1. Cell Cycle/DNA Damage
  2. CDK
  3. CDK12-IN-8

CDK12-IN-8 (Compound Cpd143) 是一种具有口服活性,高选择性的细胞周期蛋白依赖性激酶 12 (CDK12) 抑制剂。CDK12-IN-8 抑制 CDK12 对 RNA 聚合酶 II C 端结构域 (CTD) 丝氨酸 2 的磷酸化,干扰基因转录延伸和 DNA 损伤修复通路。CDK12-IN-8 有望用于 CDK12 高表达癌症的研究,如小细胞肺癌和三阴性乳腺癌。

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CDK12-IN-8 Chemical Structure

CDK12-IN-8 Chemical Structure

CAS No. : 2928619-86-5

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  • 生物活性

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  • 参考文献

生物活性

CDK12-IN-8 (Compound Cpd143) is an orally active and highly selective inhibitor of cyclin-dependent kinase 12 (CDK12). CDK12-IN-8 inhibits CDK12-mediated phosphorylation of the C-terminal domain (CTD) serine 2 of RNA polymerase II, interfering with gene transcription elongation and DNA damage repair pathways. CDK12-IN-8 is promising for research of cancers with high CDK12 expression such as small cell lung cancer and triple-negative breast cancer[1].

IC50 & Target

CDK12

 

分子量

459.42

Formula

C21H20F3N7O2

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

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参考文献
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产品名称:
CDK12-IN-8
目录号:
HY-171786
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