目錄:MedChemExpress LLC>>信號通路>> Lucitanib | 德立替尼 | MedChemExpress (MCE)
| CAS | 1058137-23-7 | 純度 | 98.94% |
|---|---|---|---|
| 分子量 | 443.49 | 分子式 | C??H??N?O? |
| 供貨周期 | 現(xiàn)貨 | 規(guī)格 | 10 mM * 1 mL |
| 貨號 | HY-15391 | 應(yīng)用領(lǐng)域 | 醫(yī)療衛(wèi)生,化工,生物產(chǎn)業(yè),制藥/生物制藥 |
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CAS No. : 1058137-23-7
MCE 國際站：Lucitanib
產(chǎn)品活性：Lucitanib (E-3810) 是 VEGFR 和 FGFR 的雙重抑制劑，有效和選擇性地抑制VEGFR1，VEGFR2，VEGFR3，FGFR1，FGFR2，IC50分別為7 nM，25 nM，10 nM，17.5 nM，82.5 nM。
研究領(lǐng)域：Protein Tyrosine Kinase/RTK
作用靶點：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 (Ki<0.05 μM), follows by PDGFRα activity (Ki=0.11 μM). The Ki 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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