Ki11502

Ki11502 is a multi-targeted receptor tyrosine kinase (RTK) inhibitor that selectively inhibits the activity of PDGF β/α receptors with IC₅₀ values less than 10 nM. Ki11502 selectively inhibits PDGF β receptor phosphorylation, proliferation, and proteoglycan synthesis in human vascular smooth muscle cells. Ki11502 can induce Apoptosis) and exhibits profound antiproliferative effects on select subsets of leukemia, including those with Imatinib (HY-15463) resistant mutations. Ki11502 is highly suitable for studying the role of PDGF in vascular diseases, particularly the role of proteoglycans in atherosclerosis^[1][2]. In Vitro:Ki11502 (0.1-1 nM; 2 days) significantly induces growth arrest, G0/G1 cell cycle arrest, and apoptosis in eosinophilic leukemia EOL-1 cells carrying the activated FIP1-like 1/PDGFRα fusion gene^[2].
Ki11502 (0.1-1 nM; 3 h) effectively reduces the levels of p-PDGFRα and its downstream signals (including p-Akt, p-ERK, and p-STAT5) in EOL-1 cells^[2]. In Vivo:Ki11502 (50 mg/kg; gavage; twice daily for 5 consecutive days) completely inhibits the proliferation of EOL-1 tumor xenografts in SCID mice^[2].