0576-88813233
THZ1 是有效,选择性的共价 CDK7 抑制剂,IC50 为 3.2 nM。THZ1 还抑制相关的激酶 CDK12 和 CDK13,并下调 MYC 表达。
中文别名:
2-[(3,5-二氟-4-羟基苯基)氨基]-7,8-二氢-5,7-二甲基-8-(3-甲基丁基)-6(5H)-蝶啶
物化属性:
密度:1.297
沸点:579.3°C at 760 mmHg
折射率:1.585
闪光点:304.2°C
PSA:81.59000
LOGP:3.62440
[1]. Kwiatkowski N, et al. Targeting transcription regulation in cancer with a covalent CDK7 inhibitor. Nature. 2014 Jul 31;511(7511):616-20.
[2]. Jiang YY, et al. Targeting super-enhancer-associated oncogenes in oesophageal squamous cell carcinoma. Gut. 2016 May 10. pii: gutjnl-2016-311818.
[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.
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