GNF-5

GNF-5 is an allosteric inhibitor of Bcr-Abl (IC50 = 0.121 µM) and a derivative of GNF-2 (Cay-16253). It also inhibits the Bcr-Abl mutants Bcr-AblG250E, Bcr-AblE255V, and Bcr-AblM351T (IC50s = 4.52, 0.38, and 0.93 µM, respectively). GNF-5 inhibits the growth of Ba/F3 cells (IC50 = 0.145 µM). It reduces viral titers in Vero cells infected with infectious bronchitis virus (IBV), a coronavirus, when used at a concentration of 10 µM via inhibition of IBV surface glycoprotein-induced syncytia formation and virus-cell fusion. GNF-5 (75 mg/kg) increases survival in a recalcitrant mutant Bcr-AblT315I mouse bone marrow transplantation model when administered alone or in combination with nilotinib.Formal Name: N-(2-hydroxyethyl)-3-[6-[[4-(trifluoromethoxy)phenyl]amino]-4-pyrimidinyl]-benzamide. CAS Number: 778277-15-9. Molecular Formula: C20H17F3N4O3. Formula Weight: 418.4. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 25 mg/ml, DMF:PBS(pH7.2) (1:2): 0.25 mg/ml, DMSO: 10 mg/ml, Ethanol: 0.25 mg/ml. lambdamax: 268 nm. SMILES: O=C(NCCO)C1=CC=CC(C2=CC(NC3=CC=C(OC(F)(F)F)C=C3)=NC=N2)=C1. InChi Code: InChI=1S/C20H17F3N4O3/c21-20(22,23)30-16-6-4-15(5-7-16)27-18-11-17(25-12-26-18)13-2-1-3-14(10-13)19(29)24-8-9-28/h1-7,10-12,28H,8-9H2,(H,24,29)(H,25,26,27). InChi Key: IIQUYGWWHIHOCF-UHFFFAOYSA-N.