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Lenvatinib

CAS No. : 417716-92-8

MCE 国际站：Lenvatinib

产品活性：Lenvatinib (E7080)一种具有口服活性的，多靶点酪氨酸激酶抑制剂，抑制血管内皮生长因子受体(VEGFR1-3)，成纤维细胞生长因子受体(FGFR1-4)，血小板衍生生长因子受体(PDGFR)，干细胞因子受体 (KIT)，转染期间重排(RET)，显示有效抗癌的活性。

研究领域：Protein Tyrosine Kinase/RTK

作用靶点：VEGFR  |  FGFR  |  PDGFR  |  c-Kit  |  RET

In Vitro: Lenvatinib (E7080)has IC50s of 4, 5.2, 22 nM for VEGFR2 (KDR),VEGFR3 (Flt-4), and VEGFR1 (Flt-1), respectively. Lenvatinibinhibits PDGFRα, PDGFRβ, FGFR1, and KIT with IC50s of 51, 39, 46, and 100 nM, respectively.

In Vivo: Lenvatinib (E7080)(100 mg/kg, p.o.) significantly inhibits local tumor growth at them.f.p., and at the end of treatment, Lenvatinib mesylate alsosignificantly inhibits metastasis to both regional lymph nodes anddistant lung.
Lenvatinib (E7080) inhibits the growth of H146 tumor at 30 and 100mg/kg (BID, QDx21) in a dose-dependent manner and causes tumorregression at 100 mg/kg in H146 xenograft model. IHC analysis withanti-CD31 antibody shows that lenvatinib at 100 mg/kg decreasesmicrovessel density more than anti-VEGF antibody and STI571treatment.

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