Motesanib has broad activity against the human VEGFR family, and displays > 1000 selectivity against EGFR, Src, and p38 kinase. Motesanib significantly inhibits VEGF-induced cellular proliferation of HUVECs with an IC50 of 10 nM, while displaying little effect at bFGF-induced proliferation with an IC50 of >3,000 nM. Motesanib also potently inhibits PDGF-induced proliferation and SCF-induced c-kit phosphorylation with IC50 of 207 nM and 37 nM, respectively, but not effective against the EGF-induced EGFR phosphorylation and cell viability of A431 cells. Althouth displaying little antiproliferative activity on cell growth of HUVECs alone, Motesanib treatment significantly sensitizes the cells to fractionated radiation.
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Pexidartinib hcl; Pexidartinib; Telatinib; Avapritinib; Amuvatinib; Dovitinib Lactate; Linifanib; OSI-930; Crenolanib; Motesanib Diphosphate; Sunitinib; Imatinib mesylate; Axitinib; Masitinib; Dovitinib; ISCK03