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Telatinib (BAY 57-9352) is a selective inhibitor of VEGFR2, VEGFR3, c-Kit and PDGFRα with IC50 value of 6 nM, 4 nM, 1 nM and 15 nM, respectively [1].

Vascular endothelial growth factor receptor (VEGFR) is the receptor of VEGF and plays an important role in stimulating vasculogenesis and angiogenesis. Platelet-derived growth factor (PDGF) is a member of growth factors and involves in blood vessel formation. C-Kit is the receptor of a growth factor. Many studies have shown that abnormal of VEGFR, c-Kit and PDGFR are correlated with a variety of tumors [1, 2, 3].

Telatinib is a potent VEGFR2/3, c-Kit and PDGFRα inhibitor. When tested with a panel of tumor cell lines (MDA-MB-231 breast caicinoma, Colo-205 colon carcinoma, DLD-1 colon carcinoma and H460 non-small cell lung carcinoma), Telatinib treatment exhibited inhibition on VEGFR-2 autophosphorylation and PDGF-βwhich involved in the angiogenic process [2].

Telatinib has been used in clinical trails to a variety of cancers treatment and has achieved promising results [2-4].

It is also reported that Telatinib restores tumor cells sensitivity to anticancer drugs and significantly reduced cellular viability by inhibiting ABCG2 expression [3].

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