CDK12-IN-2|2244987-03-7|-陌孚医药/Medlife

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CDK12-IN-2

目录号: PL02075 纯度: ≥99%

CAS No. :2244987-03-7

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中文名称	CDK12-IN-2
英文名称	CDK12-IN-2
英文别名	CDK12 inhibitor 2;GTPL10063;TQP0780;BDBM50367676;3-benzyl-1-(4-((5-cyanopyridin-2-yl)amino)cyclohexyl)-1-(4-(1-methyl-6-oxo-1,6-dihydropyridin-3-yl)phenyl)urea;3-Benzyl-1-(trans-4-((5-cyanopyridin-2-yl)amino)cyclohexyl)-1-(4-(1-methyl-6-oxo-1,6-dihydropyridin-3-yl)phenyl)urea;Urea, N-?[trans-?4-?[(5-?cyano-?2-?pyridinyl)?amino]?cyclohexyl]?-?N-?[4-?(1,?6-?dihydro-?1-?methyl-?6-?oxo-?3-?pyridinyl)?phenyl]?-?N'-?(phenylmethyl)?-;CDK12-IN-2
Cas No.	2244987-03-7
分子式	C₃₂H₃₂N₆O₂
分子量	532.64
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	CDK12-IN-2是一种高效、选择性的纳摩尔级别的CDK12 抑制剂 (IC₅₀=52 nM)，具有良好的物理化学性质。CDK12-IN-2也是一种强的CDK13抑制剂，因为CDK13是CDK12最接近的同源物。CDK12-IN-2对CDK12的激酶选择性比CDK2、9、8和7高。CDK12-IN-2抑制RNA polymerase II 的 C端Ser2磷酸化。CDK12-IN-2可以作为一种很好的化学探针用于CDK12的功能研究。
生物活性	CDK12-IN-2 is a potent, selective and nanomolar CDK12 inhibitor (IC 50 =52 nM) with good physicochemical properties. CDK12-IN-2 is also a strong CDK13 inhibitor due to CDK13 is the closest homologue of CDK12. CDK12-IN-2 shows excellent kinase selectivity for CDK12 over CDK2, 9, 8, and 7. CDK12-IN-2 inhibits the phosphorylation of Ser2 in the C-terminal domain of RNA polymerase II. CDK12-IN-2 can be used an excellent chemical probe for functional studies of CDK12.
性状	Solid
IC50 & Target[1][2]	CDK12 52 nM (IC50) CDK2 >100 μM (IC
体外研究(In Vitro)	CDK12-IN-2 inhibits the phosphorylation of the CTD Ser2 in SK-BR-3 cells at low submicromolar concentrations, it inhibits C-terminal domain ser2 phosphorylation with an IC50 of 185 nM. And CDK12-IN-2 exhibits a growth inhibition with an IC50 of 0.8 μM in SK-BR-3 cells. CDK12-IN-2 exhibits time dependency for CDK12 inhibition, the IC50 value for CDK12-IN-2 are 0.0078 μM, 0.042 μM, 0.057 μM,and 0.059 μM, for 0h, 1h, 2h and 5h respectively. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Powder -20°C 3 years；4°C 2 years
参考文献	[1]. Masahiro Ito, et al. Discovery of 3-Benzyl-1-( trans-4-((5-cyanopyridin-2-yl)amino)cyclohexyl)-1-arylurea Derivatives as Novel and Selective Cyclin-Dependent Kinase 12 (CDK12) Inhibitors. J Med Chem. 2018 Sep 13;61(17):7710-7728.

溶解度数据	In Vitro: DMSO : 50 mg/mL (93.87 mM; ultrasonic and warming and heat to 60°C)配制储备液

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