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N-Desethyl Sunitinib hydrochloride

CAS No. :

MCE 站：N-Desethyl Sunitinib hydrochloride

产品活性：N-Desethyl Sunitinib (SU-12662) (hydrochloride) 是 Sunitinib 的代谢物。Sunitinib 是有效的，ATP 竞争的 VEGFR，PDGFRβ 和 KIT 抑制剂，能够抑制 VEGFR -1，VEGFR -2，VEGFR -3，PDGFRβ 和 KIT 的活性，K_i 值分别为 2，9，17，8 和 4 nM。

研究领域：Others

作用靶点：Others

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, Met, IGFR-1, Abl, ａnd src. In serum-starved NIH-3T3 cells expressing VEGFR2 or PDGFRβ, Sunitinib inhibits VEGF-dependent VEGFR2 phosphorylation ａnd PDGF-dependent PDGFRβ phosphorylation with IC₅₀ of 10 nM ａnd 10 nM, respectively. Sunitinib inhibits VEGF-induced proliferation of serum-starved HUVECs with IC₅₀ of 40 nM, ａnd inhibits PDGF-induced proliferation of NIH-3T3 cells overexpressing PDGFRβ or PDGFRα with IC₅₀ of 39 nM ａnd 69 nM, respectively. Sunitinib inhibits phosphorylation of wild-type FLT3, FLT3-ITD, ａnd FLT3-Asp835 with IC₅₀ of 250 nM, 50 nM, ａnd 30 nM, respectively. Sunitinib inhibits the proliferation of MV4;11 ａnd OC1-AML5 cells with IC₅₀ of 8 nM ａnd 14 nM, respectively, ａnd induces apoptosis in a dose-dependent manner.

In Vivo: Sunitinib (20-80 mg/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 inhibition of VEGFR2 or PDGFR phosphorylation ａnd signaling in vivo. Sunitinib (80 mg/kg/day) for 21 days leads to complete tumor regression in six of eight mice, without tumor re-growing during a 110-day observation period after the end of treatment. Second round of treatment with Sunitinib remains efficacious against tumors that are not fully regressed during the first round of treatment. Sunitinib treatment results in significant decrease in tumor MVD, with appr 40% reduction in SF763T glioma tumors. SU11248 treatment results in a complete inhibition of additional tumor growth of luciferase-expressing PC-3M xenografts, despite no reduction in tumor size. Sunitinib treatment (20 mg/kg/day) dramatically suppresses the growth subcutaneous MV4;11 (FLT3-ITD) xenografts ａnd prolongs survival in the FLT3-ITD bone marrow engraftment model.

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