Flumatinib mesylate 是一种具有口服活性的选择性Bcr-Abl抑制剂，能够作用于 c-Abl (IC50:1.2 nM)，PDGFRβ (IC50:307.6 nM) 和 c-Kit (IC50:665.5 nM)。

Flumatinib mesylate is a selective inhibitor of c-Abl, PDGFRβ and c-Kit, effectively overcomes drug resistance of certain KIT mutants.

In vivo study consistently suggested that flumatinib had superior efficacy compared with imatinib or sunitinib against 32D cells with the secondary mutation Y823D.?Molecular modeling of flumatinib docked to the KIT kinase domain suggested a special mechanism underlying the capability of flumatinib to overcome the drug-resistance conferred by activation loop mutations.?These findings suggest that flumatinib could be a promising therapeutic agent against GISTs resistant to both imatinib and sunitinib because of secondary mutations in the activation loop[1].

895519-91-2

C30H33F3N8O4S

658.7

HHGV678 mesylate;甲磺酸氟马替尼;甲磺酸氟马替尼/氟马替尼

DMSO:50 mg/mL (75.91 mM)
H2O:50 mg/mL (75.91 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years