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Lucitanib

CAS No. : 1058137-23-7

MCE 站：Lucitanib

产品活性：Lucitanib (E-3810) 是 VEGFR 和 FGFR 的双重抑制剂，有效和选择性地抑制VEGFR1，VEGFR2，VEGFR3，FGFR1，FGFR2，IC₅₀分别为7 nM，25 nM，10 nM，17.5 nM，82.5 nM。

研究领域：Protein Tyrosine Kinase/RTK

作用靶点：VEGFR  |  FGFR

In Vitro: Consistent with the inhibitory activity of VEGFR and FGFR auto-phosphorylation, Lucitanib potently inhibits VEGF and bFGF-stimulated HUVEC proliferation with IC₅₀ of 40 and 50 nM, respectively. Besides, Lucitanib (E-3810) also inhibits CSF-1R with IC₅₀ of 5 nM. Lucitanib potently inhibits FGFR2 activity (K_i<0.05 μM), follows by PDGFRα activity (K_i=0.11 μM). The K_i values obtained for DDR2, LYN, CARDIAK, CSBP (2), EPHA2, and YES range between 0.26 and 8 μM.

In Vivo: Lucitanib (E-3810), at oral dosing of 20 mg/kg for 7 consecutive days, completely inhibits (P<0.01) the bFGF induced angiogenic response compare with the response in vehicle-treated mice. Lucitanib (E-3810) shows a broad spectrum of activity, being active in all the xenografts tested (HT29 colon carcinoma, A2780 ovarian carcinoma, A498, SN12K1, and RXF393 renal carcinomas) with dose-dependent inhibition of tumor growth. E-3810 significantly delays growth during treatment, but tumors resume their growth when treatment is suspended; in a few cases, tumor regression is observed. The activity of Lucitanib (E-3810) given at the doses of 15 mg/kg is tested on MDA-MB-231 breast cancer transplanted subcutaneously, at a late stage, when tumor masses reach 350 to 400 mg. This tumor xenograft is very sensitive to Lucitanib (E-3810), with complete tumor stabilization lasting throughout the 30-day treatment. As in other tumor models, tumors re-grow after withdrawal of Lucitanib (E-3810) at a rate similar to control tumors.

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