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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-Cyclin-dependent Kinase (CDK)-THZ1
THZ1

Chemical Structure : THZ1

CAS No.: 1604810-83-4

THZ1 (CDK7 inhibitor THZ-1)

货号: PC-46008Not For Human Use, Lab Use Only.

THZ1 is a potent, selective, covalent CDK7 inhibitor with IC50 of 3.2 nM, also weakly inhibits CDK12 with IC50 of 250 nM.

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

生物&药学活性

THZ1 is a potent, selective, covalent CDK7 inhibitor with IC50 of 3.2 nM, also weakly inhibits CDK12 with IC50 of 250 nM.
THZ1 displays broad-based activity a subset of cancer cell lines with IC50s of <200 nM.
THZ1 causes decreased cellular proliferation and an increase in apoptotic index (MCL-1, XIAP), disproportionally affects transcription of RUNX1 in Jurkat T-ALL cells.
THZ1 demonstrates efficacy against primary leukemia cells and in a bioluminescent xenografted model at 10mg/kg.

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: ≥ 27 mg/mL

Chemical Name/SMILES

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

参考文献

1. Kwiatkowski N, et al. Nature. 2014 Jul 31;511(7511):616-20.

2. Chipumuro E, et al. Cell. 2014 Nov 20;159(5):1126-39.

3. Christensen CL, et al. Cancer Cell. 2014 Dec 8;26(6):909-22.

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