Chemical Structure : BSJ-01-175
CAS No.: 2227392-55-2
货号: PC-23502Not For Human Use, Lab Use Only.
BSJ-01-175 is a potent, selective dual CDK12/13 covalent inhibitor with IC50 of 156 nM (CDK12/CycK) and 282.6 nM(CDK3/CycK), targets cysteine Cys1039 on CDK12 (or Cys1017 on CDK13).
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BSJ-01-175 is a potent, selective dual CDK12/13 covalent inhibitor with IC50 of 156 nM (CDK12/CycK) and 282.6 nM(CDK3/CycK), targets cysteine Cys1039 on CDK12 (or Cys1017 on CDK13).
BSJ-01-175 specifically targets CDK12/13 and suppresses the transcription of BRAC1 and BRAC2.
BSJ-01-175 exhibits antiproliferative activity of BSJ-01-175 in TC71 Ewing sarcoma cells with IC50 of 160 nM.
BSJ-01-175 (10 mg/kg, IP qD) suppresses tumor growth of Ewing sarcoma in TC71 xenograft mouse model of Ewing sarcoma.
分子量 | 545.08 | |
分子式 | C30H33ClN6O2 | |
外观性状 | Solid | |
储存条件 |
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Solubility |
10 mM in DMSO |
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Chemical Name/SMILES |
(E)-N-(4-(((1R,3R)-3-((5-chloro-4-(1H-indol-3-yl)pyrimidin-2-yl)amino)cyclohexyl)oxy)phenyl)-4-(dimethylamino)but-2-enamide |
1. Jiang B, et al. Eur J Med Chem. 2021 Oct 5;221:113481.
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