Cdk/Crk Inhibitor | CAS 784211-09-2

Element: inhibitor

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C-S » Chemicals » cdk-crk-inhibitor-PX80817

Identification

Cdk/Crk Inhibitor

CAS:

784211-09-2

EINECS:

Molecular Formula:

C₂₃H₂₂Cl₂N₄O₃

MDL:

SMILES:

CC(C)C1=C2C(=NC(=NC2=O)CC3=CC=C(C=C3)OCCO)N(N1)C4=C(C=CC=C4Cl)Cl

Synonym:

4H-Pyrazolo[3,4-d]pyrimidin-4-one, 1-(2,6-dichlorophenyl)-1,5-dihydro-6-[[4-(2-hydroxyethoxy)phenyl]methyl] -3-(1-methylethyl)-

Description

Cdk/Crk Inhibitor is a cell-permeable pyrazolo-pyrimidinone compound that acts as a potent, selective, and ATP-competitive inhibitor of Cdks (IC₅₀ = 48 nM, 15 nM, 9 nM, 10 nM, 71 nM, and 9 nM for Cdc2 (Cdk1)/cyclin B, Cdk2/cyclin E, Cdk3/cyclin E, Cdk5/p35, Cdk7/cyclin H/MAT1, and Cdk9, respectively). It inhibits Cdk4/cyclin D1, Cdk6/cyclin D3, and GSK-3β only at much higher concentrations (IC₅₀ = 839 nM, 282 nM, and 754 nM, respectively) and exhibits little activity towards a panel of 60 other kinases. Cdk/Crk Inhibitor is a broad-spectrum growth inhibitor toward tumor cells, but not non-transformed quiescent fibroblasts.