tafetinib

Tafetinib (SIM010603) is an oral multi-targets receptor tyrosine kinases inhibitor. Tafetinib inhibitsstem cell factor receptor (Kit),vascular endothelial growth factor receptor-2 (VEGFR-2),platelet-derived growth factor receptor-β (PDGFR-β),glial cell line-derived neurotrophic factor receptor (Rearranged during Transfection; RET), andFms-like tyrosine kinase-3 (FLT3)withIC50values between 5.0 and 68.1 nmol/l. Tafetinib inhibits the phosphorylation ofPDGFR-βandVEGFR-2. Tafetinib inhibits endothelial cell proliferation, endothelial cells chemotaxis, and corneal angiogenesis[1].

Research Areas >> Cancer

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> VEGFR

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> c-Kit

[1]. Wang D, et al. Preclinical anti-angiogenesis and anti-tumor activity of SIM010603, an oral, multi-targets receptor tyrosine kinases inhibitor. Cancer Chemother Pharmacol. 2012;69(1):173-183.