卡博替尼|T2586

Cabozantinib
849217-68-1

￥276 1mg 起订

￥393 2mg 起订

￥635 5mg 起订

上海更新日期：2024-12-02

TargetMol中国（陶术生物）

VIP12年

联系人：邵小姐

电话：021-021-33632979拨打

手机：15002134094 拨打

邮箱：marketing@targetmol.com

产品详情:

中文名称：: 卡博替尼

英文名称：: Cabozantinib

CAS号：: 849217-68-1

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 99.88%

产品类别：: 抑制剂

货号：: T2586

Product Introduction

Bioactivity

名称	Cabozantinib
描述	Cabozantinib (XL184) is a multi-targeted tyrosine kinase receptor inhibitor that inhibits VEGFR2, c-Met, Kit, Axl, and Flt3 (IC50=0.035/1.3/4.6/7/11.3 nM). Cabozantinib exhibits both antitumor and antiangiogenic activity.
细胞实验	Receptor phosphorylation of MET, VEGFR2, AXL, FLT3, and KIT were, respectively, assessed in PC3, HUVEC, MDA-MB-231, FLT3-transfected BaF3, and KIT-transfected MDA-MB-231 cells. Cells were serum starved for 3 to 24 hours, then incubated for 1 to 3 hours in serum-free medium with serially diluted cabozantinib before 10-minute stimulation with ligand: HGF (100 ng/mL), VEGF (20 ng/mL), SCF (100 ng/mL), or ANG1 (300 ng/mL). Receptor phosphorylation was determined either by ELISA using specific capture antibodies and quantitation of total phosphotyrosine or immunoprecipitation and Western blotting with specific antibodies and quantitation of total phosphotyrosine. Total protein served as loading controls [1].
激酶实验	The inhibition profile of cabozantinib against a broad panel of 270 human kinases was determined using luciferase-coupled chemiluminescence, 33P-phosphoryl transfer, or AlphaScreen technology. Recombinant human full-length, glutathione S-transferase tag or histidine tag fusion proteins were used, and half maximal inhibitory concentration (IC50) values were determined by measuring phosphorylation of peptide substrate poly(Glu, Tyr) at ATP concentrations at or below the Km for each respective kinase. The mechanism of kinase inhibition was evaluated using the AlphaScreen Assay by determining the IC50 values over a range of ATP concentrations [1].
动物实验	Female nu/nu mice were housed according to the Exelixis Institutional Animal Care and Use Committee guidelines. H441 cells (3 × 10^6) were implanted intradermally into the hind flank and when tumors reached approximately 150 mg, tumor weight was calculated using the formula: (tumor volume = length (mm) × width^2 (mm^2)]/2, mice were randomized (n = 5 per group) and orally administered a single 100 mg/kg dose of cabozantinib or vehicle. Tumors were collected at the indicated time points. Pooled tumor lysates were subjected to immunoprecipitation with anti-MET and Western blotting with anti-phosphotyrosine MET. After blot stripping, total MET was quantitated as a loading control. In a separate experiment, naive mice (n = 5 per group) were administered a single 100 mg/kg dose of cabozantinib or vehicle, followed by intravenous administration of HGF (10 μg per mouse) 10 minutes before liver collection. Analysis of MET phosphorylation in liver lysates was as described above. In a separate experiment, naive mice (n = 5 per group) were administered a single 100 mg/kg dose of cabozantinib or vehicle, followed by intravenous administration of VEGF (10 μg per mouse) 30 minutes before lung collection. Pooled lung lysates were subjected to immunoprecipitation with FLK1 and Western blotting with anti-phosphotyrosine. After blot stripping, total FLK1 was quantitated as a loading control [1].
体外活性	方法：前列腺癌细胞 LNCaP、C4-2B 和 PC-3 用 Cabozantinib (0.01-5 µM) 处理 72 h，使用 WST-1 Assay 检测细胞活力。结果：Cabozantinib 以剂量依赖的方式抑制 LNCaP、C4-2B 和 PC-3 细胞系的细胞活力。[1] 方法：人肾癌细胞 786-O 和 A498 用 Cabozantinib (10-100 nM) 处理 1 h，随后用 HGF (1 nM) 刺激 20 min，使用 Western Blot 检测靶点蛋白表达水平。结果：10 nM Cabozantinib 处理抑制了 HGF 激活的 pMET、pAKT、pERK 和 p-mTOR。[2]
体内活性	方法：为检测体内抗肿瘤活性，将 Cabozantinib (60 mg/kg) 口服给药给胫骨内注射前列腺癌细胞 Ace-1 的 SCID 小鼠，每天一次，持续五周。结果：Cabozantinib 抑制 Ace-1 细胞在体内的进展。[1] 方法：为检测体内抗肿瘤活性，将 Cabozantinib (1-60 mg/kg) 口服给药给携带肿瘤 MDA-MB-231、H441 或 C6 的 nu/nu 小鼠，每天一次，持续 12-14 天。结果：Cabozantinib 以剂量依赖的方式抑制肿瘤生长。[3]
存储条件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	H2O : < 1 mg/mL (insoluble or slightly soluble) DMSO : 50 mg/mL (99.7 mM) 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 9.3 mg/mL (18.54 mM), Suspension. Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. Ethanol : < 1 mg/mL (insoluble or slightly soluble)
关键字	CD135 \| angiogenesis \| c-Kit \| TAM Receptor \| CD117 \| Tyro3 \| HT1080 \| Fms like tyrosine kinase 3 \| Inhibitor \| Axl \| A431 \| VEGFR \| antiangiogenic \| FLT3 \| c-Met/HGFR \| BMS 907351 \| B16F10 cells \| SCFR \| Apoptosis \| inhibit \| BMS907351 \| XL-184 \| Cabozantinib \| Vascular endothelial growth factor receptor \| Cluster of differentiation antigen 135 \| XL 184 \| Mer
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卡博替尼|||XL184|||BMS-907351|TargetMol

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起，为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部，化学事业部，生物事业部和新材料部。从虚拟筛选到实体化合物分子供应；从商业化产品销售到个性化定制合成；从对明确靶点的分子筛选到对明确分子的多靶点筛选，从高通量筛选到化学结构优化，我们都可以满足您的科研用品及技术服务的需求。经过在中国市场五年的精心耕耘，我们已成为筛选化合物领域优秀的供应商，为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

成立日期	(12年)
注册资本	566.2651万人民币
员工人数	100-500人
年营业额	￥ 1亿以上
经营模式	贸易,试剂,定制,服务
主营行业	化学试剂,生物活性小分子