332012-40-5

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). It also binds to the transmembrane region of the ABCG2 efflux transporter and enhances intracellular accumulation of [³H]-mitoxantrone in ABCG2-overexpressing cells. Telatinib (15 mg/kg) decreases tumor growth rate and size in an H460/MX20 mouse xenograft model.

Telatinib (BAY 57-9352) is an orally available, potent multitargeted VEGFR-2, VEGFR-3, PDGFR-β and c-Kit tyrosine kinases inhibitor with an IC50 of 19 nM for the inhibition of VEGFR-2 autophosphorylation.

Telatinib small-molecule inhibitor of vascular endothelial growth factor receptors 2 and 3 (VEGFR-2/-3) and platelet-derived growth factor receptor β tyrosine kinases. Telatinib is used therapeuticall y in patients with advanced solid tumors.

c-Kit

VEGFR2: 6 nM (IC₅₀); VEGFR3: 4 nM (IC₅₀); PDGFRα: 15 nM (IC₅₀); c-Kit: 1 nM (IC₅₀)

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