A multi-kinase inhibitor
Telatinib is a multi-kinase inhibitor that inhibits VEGF receptor 2 (VEGFR2), VEGFR3, PDGFRα, and c-Kit (IC50s = 6, 4, 15, and 1 nM, respectively).1 It also binds to the transmembrane region of the ABCG2 efflux transporter and enhances intracellular accumulation of [3H]-mitoxantrone in ABCG2-overexpressing cells.2 Telatinib (15 mg/kg) decreases tumor growth rate and size in an H460/MX20 mouse xenograft model.
1.Steeghs, N., Gelderblom, H., Roodt, J.O., et al.Hypertension and rarefaction during treatment with telatinib, a small molecule angiogenesis inhibitorClin. Cancer Res.14(11)3470-3476(2008) 2.Sodani, K., Patel, A., Anreddy, N., et al.Telatinib reverses chemotherapeutic multidrug resistance mediated by ABCG2 efflux transporter in vitro and in vivoBiochem. Pharmacol.89(1)52-61(2014)
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