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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.
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1. Hypertension and rarefaction during treatment with telatinib, a small molecule angiogenesis inhibitor. Clin. Cancer Res. 14(11), 3470-3476 (2008).
2. Telatinib reverses chemotherapeutic multidrug resistance mediated by ABCG2 efflux transporter in vitro and in vivo. Biochem. Pharmacol. 89(1), 52-61 (2014).