FLT3-IN-3

FLT3-IN-3 is an inhibitor of FMS-related tyrosine kinase 3 (FLT3). It inhibits wild-type, FLT3D835Y, and FLT3 bearing internal-tandem duplication (FLT3-ITD, IC50s = 13, 8, and 3 nM, respectively). FLT3-IN-3 suppresses the growth of MV4-11 acute myeloid leukemia (AML) cells that express FLT3-ITD (GI50 = 7 nM). It induces cell cycle arrest at the G1 phase and apoptosis in the same cells. FLT3-IN-3 (10 mg/kg) reduces intratumor FLT3-ITD autophosphorylation in a MV4-11 mouse xenograft model.Formal Name: N2-(trans-4-aminocyclohexyl)-9-cyclopentyl-N6-[4-(4-morpholinylmethyl)phenyl]-9H-purine-2,6-diamine. CAS Number: 2229050-90-0. Synonyms: SAN50900. Molecular Formula: C27H38N8O. Formula Weight: 490.6. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMF: 10 mg/ml, DMSO: 10 mg/ml, Ethanol: 15 mg/ml, PBS (pH 7.2): insol. lambdamax: 262, 312 nm. SMILES: N[C@H](CC1)CC[C@@H]1NC2=NC(NC3=CC=C(C=C3)CN4CCOCC4)=C5C(N(C6CCCC6)C=N5)=N2. InChi Code: InChI=1S/C27H38N8O/c28-20-7-11-22(12-8-20)31-27-32-25(24-26(33-27)35(18-29-24)23-3-1-2-4-23)30-21-9-5-19(6-10-21)17-34-13-15-36-16-14-34/h5-6,9-10,18,20,22-23H,1-4,7-8,11-17,28H2,(H2,30,31,32,33)/t20-,22-. InChi Key: SAEGVASGMTZGFI-AQYVVDRMSA-N.