D-263MG Growth Inhibition Assay IC50=0.807 nM SANGER
LB2241-RCC Growth Inhibition Assay IC50=0.804 nM SANGER
GI-1 Growth Inhibition Assay IC50=0.764 nM SANGER
ES7 Growth Inhibition Assay IC50=0.766 nM SANGER
LS-513 Growth Inhibition Assay IC50=0.739 nM SANGER
KINGS-1 Growth Inhibition Assay IC50=0.722 nM SANGER
UACC-257 Growth Inhibition Assay IC50=0.71 nM SANGER
LB373-MEL-D Growth Inhibition Assay IC50=0.7 nM SANGER
SF126 Growth Inhibition Assay IC50=0.701 nM SANGER
Ramos-2G6-4C10 Growth Inhibition Assay IC50=0.693 nM SANGER
TK10 Growth Inhibition Assay IC50=0.679 nM SANGER
D-336MG Growth Inhibition Assay IC50=0.657 nM SANGER
BB49-HNC Growth Inhibition Assay IC50=0.652 nM SANGER
HOP-62 Growth Inhibition Assay IC50=0.647 nM SANGER
LB831-BLC Growth Inhibition Assay IC50=0.641 nM SANGER
GI-ME-N Growth Inhibition Assay IC50=0.634 nM SANGER
A4-Fuk Growth Inhibition Assay IC50=0.623 nM SANGER
HT-144 Growth Inhibition Assay IC50=0.576 nM SANGER
COLO-829 Growth Inhibition Assay IC50=0.614 nM SANGER
NCI-H747 Growth Inhibition Assay IC50=0.539 nM SANGER
CESS Growth Inhibition Assay IC50=0.538 nM SANGER
HUTU-80 Growth Inhibition Assay IC50=0.533 nM SANGER
DSH1 Growth Inhibition Assay IC50=0.48 nM SANGER
LB771-HNC Growth Inhibition Assay IC50=0.474 nM SANGER
CP66-MEL Growth Inhibition Assay IC50=0.473 nM SANGER
OCUB-M Growth Inhibition Assay IC50=0.447 nM SANGER
MFH-ino Growth Inhibition Assay IC50=0.443 nM SANGER
OS-RC-2 Growth Inhibition Assay IC50=0.44 nM SANGER
HCE-T Growth Inhibition Assay IC50=0.439 nM SANGER
ES1 Growth Inhibition Assay IC50=0.43 nM SANGER
LB2518-MEL Growth Inhibition Assay IC50=0.425 nM SANGER
ACN Growth Inhibition Assay IC50=0.417 nM SANGER
D-247MG Growth Inhibition Assay IC50=0.413 nM SANGER
HCC2998 Growth Inhibition Assay IC50=0.412 nM SANGER
MZ2-MEL Growth Inhibition Assay IC50=0.407 nM SANGER
ES8 Growth Inhibition Assay IC50=0.4 nM SANGER
A388 Growth Inhibition Assay IC50=0.356 nM SANGER
KS-1 Growth Inhibition Assay IC50=0.34 nM SANGER
BB30-HNC Growth Inhibition Assay IC50=0.335 nM SANGER
ONS-76 Growth Inhibition Assay IC50=0.33 nM SANGER
D-542MG Growth Inhibition Assay IC50=0.329 nM SANGER
BB65-RCC Growth Inhibition Assay IC50=0.304 nM SANGER
LOUCY Growth Inhibition Assay IC50=0.293 nM SANGER
OVCAR-4 Growth Inhibition Assay IC50=0.289 nM SANGER
LXF-289 Growth Inhibition Assay IC50=0.269 nM SANGER
KNS-42 Growth Inhibition Assay IC50=0.258 nM SANGER
8-MG-BA Growth Inhibition Assay IC50=0.25 nM SANGER
NTERA-S-cl-D1 Growth Inhibition Assay IC50=0.243 nM SANGER
A101D Growth Inhibition Assay IC50=0.225 nM SANGER
MMAC-SF Growth Inhibition Assay IC50=0.216 nM SANGER
no-10 Growth Inhibition Assay IC50=0.21 nM SANGER
A253 Growth Inhibition Assay IC50=0.208 nM SANGER
TE-9 Growth Inhibition Assay IC50=0.182 nM SANGER
SH-4 Growth Inhibition Assay IC50=0.173 nM SANGER
SK-UT-1 Growth Inhibition Assay IC50=0.163 nM SANGER
ES6 Growth Inhibition Assay IC50=0.0021 nM SANGER
Molt4 Function assay EC50 = 0.021 μM 18247547
Molt4 Function assay EC50 = 0.021 μM 22503349
RPMI8226 Growth inhibition assay GI50 = 0.00023 μM 24946214
CCRF-CEM Growth inhibition assay GI50 = 0.00035 μM 24946214
MDA-MB-435 Growth inhibition assay GI50 = 0.00044 μM 24946214
MALME-3M Growth inhibition assay GI50 = 0.00045 μM 24946214
NCI-H226 Growth inhibition assay GI50 = 0.00046 μM 24946214
SK-MEL-28 Growth inhibition assay GI50 = 0.00046 μM 24946214
A498 Growth inhibition assay GI50 = 0.00048 μM 24946214
MOLT4 Growth inhibition assay GI50 = 0.00051 μM 24946214
OVCAR3 Growth inhibition assay GI50 = 0.00054 μM 24946214
SW620 Growth inhibition assay GI50 = 0.00055 μM 24946214
MCF7 Growth inhibition assay GI50 = 0.00055 μM 24946214
BT549 Growth inhibition assay GI50 = 0.00055 μM 24946214
UACC257 Growth inhibition assay GI50 = 0.00059 μM 24946214
SF539 Growth inhibition assay GI50 = 0.00059 μM 24946214
HCC2998 Growth inhibition assay GI50 = 0.0006 μM 24946214
HCT116 Growth inhibition assay GI50 = 0.0006 μM 24946214
T47D Growth inhibition assay GI50 = 0.0006 μM 24946214
CAKI-1 Growth inhibition assay GI50 = 0.00066 μM 24946214
SK-MEL-5 Growth inhibition assay GI50 = 0.00068 μM 24946214
RXF393 Growth inhibition assay GI50 = 0.00071 μM 24946214
LOXIMVI Growth inhibition assay GI50 = 0.00078 μM 24946214
ACHN Growth inhibition assay GI50 = 0.00079 μM 24946214
SR Growth inhibition assay GI50 = 0.00085 μM 24946214
UACC62 Growth inhibition assay GI50 = 0.00091 μM 24946214
M14 Growth inhibition assay GI50 = 0.00093 μM 24946214
HT-29 Growth inhibition assay GI50 = 0.00095 μM 24946214
HOP92 Growth inhibition assay GI50 = 0.001 μM 24946214
NCI-H23 Growth inhibition assay GI50 = 0.001 μM 24946214
TK10 Growth inhibition assay GI50 = 0.001 μM 24946214
Hs 578T Growth inhibition assay GI50 = 0.00102 μM 24946214
UO31 Growth inhibition assay GI50 = 0.00105 μM 24946214
SK-MEL-2 Growth inhibition assay GI50 = 0.00107 μM 24946214
SN12C Growth inhibition assay GI50 = 0.0011 μM 24946214
K562 Growth inhibition assay GI50 = 0.00117 μM 24946214
SF268 Growth inhibition assay GI50 = 0.00117 μM 24946214
COLO205 Growth inhibition assay GI50 = 0.00123 μM 24946214
MDA-MB-231 Growth inhibition assay GI50 = 0.00126 μM 24946214
NCI-H522 Growth inhibition assay GI50 = 0.00144 μM 24946214
786-0 Growth inhibition assay GI50 = 0.00144 μM 24946214
MDA-MB-468 Growth inhibition assay GI50 = 0.00148 μM 24946214
HCT15 Growth inhibition assay GI50 = 0.00151 μM 24946214
U251 Growth inhibition assay GI50 = 0.00155 μM 24946214
OVCAR5 Growth inhibition assay GI50 = 0.00155 μM 24946214
KM12 Growth inhibition assay GI50 = 0.0017 μM 24946214
SF295 Growth inhibition assay GI50 = 0.0017 μM 24946214
DU145 Growth inhibition assay GI50 = 0.0017 μM 24946214
HL-60(TB) Growth inhibition assay GI50 = 0.0019 μM 24946214
OVCAR4 Growth inhibition assay GI50 = 0.00195 μM 24946214
SNB19 Growth inhibition assay GI50 = 0.00204 μM 24946214
SNB75 Growth inhibition assay GI50 = 0.00204 μM 24946214
IGROV1 Growth inhibition assay GI50 = 0.00224 μM 24946214
OVCAR8 Growth inhibition assay GI50 = 0.00263 μM 24946214
PC3 Growth inhibition assay GI50 = 0.00263 μM 24946214
EKVX Growth inhibition assay GI50 = 0.00302 μM 24946214
A549/ATCC Growth inhibition assay GI50 = 0.00309 μM 24946214
HOP62 Growth inhibition assay GI50 = 0.00447 μM 24946214
NCI-H460 Growth inhibition assay GI50 = 0.00447 μM 24946214
NCI-ADR-RES Growth inhibition assay GI50 = 0.0123 μM 24946214
SKOV3 Growth inhibition assay GI50 = 0.0138 μM 24946214
NCI-H322M Growth inhibition assay GI50 = 0.0178 μM 24946214
A2780 Cytotoxicity assay IC50 = 0.0017 μM 18247547
RPMI8226 Cytotoxicity assay IC50 = 0.0088 μM 20727746
HCT116 Function assay Inhibition of proteasome in human HCT116 cells assessed as accumulation of p53 by Western blotting analysis 23547757
HCT116 Apoptosis assay Induction of apoptosis in human HCT116 cells assessed as induction of PARP cleavage by Western blotting analysis 23547757
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells 29435139
U-2 OS qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY 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
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) 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
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells 29435139
fibroblast qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells 29435139
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells 29435139
Rh30 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells 29435139
Rh30 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells 29435139
fibroblast qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for control Hh wild type fibroblast cells 29435139
U-2 OS qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for SK-N-SH cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells 29435139
Daoy qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for Daoy cells 29435139
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D caspase screen for TC32 cells 29435139
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for TC32 cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for MG 63 (6-TG R) cells 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 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
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells 29435139
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells 29435139
Rh18 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for SJ-GBM2 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for RD cells 29435139
HepG2 Cell viability assay HepG2 cells viability qHTS for Zika virus inhibitors 33229545
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生物活性

產(chǎn)品描述 Bortezomib是有效的蛋白酶抑制劑，Ki為0.6 nM。它對腫瘤細(xì)胞表現(xiàn)出良好的選擇性。Bortezomib可抑制 NF-κB 并誘導(dǎo) ERK 的磷酸化從而抑制cathepsin B并在卵巢癌和其他固體腫瘤中抑制自噬的催化過程。
靶點
NF-κB [6] 20S proteasome [1]
(Cell-free assay)
0.6 nM(Ki)
體外研究(In Vitro)
體外研究活性

Bortezomib，一種硼酸二肽，是一種26S蛋白酶體的高選擇性可逆抑制劑，其作用于錯誤折疊蛋白的降解，并且對細(xì)胞周期的調(diào)控是必要的。暴露于Bortezomib能夠穩(wěn)定p21，p27，和p53，以及促凋亡Bid和Bax蛋白，微囊蛋白-1，和抑制劑κB-α，這防止了核因子κB誘導(dǎo)的細(xì)胞存活途徑的激活。Bortezomib也會促進(jìn)促凋亡c-Jun-NH2末端激酶，以及內(nèi)質(zhì)網(wǎng)應(yīng)激反應(yīng)的激活。這些細(xì)胞蛋白水平的改變導(dǎo)致對增殖，遷移的抑制，和癌細(xì)胞凋亡的促進(jìn)。[2] Bortezomib能夠滲透到細(xì)胞，并抑制蛋白酶體介導(dǎo)的細(xì)胞內(nèi)長壽蛋白水解，抑制50%蛋白質(zhì)水解的濃度為∼0.1 μM。Bortezomib對衍生自美國國家癌癥研究所(NCI)多重人類腫瘤的一組60個癌細(xì)胞系的IC50值為7 nM。PC-3細(xì)胞用Bortezomib (100 nM)處理8小時導(dǎo)致細(xì)胞積聚在G2-M期，相應(yīng)的G1期細(xì)胞數(shù)量減少。Bortezomib在24和48小時殺死PC-3細(xì)胞，IC50分別為100和20 nM。Bortezomib治療16-24小時后誘導(dǎo)細(xì)胞核縮合。Bortezomib在低至100 nM濃度下以時間依賴的方式導(dǎo)致PARP裂解，在處理24小時后產(chǎn)生效果。[1]
激酶實驗 動力學(xué)法
在典型的動力學(xué)試驗中，2.00 mL試驗緩沖液(20 mM HEPES，0.5 mM EDTA，0.035% SDS，pH 7.8) 和 Suc-Leu-Leu-Val-Tyr-AMC溶于DMSO，加入3 mL熒光比色皿中，并將比色皿放置于熒光分光光度計的夾套細(xì)胞皿座。反應(yīng)溫度通過循環(huán)水浴維持在37℃。反應(yīng)溶液達(dá)到熱平衡后(5 分鐘)，1 μL?10 μL儲存酶溶液加入培養(yǎng)皿。伴隨AMC 從多肽AMC底物裂解的反應(yīng)進(jìn)程通過440 nm (λex= 380 nm)下熒光發(fā)射的增加監(jiān)測。
細(xì)胞實驗 細(xì)胞系 人多發(fā)性骨髓瘤細(xì)胞系U266
濃度 ~10 μM
孵育時間 2天
方法

通過測定細(xì)胞吸收 MTT染料的情況而測定 Bortezomib對 MM和 BMSC 生長的抑制情況。每孔使用10 μL 5 mg/mL MTT對培養(yǎng)48小時的細(xì)胞進(jìn)行脈沖處理，至少處理4小時， 隨后加入100 μL 含0.04 N HCl的異丙醇 。使用分光光度計在 570 nm處測定吸光值。
實驗圖片 檢測方法 檢測指標(biāo) 實驗圖片 PMID
Western blot phospho-PERK / ATF-4 GRP-78 / GADD-34 pro-caspase-12 / pro-caspase-3 pro-caspase-9 p-IκBα / IκBα COX-2 / cIAP2 15509775
Immunofluorescence Vimentin Ubiquitin 19010849
Growth inhibition assay Cell viability 20571067
ELISA IL-8 24085292
體內(nèi)研究(In Vivo)
體內(nèi)研究活性

Bortezomib單一用藥的抗癌作用已在多發(fā)性骨髓瘤的異種移植模型，成人白血病，肺癌，乳腺癌，前列腺癌，胰腺癌，頭頸癌，和結(jié)腸癌，以及在黑色素瘤中得到證實。[2]在Lewis肺癌模型中，口服bortezomib (1.0 mg/ kg，每天)，服用18天引起腫瘤生長延遲，并減少轉(zhuǎn)移數(shù)量。Bortezomib單一用藥， 高達(dá)5 mg/kg劑量時顯著降低乳腺癌細(xì)胞的存活率。在前列腺癌小鼠異種移植模型中，Bortezomib (1.0 mg/kg，每周一次)用藥4周減少60%腫瘤生長。1.0 mg/kg Bortezomib給藥4周導(dǎo)致胰腺癌小鼠異種移植物生長減少72%或84%，并導(dǎo)致腫瘤細(xì)胞凋亡增加。1.0 mg/kg Bortezomib顯著抑制人漿細(xì)胞瘤異種移植物生長，增加腫瘤細(xì)胞凋亡和總存活率，并減少腫瘤血管生成。[3]
動物實驗 Animal Models 人漿細(xì)胞瘤異種移植物RPMI 8226
Dosages 1mg/kg
Administration i.v.，一周兩次，使用4周，然后一周一次
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05599880 Recruiting
Relapsed/Refractory Immune Thrombocytopenia
Seoul National University Hospital
 July 7 2023 Phase 2
NCT05781425 Recruiting
Chemotherapy-induced Peripheral Neuropathy
Odense University Hospital|Aarhus University Hospital|Sygehus Lillebaelt|University of Southern Denmark
 May 12 2023 --
NCT05383547 Unknown status
Bortezomib|Glomerulonephritis|MN|MPGN|FSGS|IgA Nephropathy
Ruijin Hospital
 August 2 2022 Not Applicable
NCT04915248 Recruiting
Plasmablastic Lymphoma
Fondazione Italiana Linfomi - ETS|Janssen-Cilag S.p.A.
 July 11 2022 Phase 2
NCT04656951 Recruiting
Multiple Myeloma
University of Cologne|Janssen-Cilag G.m.b.H
 June 1 2021 Phase 2

化學(xué)信息&溶解度

分子量 384.24 分子式

C19H25BN4O4
CAS號 179324-69-7 SDF Download Bortezomib SDF
Smiles B(C(CC(C)C)NC(=O)C(CC1=CC=CC=C1)NC(=O)C2=NC=CN=C2)(O)O
儲存條件(自收到貨起) 3年 -20°C(避光) 粉狀

體外溶解度
批次：

DMSO : 77 mg/mL ( (200.39 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
批次：

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

實驗計算

摩爾濃度計算器

質(zhì)量 濃度 體積 分子量

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）

mg/kg g μL 只

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）

% DMSO % % Tween 80 % ddH2O
%DMSO %

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(jìn)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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常見問題及建議解決方法

問題 1:
On your website, it is mentioned that Bortezomib should be prepared at a concentration of 5 mg/ml in 2% DMSO/30% PEG300/ddH2O for in vivo use. But on the product sheet we received with the compound, it is mentioned: 5mg/ml in 0.5% methylcellulose, 0.2% tween 80. So which is the correct preparation buffer?

回答：
S1013 Bortezomib in 2% DMSO+30% PEG 300+ddH2O at 5 mg/ml is a clear solution, and it in 0.5% methylcellulose+0.2% Tween 80 is a suspension. Please choose the suitable vehicle according to your administration route. When you prepare the clear solution, please dissolve Bortezomib in DMSO first, make sure it dissolves well, warm it up to 45 degree and/or sonicate if necessary, then add PEG, mix well, and finally add water.

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