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AdipoGen Orantinib
SDP

Supplier:  AdipoGen CDXO0202M100

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Chemical. CAS 252916-29-3. Formula C18H18N2O3. MW 310.35. Orantinib is an orally bioavailable receptor tyrosine kinase inhibitor. Orantinib binds to and inhibits the autophosphorylation of vascular endothelial growth factor receptor 2 VEGFR2, platelet-derived growth factor receptor PDGFR, and fibroblast growth factor receptor FGFR, thereby inhibiting angiogenesis and cell proliferation. It is a potent ATP-competitive inhibitor of PDGFRbeta, VEGFR2, and FGFR1 IC50 = 0.06, 2.4, and 3.0 µM, respectively but not EGFR IC50 >100 µM. Orantinib suppresses tumor growth, blocks angiogenesis in tumors and induces apoptosis of tumor vasculature and regression of established tumors. Orantinib inhibits the phosphorylation of the stem cell factor receptor tyrosine kinase c-kit, often expressed in acute myelogenous leukemia cells, inhibits Aurora kinases B and C IC50=35 and 210nM, respectively, and inhibits Unc-51-like serine/threonine kinase Ulk3, involved in hedgehog signaling.

Catalog No. 50-256-0291


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