CDK/CRK Inhibitor

CDK/CRK inhibitor is an inhibitor of cyclin-dependent kinases (CDK) and CDK-related kinases (CRK) with IC50 values ranging from 9-839 nM in vitro. It is selective, exhibiting less than 20% inhibition of 60 non-CDK/CRK kinases, at a concentration of 1 µM. CDK/CRK inhibitor induces cell cycle arrest in the G1 phase, endoreduplication, and apoptosis in HCT116 cells. It exhibits broad anti-tumor activity with an average GI50 value of 50 value of 40 nM.Formal Name: 1-(2,6-dichlorophenyl)-1,5-dihydro-6-[[4-(2-hydroxyethoxy)phenyl]methyl]-3-(1-methylethyl)-4H-pyrazolo[3,4-d]pyrimidin-4-one. CAS Number: 784211-09-2. Synonyms: Cdk7 Inhibitor IV, Cyclin-dependent kinase 7 Inhibitor IV, Cyclin-dependent kinase/CDK-related kinase Inhibitor, RGB-286147. Molecular Formula: C23H22Cl2N4O3. Formula Weight: 473.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, DMSO:PBS (pH 7.2) (1:4): 0.2 mg/ml. lambdamax: 214 nm. SMILES: O=C1C2=C(N(C3=C(Cl)C=CC=C3Cl)N=C2C(C)C)NC(CC4=CC=C(OCCO)C=C4)=N1. InChi Code: InChI=1S/C23H22Cl2N4O3/c1-13(2)20-19-22(29(28-20)21-16(24)4-3-5-17(21)25)26-18(27-23(19)31)12-14-6-8-15(9-7-14)32-11-10-30/h3-9,13,30H,10-12H2,1-2H3,(H,26,27,31). InChi Key: RSQPNXBTPUXMQN-UHFFFAOYSA-N.