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N-Desethyl Sunitinib (SU-12662) (hydrochloride) is a metabolite of sunitinib. Sunitinib is a potent, ATP-competitive VEGFR , PDGFRβ and KIT inhibitor with K i values of 2, 9, 17, 8 and 4 nM for VEGFR -1, -2, -3, PDGFRβ and KIT, respectively.
Appearance:Solid
In Vitro:Sunitinib also potently inhibits Kit and FLT-3. Sunitinib is a potent ATP-competitive inhibitor of VEGFR2 (Flk1) and PDGFRβ with K i of 9 nM and 8 nM, respectively, displaying >10-fold higher selectivity for VEGFR2 and PDGFR than FGFR-1, EGFR, Cdk2,
In Vivo:Sunitinib (20-80mg/kg/day) exhibits broad and potent dose-dependent anti-tumor activity against a variety of tumor xenograft models including HT-29, A431, Colo205, H-460, SF763T, C6, A375, or MDA-MB-435, consistent with the substantial and selective inhi
Biological Activity:N-Desethyl Sunitinib (SU-12662) (hydrochloride) is a metabolite of sunitinib. Sunitinib is a potent, ATP-competitive VEGFR , PDGFRβ and KIT inhibitor with K i values of 2, 9, 17, 8 and 4 nM for VEGFR -1, -2, -3, PDGFRβ and KIT, respectively.