Flumatinib

• CAT Number: I005358
• CAS Number: 895519-90-1
• Molecular Formula: C29H29F3N8O
• Molecular Weight: 562.59
• Purity: ≥95%
• Target: c-Abl; c-Kit; PDGRFβ
• Solubility: DMSO: ≥ 32 mg/mL
• Storage: Store at -20°C
• IC50: 1.2 nM (c-Abl); 307.6 nM(PDGFRβ); 2662 nM (c-Kit) [1]
• IUPAC Name: 4-[(4-methylpiperazin-1-yl)methyl]-N-[6-methyl-5-[(4-pyridin-3-ylpyrimidin-2-yl)amino]pyridin-3-yl]-3-(trifluoromethyl)benzamide
• InChI: 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)
• InChIKey: BJCJYEYYYGBROF-UHFFFAOYSA-N
• SMILES: CC1=C(C=C(C=N1)NC(=O)C2=CC(=C(C=C2)CN3CCN(CC3)C)C(F)(F)F)NC4=NC=CC(=N4)C5=CN=CC=C5

Flumatinib (Cat.No:I005358) is a tyrosine kinase inhibitor primarily used for the treatment of chronic myeloid leukemia (CML). It specifically targets BCR-ABL1, a fusion protein responsible for the pathogenesis of CML. Flumatinib inhibits the activity of BCR-ABL1, leading to reduced proliferation of cancer cells and improved clinical outcomes.

Reference

[1]. Luo H, et al. HH-GV-678, a novel selective inhibitor of Bcr-Abl, outperforms imatinib and effectively overrides imatinib resistance. Leukemia. 2010 Oct;24(10):1807-9.

[2]. Zhao J, et al. Flumatinib, a selective inhibitor of BCR-ABL/PDGFR/KIT, effectively overcomes drug resistance of certain KIT mutants. Cancer Sci. 2013 Nov 10.

[3]. Gong A, et al. Metabolism of flumatinib, a novel antineoplastic tyrosine kinase inhibitor, in chronic myelogenous leukemia patients. Drug Metab Dispos. 2010 Aug;38(8):1328-40.