1. Cell Cycle/DNA Damage
  2. CDK
  3. CDK12-IN-9

CDK12-IN-9 是一种强效且高选择性的 CDK12 抑制剂,其 IC50 为 2.2 nM。CDK12-IN-9 可抑制 pSER2 (CDK12/13 活性的下游标志物)。CDK12-IN-9 可用于癌症研究。

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CDK12-IN-9

CDK12-IN-9 Chemical Structure

CAS No. : 3024723-74-5

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CDK12-IN-9 is a potent and selective CDK12 inhibitor with an IC50 of 2.2 nM. CDK12-IN-9 inhibits pSER2 (a downstream marker of CDK12/13 activity). CDK12-IN-9 can be used for the research of cancer[1].

IC50 & Target[1]

CDK12

2.2 nM (IC50)

CDK13

13 nM (IC50)

CDK9

466 nM (IC50)

CDK2

551 nM (IC50)

CDK7

1491 nM (IC50)

体外研究
(In Vitro)

CDK12-IN-9 (Compound 17) 可强效抑制纯化的 CDK12 激酶,其 IC50 为 2.2 ± 0.74 nM[1]
CDK12-IN-9 可抑制抑制纯化的 CDK13、CD9、CD7 和 CD2 激酶,其 13、466、1491 和 551 nM[1]
CDK12-IN-9 可抑制细胞内 pSER2 (CDK12/13 活性的下游标志物),其 IC50 为 17 ± 4.1 nM[1]
CDK12-IN-9 可抑制全血中的 pSER2 活性,其 IC50 为 209 ± 106 nM[1]

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

药代动力学
(Parmacokinetics)
Species Dose Route Cmax AUC T1/2 F
Mice[1] 0.2 mg/kg i.v. / / 3.6 h /
Mice[1] 3 mg/kg p.o. 1320 nM 9518 nM·h / 72 %
Cynomolgus Monkey[1] 0.3 mg/kg p.o. 94 nM 983 nM·h / /
Dog[1] 0.3 mg/kg p.o. 137 nM 1035 nM·h / /
分子量

474.47

Formula

C23H20F2N10

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
  • 摩尔计算器

  • 稀释计算器

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

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Help & FAQs
  • 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-9
目录号:
HY-181645
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