Flumatinib mesylate (HHGV678) is an orally active and selective inhibitor of Bcr-Abl, PDGFRβ, and c-Kit. It inhibits c-Abl, PDGFRβ, and c-Kit with IC50 values of 1.2 nM, 307.6 nM, and 665.5 nM, respectively. This compound also inhibits Bcr-Abl autophosphorylation and Stat5 and Erk1/2 phosphorylation. Flumatinib mesylate has been shown to inhibit tumor growth in chronic myelogenous leukemia models.
- Orally active and selective Bcr-Abl inhibitor.
- Inhibits c-Abl (IC50: 1.2 nM), PDGFRβ (IC50: 307.6 nM), and c-Kit (IC50: 665.5 nM).
- Suppresses Bcr-Abl autophosphorylation, Stat5, and Erk1/2 phosphorylation in K562 leukemia cells.
- Demonstrates tumor growth inhibition in chronic myelogenous leukemia models.