THZ1

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Chemical Structure| 1604810-83-4 同义名 : -
CAS号 : 1604810-83-4
货号 : A218107
分子式 : C31H28ClN7O2
纯度 : 98%+
分子量 : 566.05
MDL号 : MFCD28167785
存储条件：

Pure form Keep in dark place, inert atmosphere, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：

IP 2% DMSO+water 8 mg/mL clear

PO 0.5% CMC-Na 22 mg/mL suspension

生物活性
描述 THZ1 is a potent and selective covalent inhibitor of CDK7 with an IC50 of 3.2 nM, affecting CDK12 and CDK13 at higher concentrations and leading to the downregulation of MYC expression.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.77mL

0.35mL

0.18mL

8.83mL

1.77mL

0.88mL

17.67mL

3.53mL

1.77mL
参考文献

[1]Kwiatkowski N, et al. Targeting transcription regulation in cancer with a covalent CDK7 inhibitor. Nature. 2014 Jul 31;511(7511):616-20.

[2]Zeng M, et al. Targeting MYC dependency in ovarian cancer through inhibition of CDK7 and CDK12/13. Elife. 2018 Nov 13;7. pii: e39030.

[3]Christensen CL, et al. Targeting transcriptional addictions in small cell lung cancer with a covalent CDK7 inhibitor. Cancer Cell. 2014 Dec 8;26(6):909-22.

[4]Chipumuro, et al. CDK7 inhibition suppresses super-enhancer-linked oncogenic transcription in MYCN-driven cancer. Cell. 2014 Nov 20;159(5):1126-39. ?

[5]Jiang YY, et al. Targeting super-enhancer-associated oncogenes in oesophageal squamous cell carcinoma. Gut. 2016 May 10. pii: gutjnl-2016-311818.