332013-26-0

Telatinib mesylate (Bay 57-9352 mesylate) is a potent and orally active VEGFR2, VEGFR3, PDGFα, and c-Kit inhibitor with IC50s of 6 nM, 4 nM, 15 nM and 1 nM, respectively[1].

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

[1] Steeghs N, et al.Hypertension and rarefaction during treatment with telatinib, a small molecule angiogenesis inhibitor.Clin Cancer Res. 2008 Jun 1;14(11):3470-6. DOI:10.1158/1078-0432.CCR-07-5050
[2] [2] Sodani K, et al. Telatinib reverses chemotherapeutic multidrug resistance mediated by ABCG2 efflux transporter in vitro and in vivo. Biochem Pharmacol. 2014 May 1;89(1):52-61. DOI:10.1016/j.bcp.2014.02.012