1. Cell Cycle/DNA Damage
  2. CDK
  3. CDK12-IN-6

CDK12-IN-6 是一种吡唑并三嗪,是有效的 CDK12 抑制剂,在高 ATP (2 mM) 下的 IC50 为 1.19 μM。CDK12-IN-6 在高 ATP (2 mM) 下对 CDK2/Cyclin E (IC50>20 μM) 和 CDK9/Cyclin T1 (IC50>20 μM) 没有影响(WO2021116178A1)。

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CDK12-IN-6 Chemical Structure

CDK12-IN-6 Chemical Structure

CAS No. : 2651196-71-1

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CDK12-IN-6, a pyrazolotriazine, is a potent CDK12 inhibitor with an IC50 of 1.19 μM at high ATP (2 mM). CDK12-IN-6 has no effect on CDK2/Cyclin E (IC50>20 μM) and CDK9/Cyclin T1 (IC50>20 μM) at high ATP (2 mM) (WO2021116178A1)[1].

IC50 & Target[1]

CDK12

1.19 μM (IC50)

CDK2/cyclinE

>20 μM (IC50)

CDK9/cyclinT1

>20 μM (IC50)

体外研究
(In Vitro)

CDK12-IN-6 (Example 174) inhibits BRCA1 MRNA expression in MDA-MB-231 cells (IC50=0.872 nM) and has no effect on CAL-120 cells[1].
CDK12-IN-6 has antproliferative activity in MDA-MB-231 cells (IC50=2.19 nM) and CAL-120 cells (IC50=1 nM)[1].
CDK12-IN-6 has a inhibition IC50 CDK12 high ATP to Degradation DC50 CDK12 ratio of 1851[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

425.44

Formula

C20H21F2N9

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

CDK12-IN-6 相关分类

  • 摩尔计算器

  • 稀释计算器

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
CDK12-IN-6
目录号:
HY-139329
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