Cabozantinib (BMS-907351, BMS907351, XL-184, XL184)是多种受体酪氨酸激酶小分子抑制剂,尤其抑制c-Met和VEGFR2表达水平,其IC50值分别为1.3 nM和0.035 nM。Cabozantinib也作用于Ret、Kit、Flt-1/3/4、Tie2和AXL,其IC50值分别为4 nM、4.6 nM、12 nM/11.3 nM/6 nM、14.3 nM和7 nM。Cabozantinib可用于转移甲状腺髓样癌(MTC)的治疗,降低肿瘤增殖,抑制肿瘤生长。
参考文献
[1]. You WK, et al.VEGF and c-Met blockade amplify angiogenesis inhibition in pancreatic islet cancer. Cancer Res, 2011, 71(14), 4758-4768.
[2]. Torres KE, et al. Activated MET is a molecular prognosticator and potential therapeutic target for malignant peripheral nerve sheath tumors.Clin Cancer Res, 2011, 17(12), 3943-3955.
[3]. Yakes FM, et al.Cabozantinib (XL184), a novel MET and VEGFR2 inhibitor, simultaneously suppresses metastasis, angiogenesis, and tumor growth. Mol Cancer Ther, 2011, 10(12), 2298-2308.
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