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卡博替尼(Cabozantinib、XL184、Cometriq)由美国Exelixis生物制药公司研发,是一个多靶点的广谱抗癌药,能抑制的靶点包括:MET扩增、VEGFR1/2/3、ROS1、RET、AXL、NTRK、KIT等至少9个靶点。 目前,卡博替尼已经在肾癌、甲状腺癌、肝癌、...
XL880抑制MKN-45细胞中MET和下游信号分子的磷酸化,而在KATO-III细胞中靶向作用于GFGR2。 体内研究 XL880(100mg/kg,单一剂量,口服强喂)很大程度上抑制B16F10肿瘤Met的磷酸化和配体(比如,HGF或VEGF)诱导的*中Met和肺中Flk-1/KDR受体磷酸化,两者都能持续24小时。XL880(30-100mg/kg,每天一次,口服强喂)处理...
体内研究XL880(100mg/kg,单一剂量,口服强喂)很大程度上抑制B16F10肿瘤Met的磷酸化和配体(比如,HGF或VEGF)诱导的肝脏中Met和肺中Flk-1/KDR受体磷酸化,两者都能持续24小时。XL880(30-100mg/kg,每天一次,口服强喂)处理导致肿瘤负荷减少。30和100mg/kg XL880处理后,肺表面肿瘤负荷分别减少50%和58%。XL880处理...
Cabozantinib will be taken by mouth (orally), as a tablet, once a day. Cabozantinib will be provided to participants who tolerate it for as long as their disease does not progress. Participants in the study receiving best supportive care alone may switch to treatment with cabozantinib and best...
Protease inhibitor cocktail tablet was pur- chased from Roche Applied Science (Mannheim, Germany). Phosphatase inhibitors and other reagents not specified were from Sigma Chemical Co. (St. Louis, MO). Cell culture The human gastric adenocarcinoma cell lines were purchased from Korean Cell Line Bank...
体内：Cabozantinib (100 mg/kg, Orally, once) inhibits MET and VEGFR2 phosphorylation in mice[1].Cabozantinib (100 mg/kg, Orally, once) 显着增加肿瘤缺氧和细胞凋亡[1].卡博替尼（0-60 mg/kg，口服，每日一次，持续 14 天）以剂量依赖性方式抑制肿瘤生长[1]。参考文献：[1]. You WK, et al. ...
The role of aberrant hepatocyte growth factor receptor (c-MET, also known as tyrosine-protein kinase MET)/hepatocyte growth factor (HGF) signaling in cancer progression and invasion has been extensively studied. c-MET inhibitors have shown promising pre-clinical and early phase clinical trial anti-...
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