Flumatinib

Flumatinib is an inhibitor of the non-receptor tyrosine kinase Bcr-Abl (IC50 = 1.2 nM). It is selective for Bcr-Abl over VEGFR2, c-Src, EGFR, and HER2 at 1 µM but does inhibit PDGFRbeta and c-Kit (IC50s = 307.6 and 665.5 nM, respectively). Flumatinib inhibits the proliferation of K562 chronic myelogenous leukemia (CML) cells expressing wild-type Bcr-Abl (IC50 = 5.1 nM) and 32D cells expressing the Bcr-Abl mutations Bcr-AblQ252H, Bcr-AblY253F, Bcr-AblE255K, Bcr-AblM351T, and Bcr-AblH396P (IC50s = 76.3, 40.4, 123.2, 20.2, and 34.6 nM, respectively), which confer resistance to the c-Abl, Bcr-Abl, PDGFR, and c-Kit inhibitor imatinib (Cay-13139). It also induces tumor regression and increases survival time in a K562 mouse xenograft model when administered at a dose of 75 mg/kg per day. Flumatinib also increases the viability of Vero E6 cells infected with severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2, EC50 = 1.6 µM) and reduces the levels of SARS-CoV-2 in the supernatant of Vero E6 infected cells.Formal Name: 4-[(4-methyl-1-piperazinyl)methyl]-N-[6-methyl-5-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]-3-pyridinyl]-3-(trifluoromethyl)-benzamide. CAS Number: 895519-90-1. Synonyms: HH-GV-678. Molecular Formula: C29H29F3N8O. Formula Weight: 562.6. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMF: Slightly soluble, DMSO: 2 mg/ml, Ethanol: Slightly soluble, PBS (pH 7.2): 0.25 mg/ml. lambdamax: 239, 273 nm. SMILES: O=C(C1=CC(C(F)(F)F)=C(CN2CCN(CC2)C)C=C1)NC3=CN=C(C)C(NC4=NC=CC(C5=CN=CC=C5)=N4)=C3. InChi Code: InChI=1S/C29H29F3N8O/c1-19-26(38-28-34-9-7-25(37-28)21-4-3-8-33-16-21)15-23(17-35-19)36-27(41)20-5-6-22(24(14-20)29(30,31)32)18-40-12-10-39(2)11-13-40/h3-9,14-17H,10-13,18H2,1-2H3,(H,36,41)(H,34,37,38). InChi Key: BJCJYEYYYGBROF-UHFFFAOYSA-N.