S80994 |
Cabozantinib (XL184, BMS-907351) |
源叶(MedMol) | 98% |
- 产品描述: Cabozantinib is a potent and orally active inhibitor of VEGFR2 and MET, with IC50 values of 0.035, and 1.3 nM, respectively. Cabozantinib displays strong inhibition of KIT, RET, AXL, TIE2, and FLT3 (IC50=4.6, 5.2, 7, 14.3, and 11.3 nM, respectively). Cabozantinib shows antiangiogenic activity. Cabozantinib disrupts tumor vasculature and promotes tumor and endothelial cell apoptosis
- 靶点: VEGFR2:0.035 nM (IC50);Flt-4:6 nM (IC50);Flt-1:12 nM (IC50);VEGFR;FLT;c-Met/HGFR;TAMReceptor;c-Kit;ROR
- 体内研究:
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.
- 参考文献:
1. 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. 2. You WK, et al. VEGF and c-Met blockade amplify angiogenesis inhibition in pancreatic islet cancer. Cancer Res, 2011, 71(14), 4758-4768. 3. Fuse MA, et al. Combination Therapy With c-Met and Src Inhibitors Induces Caspase-Dependent Apoptosis of Merlin-Deficient Schwann Cells and Suppresses Growth of Schwannoma Cells. Mol Cancer Ther. Mol Cancer Ther. 2017 Nov;16(11):2387-2398.
- 溶解性: DMSO : 25 mg/mL (49.85 mM; Need ultrasonic) H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)
- 保存条件: -20℃
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 1.994 ml 9.97 ml 19.939 ml 5 mM 0.399 ml 1.994 ml 3.988 ml 10 mM 0.199 ml 0.997 ml 1.994 ml 50 mM 0.04 ml 0.199 ml 0.399 ml
- 注意:部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)