1. Cell Cycle/DNA Damage Stem Cell/Wnt JAK/STAT Signaling
  2. CDK STAT Wnt
  3. CDK8-IN-16

CDK8-IN-16 (Compound 51) 是口服有效的 CDK8CDK19 双重抑制剂,IC50 分别为 5.1 nM 和 5.6 nM。CDK8-IN-16 在 SW620 细胞中抑制 STAT1SER727 磷酸化,IC50 为 17.9 nM,在 7dF3 细胞中抑制 WNT 信号通路,IC50 为 7.2 nM。CDK8-IN-16 在大鼠模型中表现出良好的药代动力学特征,口服生物利用度为 57%。

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CDK8-IN-16 Chemical Structure

CDK8-IN-16 Chemical Structure

CAS No. : 1860885-61-5

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CDK8-IN-16 (Compound 51) is an orally active dual inhibitor for CDK8 and CDK19 wih IC50 of 5.1 nM and 5.6 nM. CDK8-IN-16 inhibits the phospho-STAT1SER727 with an IC50 of 17.9 nM in SW620 cell, inhibits WNT signaling pathway with an IC50 of 7.2 nM in 7dF3 cell. CDK8-IN-16 exhibits good pharmacokinetic characteristics in rat models with an oral bioavailability of 57%[1].

IC50 & Target

CDK8

5.1 nM (IC50)

CDK19

5.6 nM (IC50)

分子量

414.46

Formula

C23H22N6O2

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.

纯度 & 产品资料
参考文献
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产品名称:
CDK8-IN-16
目录号:
HY-171174
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