SR 3029

SR 3029 is an inhibitor of casein kinase 1delta (CK1delta) and CK1epsilon (IC50s = 44 and 260 nM, respectively). It is selective for CK1delta and CK1epsilon over 438 kinases in a panel but also inhibits MYLK4, FLT3, Cdk4/cyclin D1, and MARK2 by greater than 90% at 10 µM. SR 3029 inhibits Cdk4/cyclin D1, Cdk4/cyclin D3, Cdk6/cyclin D1, Cdk6/cyclin D3, and FLT3 with IC50 values of 576, 368, 428, 427, and 3,000 nM, respectively. It inhibits proliferation of A375 human melanoma cells in vitro (EC50 = 86 nM). SR 3029 (20 mg/kg per day) reduces tumor growth and increases lifespan in MDA-MB-231 and MDA-MB-468 mouse xenograft models. It reduces the expression of the Wnt/beta-catenin target CCND1 and decreases protein levels of nuclear beta-catenin and cyclin D1 in mouse tumor tissue.Formal Name: N-[(6,7-difluoro-1H-benzimidazol-2-yl)methyl]-9-(3-fluorophenyl)-2-(4-morpholinyl)-9H-purin-6-amine. CAS Number: 1454585-06-8. Molecular Formula: C23H19F3N8O. Formula Weight: 480.5. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml. lambdamax: 231, 281 nm. SMILES: FC1=C(F)C(N2)=C(C=C1)N=C2CNC3=C4C(N(C5=CC=CC(F)=C5)C=N4)=NC(N6CCOCC6)=N3. InChi Code: InChI=1S/C23H19F3N8O/c24-13-2-1-3-14(10-13)34-12-28-20-21(31-23(32-22(20)34)33-6-8-35-9-7-33)27-11-17-29-16-5-4-15(25)18(26)19(16)30-17/h1-5,10,12H,6-9,11H2,(H,29,30)(H,27,31,32). InChi Key: CEBMEQPREMCWOL-UHFFFAOYSA-N.