CCT241736

CCT241736 is a dual inhibitor of Aurora kinases (Kds = 7.5 and 48 nM for Aurora A and B, respectively) and FLT3 (Kds = 6.2, 38, and 14 nM for wild-type, FLT3ITD, and FLT3D835Y, respectively). It also inhibits the activity of 22 additional kinases by greater than 90% in a panel of 386 nonmutant kinases at 1 µM. CCT241736 inhibits cell growth of SW620, HCT116, MOLM-13, and MV4-11 cancer cells (GI50s = 1, 0.3, 0.1, and 0.3 µM, respectively). Oral administration of CCT241736 (50 mg/kg twice per day) reduces tumor growth by 58% in an MV4-11 mouse xenograft model.Formal Name: 6-chloro-7-[4-[(4-chlorophenyl)methyl]-1-piperazinyl]-2-(1,3-dimethyl-1H-pyrazol-4-yl)-3H-imidazo[4,5-b]pyridine. CAS Number: 1402709-93-6. Molecular Formula: C22H23Cl2N7. Formula Weight: 456.4. Purity: >90%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 10mg/mL, DMF:PBS (pH 7.2) (1:2): 0.3mg/mL, DMSO: 2mg/mL. lambdamax: 218, 256, 310 nm. SMILES: ClC1=CN=C(N=C(C2=CN(C)N=C2C)N3)C3=C1N4CCN(CC5=CC=C(Cl)C=C5)CC4. InChi Code: InChI=1S/C22H23Cl2N7/c1-14-17(13-29(2)28-14)21-26-19-20(18(24)11-25-22(19)27-21)31-9-7-30(8-10-31)12-15-3-5-16(23)6-4-15/h3-6,11,13H,7-10,12H2,1-2H3,(H,25,26,27). InChi Key: AKJBLKUZXRMECW-UHFFFAOYSA-N.