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Cabozantinib

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产品编号 T2586Cas号 849217-68-1
别名 卡博替尼, XL184, BMS-907351

Cabozantinib (XL184) 是一种多靶点酪氨酸激酶受体抑制剂,可以抑制 VEGFR2、c-Met、Kit、Axl 和 Flt3 (IC50=0.035/1.3/4.6/7/11.3 nM)。Cabozantinib 具有抗肿瘤和抗血管生成活性。

Cabozantinib

Cabozantinib

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纯度: 99.88%
产品编号 T2586 别名 卡博替尼, XL184, BMS-907351Cas号 849217-68-1

Cabozantinib (XL184) 是一种多靶点酪氨酸激酶受体抑制剂,可以抑制 VEGFR2、c-Met、Kit、Axl 和 Flt3 (IC50=0.035/1.3/4.6/7/11.3 nM)。Cabozantinib 具有抗肿瘤和抗血管生成活性。

规格价格库存数量
1 mg¥ 276现货
2 mg¥ 393现货
5 mg¥ 635现货
10 mg¥ 898现货
25 mg¥ 1,550现货
50 mg¥ 2,370现货
100 mg¥ 3,320现货
200 mg¥ 4,530现货
500 mg¥ 6,560现货
1 mL x 10 mM (in DMSO)¥ 713现货
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产品介绍

生物活性
产品描述
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.
靶点活性
Axl:7 nM (cell free), RET:5.2 nM (cell free), VEGFR2:0.035 nM (cell free), MET (Y1248H):3.8 nM (cell free), FLT3:11.3 nM (cell free), MET:1.3 nM (cell free)
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]
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].
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].
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].
别名卡博替尼, XL184, BMS-907351
化学信息
分子量501.51
分子式C28H24FN3O5
CAS No.849217-68-1
SmilesC(NC1=CC=C(OC=2C3=C(C=C(OC)C(OC)=C3)N=CC2)C=C1)(=O)C4(C(NC5=CC=C(F)C=C5)=O)CC4
密度1.397 g/cm3
储存&溶解度
存储Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度信息
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)
溶液配制表
1mg5mg10mg50mg
1 mM1.9940 mL9.9699 mL19.9398 mL99.6989 mL
5 mM0.3988 mL1.9940 mL3.9880 mL19.9398 mL
10 mM0.1994 mL0.9970 mL1.9940 mL9.9699 mL
1mg5mg10mg50mg
20 mM0.0997 mL0.4985 mL0.9970 mL4.9849 mL
50 mM0.0399 mL0.1994 mL0.3988 mL1.9940 mL

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请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法:
TargetMol | Animal experiments比如您的给药剂量是 10 mg/kg ,每只动物体重 20 g ,给药体积 100 μLTargetMol | Animal experiments 一共给药动物 10 只 ,您使用的配方为 5% TargetMol | reagent DMSO+ 30%PEG300+ 5%Tween 80 + 60% ddH2O. 那么您的工作液浓度为 2 mg/mL
母液配置方法: 2 mg 药物溶于 50 μLDMSOTargetMol | reagent ( 母液浓度为 40 mg/mL ), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:50μLDMSOTargetMol | reagent 母液,添加 300 μLPEG300TargetMol | reagent 混匀澄清,再加 50μLTween 80, 混匀澄清,再加 600μLddH2OTargetMol | reagent 混匀澄清

以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。

1 请输入动物实验的基本信息
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2 请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
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