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Cabozantinib

CAS No. : 849217-68-1

MCE 国际站：Cabozantinib

产品活性：Cabozantinib 是一种口服有效的 VEGFR2 和 MET 抑制剂，IC₅₀ 分别为 0.035 和 1.3 nM。Cabozantinib 对 KIT、RET、AXL、TIE2 和 FLT3 有较强的抑制作用 (IC₅₀=4.6、5.2、7、14.3 和 11.3 nM)。Cabozantinib 显示出抗血管生成活性。Cabozantinib 可以破坏肿瘤血管，促进肿瘤和内皮细胞凋亡 (apoptosis)。

研究领域：Protein Tyrosine Kinase/RTK  |  Apoptosis

作用靶点：VEGFR  |  c-Met/HGFR  |  c-Kit  |  TAM Receptor  |  FLT3  |  Apoptosis

In Vitro: Cabozantinib inhibits phosphorylation of MET and VEGFR2, as well as KIT, FLT3, and AXL with IC₅₀ values of 7.8, 1.9, 5.0, 7.5, and 42 μM, respectively.
Cabozantinib (4.6 nM) inhibits tubule formation with no evidence of cytotoxicity, with IC₅₀ values of 6.7, 5.1, 4.1, 7.7, and 4.7 nM in HMVEC, MDA-MB-231, A431, HT1080, and B16F10 cells, respectively.
Cabozantinib (0-370 nM, 24 h) inhibits cellular migration and invasion.
Cabozantinib (48 h) inhibits tumor cell proliferation in a variety of tumor types.

In Vivo: Cabozantinib (100 mg/kg, Orally, once) inhibits MET and VEGFR2 phosphorylation in mice.
Cabozantinib (100 mg/kg, Orally, once) significantly increases tumor hypoxia and apoptosis.
Cabozantinib (0-60 mg/kg, Orally, once daily for 14 days) inhibits tumor growth in a dose-dependent manner.

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