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CDK12 inhibitor 2

Chemical Structure : CDK12 inhibitor 2

CAS No.: 2244987-03-7

CDK12 inhibitor 2 (CDK12-IN-2)

Catalog No.: PC-35525Not For Human Use, Lab Use Only.

CDK12 inhibitor 2 is (CDK12-IN-2) is a potent, selective, non-covalent CDK12 inhibitor with IC50 of 52 nM, displays >192-fold selectivity over CDK2/7/8/9.

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Biological Activity

CDK12 inhibitor 2 is (CDK12-IN-2) is a potent, selective, non-covalent CDK12 inhibitor with IC50 of 52 nM, displays >192-fold selectivity over CDK2/7/8/9.
CDK12 inhibitor 2 also potently inhibitor CDK13 with IC50 of 10 nM.
CDK12 inhibitor 2 inhibits the phosphorylation of Ser2 in the C-terminal domain (CTD) of RNA polymerase II in SK-BR-3 cells at low submicromolar concentrations (iC50=0.195 uM), inhibits the growth of SK-BR-3 cells with IC50 of 0.8 uM.

Physicochemical Properties

M.Wt 532.648
Formula C32H32N6O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

3-benzyl-1-((1r,4r)-4-((5-cyanopyridin-2-yl)amino)cyclohexyl)-1-(4-(1-methyl-6-oxo-1,6-dihydropyridin-3-yl)phenyl)urea

References

1. Ito M, et al. J Med Chem. 2018 Aug 1. doi: 10.1021/acs.jmedchem.8b00683.

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