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THZ2

Chemical Structure : THZ2

CAS No.: 1604810-84-5

THZ2 (CDK7 inhibitor, THZ-2)

货号: PC-42944Not For Human Use, Lab Use Only.

THZ2, an analogue of THZ1 with improved pharmacokinetic features, is a potent, selective CDK7 inhibitor with IC50 of 13.9 nM, displays a 5-fold improved half-life in vivo compared with THZ1.

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

生物&药学活性

THZ2, an analogue of THZ1 with improved pharmacokinetic features, is a potent, selective CDK7 inhibitor with IC50 of 13.9 nM, displays a 5-fold improved half-life in vivo compared with THZ1.
THZ2 selectively targets CDK7 and potently inhibits the growth of triple-negative but not ER/PR+ breast cancer cells, efficiently suppresses the clonogenic growth of TNBC cells with IC50 of 10 nM.
Like THZ1, THZ2 induces apoptotic cell death in triple-negative but not ER/PR+ breast cancer cells or normal human cells.
THZ2 suppresses the growth of triple-negative breast tumors in xenograft models.

物理化学性质&存储条件

分子量 566.0527
分子式 C31H28ClN7O2
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

DMSO: ≥ 39 mg/mL

Chemical Name/SMILES

Benzamide, N-[3-[[5-chloro-4-(1H-indol-3-yl)-2-pyrimidinyl]amino]phenyl]-3-[[(2E)-4-(dimethylamino)-1-oxo-2-buten-1-yl]amino]-

参考文献

1. Wang Y, et al. Cell. 2015 Sep 24;163(1):174-86.

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