GNF-7

GNF-7 is a multi-kinase inhibitor (IC50s = 25, 8, 61, 122, 136, and 133 nM for ACK1, GCK, Bcr-AblT315I, Bcr-AblE255V, Bcr-AblG250E, and c-Abl, respectively). It also inhibits several additional kinases in a panel by greater than 50% when used at a concentration of 10 µM. GNF-7 inhibits the growth of Ba/F3 cells transformed with wild-type Bcr-Abl, Bcr-AblT315I, Bcr-AblE255V, and Bcr-AblG250E (IC50s = 50s = 1 and 5 nM, respectively) in vitro. In vivo, GNF-7 (10 and 20 mg/kg) reduces tumor growth in a Bcr-AblT315I Ba/F3 mouse xenograft model. It also reduces tumor volume in an OCI-AML3 mouse xenograft model when administered at a dose of 8 mg/kg.Formal Name: N-[3-[1,4-dihydro-1-methyl-7-[(6-methyl-3-pyridinyl)amino]-2-oxopyrimido[4,5-d]pyrimidin-3(2H)-yl]-4-methylphenyl]-3-(trifluoromethyl)-benzamide. CAS Number: 839706-07-9. Molecular Formula: C28H24F3N7O2. Formula Weight: 547.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 10 mg/ml, DMF:PBS(pH7.2) (1:2): 0.3 mg/ml, DMSO: 2 mg/ml, Ethanol: 0.1 mg/ml. lambdamax: 277 nm. SMILES: CC1=NC=C(NC2=NC=C(CN(C3=C(C)C=CC(NC(C4=CC(C(F)(F)F)=CC=C4)=O)=C3)C(N5C)=O)C5=N2)C=C1. InChi Code: InChI=1S/C28H24F3N7O2/c1-16-7-9-21(34-25(39)18-5-4-6-20(11-18)28(29,30)31)12-23(16)38-15-19-13-33-26(36-24(19)37(3)27(38)40)35-22-10-8-17(2)32-14-22/h4-14H,15H2,1-3H3,(H,34,39)(H,33,35,36). InChi Key: SZNYUUZOQHNEKB-UHFFFAOYSA-N.