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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-Cyclin-dependent Kinase (CDK)-BSJ-01-175
BSJ-01-175

Chemical Structure : BSJ-01-175

CAS No.: 2227392-55-2

BSJ-01-175

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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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.

物理化学性质&存储条件

分子量 545.08
分子式 C30H33ClN6O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

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

参考文献

1. Jiang B, et al. Eur J Med Chem. 2021 Oct 5;221:113481.

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