Cabozantinib L-Malate Salt-Cabozantinib L-Malate Salt代理/参数/厂家-生化试剂-艾美捷科技有限公司

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中文名称: Cabozantinib L-Malate Salt

英文名字: Cabozantinib L-Malate Salt

供应商: USBiological

产品货号: 005487

产品报价: ￥询价/25mg

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背景资料: USBiological品牌是全球有名的抗原抗体和生化试剂供应商，生产世界上种类最多的抗体，用于Western Blot、免疫沉淀、免疫荧光、免疫组化和流式细胞术等多种检测方法。武汉艾美捷科技作为USBiological品牌中国区域总代理，是行业中少有的致力于服务客户，帮助客户，且拥有独立的专业销售团队、技术支持团队、市场营销团队、进出口报关团队的高科技生物企业。可以为您提供及时的咨询响应，专业的产品和解决方案支持，稳健快捷的交货周期，优质放心的售后服务。我们致力于为您提供有价值的产品和服务，在意您的成功！

产品描述: Cabozantinib is a small molecule C-Met modulator. Cabozantinib acts as a potent multitargeted VEGFR2, Met, FLT3, Tie2, Kit and Ret inhibitor with IC50 of 0.035, 1.8, 14.4, 14.3 and 4.6 nM for VEGFR2, Met, FLT3, Tie2 and Kit, respectively. Cabozantinib shows dose-dependent inhibition of tumor growth and tumor regression, associated with disruption of the tumor vasculature and extensive tumor cell apoptosis.Cabozantinib, also known as XL184, is an orally bioavailable novel tysosine kinase inhibitor of c-MET and VEGF receptor 2 (VEGFR2). It inhibited MET and VEGFR2 with IC50 values of 1.3 nM and 35 pM, respectively. It also inhibited MET-activating kinase domain mutations Y1248H, D1246N, or K1262R with IC50 values of 3.8, 11.8, and 14.6 nM, respectively. It strongly inhibited several kinases that are implicated in tumor pathobiology including KIT, RET, AXL, TIE2, and FLT3 with IC50 values of 4.6, 5.2, 7, 14.3, and 11.3 nM, respectively. In cellular assays, cabozantinib inhibited phosphorylation of MET, VEGFR2, KIT, FLT3, and AXL with IC50 values of 7.8, 1.9, 5.0, 7.5, and 42 [micro]M, respectively. Cabozantinib inhibited tumor angiogenesis, tumor growth and metastasis in cancers with dysregulated MET and VEGFR signaling. Yakes F.M., et al "Cabozantinib (XL184), a novel MET and VEGFR2 inhibitor, simultaneously suppresses metastasis, angiogenesis, and tumor growth." Mol. Cancer Ther. 10: 2298-2308 (2011).Treatment of RIP-Tag2 mice with cabozantinib eliminated approximately 80% of the vasculature of spontaneous pancreatic islet tumors over 7 days, reduced pericytes and empty basement membrane sleeves, resulted in widespread intratumoral hypoxia and tumor cell apoptosis, and delayed regrowth of the tumor vasculature after drug withdrawal. Importantly, it also inhibited invasiveness of primary tumors and reduced metastasis. You W.K., et al. "VEGF and c-Met blockade amplify angiogenesis inhibition in pancreatic islet cancer." Cancer Res. 71: 4758-4768 (2011).Cabozantinib is active in patients with medullary thyroid cancer and has an acceptable safety profile. Kurzrock R., et al. "Activity of XL184 (Cabozantinib), an oral tyrosine kinase inhibitor, in patients with medullary thyroid cancer." J. Clin. Oncol. 29: 2660-2666 (2011).Cabozantinib 40 mg daily was associated with a high rate of bone scan response and better tolerability in patients with metastatic castration-resistant prostate cancer when compared with previously reported results for cabozantinib 100 mg daily. Lee R.J., et al. "A dose-ranging study of cabozantinib in men with castration-resistant prostate cancer and bone metastases." Clin Cancer Res. 19: 3088-3094 (2013).Cabozantinib demonstrated activity in patients with metastatic melanoma in a phase 2 randomized discontinuation trial. Gordon M.S. etal. "Activity of Cabozantinib (XL184) in Metastatic Melanoma: Results From a Phase 2 Randomized Discontinuation Trial (RDT)." http://www.exelixis.com/sites/default/files/2012-06-02_Gordon%20Melanoma_ASCO%202012%20FINAL_poster_8531.pdfCabozantinib was active in patients with metastatic non-small cell lung cancer (NSCLC) in a phase 2 randomized discontinuation trial. Hellerstedt B.A. et al. "Activity of Cabozantinib (XL184) in Metastatic NSCLC: Results From a Phase 2 Randomized Discontinuation Trial (RDT)." http://www.exelixis.com/sites/default/files/2012-06-05_Hellerstedt%20NSCLC_ASCO%202012_FINAL_poster_7514.pdf response to anthracycline therapy." Cell Cycle 11: 2747-2755 (2012).Appearance:White to off-white, cystalline powderPurity:≥99% (HPLC, TLC)Melting Point:As reportedSolubility:DMSOMethod for Determining Identity: NMR (DMSO-d6) and MSStorage and Stability:May be stored at RT for short-term only. Long-term storage is recommended at -20°C. For maximum recovery of product, centrifuge the original vial prior to removing the cap.

产品形式: 该产品为类白色固体。

保存建议: 接收到Cabozantinib L-Malate Salt产品后，置于4°C温度下保存。

其他: Usbiological公司是美国著名的抗体和生化试剂供应商，生产世界上种类最多的抗体，用于Western Blot、免疫沉淀、免疫荧光、免疫组化和流式细胞术等多种检测方法。Usbiological公司现已拥有超过50,19234种抗体、抗原和生化产品，为科研用户提供了诸多超值选择。