VEGFR2-IN-84 is an orally active, multi-targeted tyrosine kinase inhibitor based on a naphthalene ring scaffold. VEGFR2-IN-84 inhibits VEGFR2 with sub-nanomolar affinity and broadly targets kinases including Kit , FGFR , PDGFR , and Ret . By competitively binding to the ATP -binding pocket, VEGFR2-IN-84 blocks the phosphorylation of VEGFR2 and its downstream AKT/ERK signaling pathway, thereby significantly inhibiting endothelial cell proliferation, migration, and tumor angiogenesis. VEGFR2-IN-84 exhibits broad-spectrum antiproliferative activity against various solid tumors such as liver cancer , lung cancer , and renal cancer , shows weak toxicity to normal cells, and has superior potency to Lenvatinib ( HY-10981 ). VEGFR2-IN-84 possesses favorable pharmacokinetic properties and high safety ( LD 50 >2000 mg/kg), and can be used in related studies of various malignant tumors.
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