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CDK7/9-IN-1

CDK7/9-IN-1 是一种细胞周期蛋白依赖性激酶 7/9 (CDK7/9) 抑制剂。CDK7/9-IN-1 选择性抑制 CDK7。CDK7/9-IN-1 在非预孵育和预孵育 3 小时后抑制 CDK7，IC₅₀ 分别为 0.0656 μM 和 0.00574 μM。 CDK7/9-IN-1 在预孵育 3 小时后抑制 CDK9，IC₅₀ 为 2.14 μM。 CDK7/9-IN-1可用于癌症研究。

CDK7/9-IN-1 Chemical Structure

CAS No. : 2747919-19-1

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生物活性

CDK7/9-IN-1 is a cyclin-dependent kinases 7/9 (CDK7/9) inhibitor. CDK7/9-IN-1 selectively inhibits CDK7 over CDK9. CDK7/9-IN-1 inhibits CDK7 with IC₅₀s of 0.0656 μM and 0.00574 μM without pre-incubation and after 3 hours pre-incubation, respectively. CDK7/9-IN-1 inhibits CDK9 with an IC₅₀ of 2.14 μM after 3 hours pre-incubation. CDK7/9-IN-1 can be used for the research of cancer^[1].

IC₅₀ & Target^[1]

CDK7

5.74-65.6 nM (IC₅₀)

CDK9

2.14 μM (IC₅₀)

体外研究
(In Vitro)

CDK7/9-IN-1 (example 8; 0.001-20 μM; 4 h) inhibits CDK7 with an relative IC₅₀ of 0.0262 μM for phospho-carboxyl terminal domain (Rbp2) (Ser5) in HCT116 cells^[1].
CDK7/9-IN-1 (0.001-20 μM; 4 h) inhibits CDK9 with an IC₅₀ of 2.59 μM for phospho-carboxyl terminal domain (Rbp2) (Ser2) in HCT116 cells^[1].
CDK7/9-IN-1 (0.001-20 μM; 4 h) inhibits cMyc with an relative IC₅₀ of 0.0138 μM in HCT116 cells^[1].
CDK7/9-IN-1 (20 μΜ, 2 μΜ, and 0.2 μΜ; 1 h) shows excellent selectivity against the 468 protein kinases panel. CDK7/9-IN-1 shows approximately 96% inhibition against CDK7^[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

479.54

Formula

C₂₄H₃₂F₃N₅O₂

CAS 号

2747919-19-1

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.

参考文献

[1]. Maria Carmen FERNANDEZ FIGUEROA, et al. Compounds useful for inhibiting cdk7. WO2021242602 A1.

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