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苹果酸盐原料药小分子抑制剂 研究用药效强 现货供应
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产品/服务: 浏览次数:118苹果酸盐原料药 
型 号: 942275-12-9 
规 格: 医药级 
品 牌: yanyebio 
单 价: 1.00元/公斤 
起订量: 1 公斤 
供货总量: 1135 公斤
发货期限: 自买家付款之日起 3 天内发货
更新日期: 2017-04-07  有效期至:长期有效
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 产品型号:  942275-12-9
 产品规格:  医药级
 产品品牌:  yanyebio
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苹果酸盐原料药 小分子抑制剂 研究用药效强 现货供应顺丰发货仅供科研
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苹果酸盐原料药 小分子抑制剂 研究用药效强 现货供应顺丰发货仅供科研
产品名称:苹果酸盐
产品别名:Cabozantinib malate (XL184)
CAS.NO:1140909-48-3
分子式:C28H24FN3O5.C4H6O5
分子量:635.59
纯度级别:实验试剂LR
产品性状:固态粉末
稳定性:3年 -20℃粉状 6个月-80℃溶于溶剂
有效成分含量:99%
用途:科研
产品描述:Cabozantinib malate (XL184)是Cabozantinib的苹果酸盐,是有效的VEGFR2抑制剂,IC50为0.035 nM,也抑制c-Met, Ret, Kit, Flt-1/3/4, Tie2和AXL,无细胞试验中IC50分别为1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM和7 nM。
靶点:VEGFR2/KDR [1] c-Met [1] Kit [1] VEGFR3/FLT4 [1] Axl [1]
体外研究:Cabozantinib has weak inhibitory activity against RON and PDGFRβ with IC50 of 124 nM and 234 nM, respectivey, and has low activity against FGFR1 with IC50 of 5.294 μM. [1] Cabozantinib at low concentration (0.1-0.5 μM) is sufficient to induce marked inhibition of constitutive and inducible Met phosphorylation and its resultant downstream signaling in MPNST cells, and inhibit HGF-induced MPNST cell migration and invasion. Cabozantinib also induces marked inhibition of Met and VEGFR2 phosphorylation in cytokine-stimulated human umbilical vein endothelial cells (HUVECs). Although Cabozantinib has no significant effect on MPNST cell growth at 0.1 μM, Cabozantinib at 5-10 μM significantly inhibits the MPNST cell growth. [2]
体内研究:Cabozantinib treatment at 30 mg/kg in RIP-Tag2 mice with spontaneous pancreatic islet tumors disrupts 83% of the tumor vasculature, reduces pericytes and empty basement membrane sleeves, causes widespread intratumoral hypoxia and extensive tumor cell apoptosis, and slows regrowth of the tumor vasculature after drug withdrawal, more significantly compared with XL999 that blocks VEGFR but not c-Met, leading to only 43% reduction in vascularity, suggesting that concurrent inhibition of VEGFR and other functionally relevant receptor tyrosine kinases (RTK) amplifies angiogenesis inhibition. Cabozantinib also decreases invasiveness of primary tumors and reduces metastasis. [1] Cabozantinib at 30 mg/kg/day significantly abrogates human MPNST xenografts growth and metastasis in SCID mice. [2] Administration of Cabozantinib induces dose-dependent inhibition of tumor growth in breast, lung, and glioma tumor models, in association with decreased tumor and endothelial cell proliferation as well as increased apoptosis. A single oral dose of Cabozantinib is sufficient to induce sustained tumor growth inhibition in MDA-MB-231 tumor-bearing mice and C6 tumor-bearing rats at 100 mg/kg and 10 mg/kg, respectively. [3]









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