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Cabozantinib

产品编号 T2586 CAS 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。

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Cabozantinib, CAS 849217-68-1

规格	价格/CNY	货期
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 * 10 mM (in DMSO)	￥ 713	现货

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其他形式的 Cabozantinib:

Cabozantinib S-malate
现货
Cabozantinib hydrochloride
现货

选择批次

纯度: 99.88%

纯度: 99.59%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

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	MET (Y1248H):3.8 nM (cell free), FLT3:11.3 nM (cell free), MET:1.3 nM (cell free), Axl:7 nM (cell free), RET:5.2 nM (cell free), VEGFR2:0.035 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
分子量	501.51
分子式	C28H24FN3O5
CAS No.	849217-68-1

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 93 mg/mL (185.4 mM)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.994 mL	9.9699 mL	19.9398 mL	49.8495 mL
	5 mM	0.3988 mL	1.994 mL	3.988 mL	9.9699 mL
	10 mM	0.1994 mL	0.997 mL	1.994 mL	4.9849 mL
	20 mM	0.0997 mL	0.4985 mL	0.997 mL	2.4925 mL
	50 mM	0.0399 mL	0.1994 mL	0.3988 mL	0.997 mL
	100 mM	0.0199 mL	0.0997 mL	0.1994 mL	0.4985 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Dai J, et al. Cabozantinib inhibits prostate cancer growth and prevents tumor-induced bone lesions. Clin Cancer Res. 2014 Feb 1;20(3):617-30. 2. Xie Z, et al. MET Inhibition in Clear Cell Renal Cell Carcinoma. J Cancer. 2016 Jun 18;7(10):1205-14. 3. Yakes FM, et al. Cabozantinib (XL184), a novel MET and VEGFR2 inhibitor, simultaneously suppresses metastasis, angiogenesis, and tumor growth. Mol Cancer Ther. 2011 Dec;10(12):2298-308.

文献引用

1. Chu T H, Ko C Y, Tai P H, et al. Leukocyte cell-derived chemotaxin 2 regulates epithelial-mesenchymal transition and cancer stemness in hepatocellular carcinoma. Journal of Biological Chemistry. 2022: 102442. 2. Sequera C, Grattarola M, Holczbauer A, et al.MYC and MET cooperatively drive hepatocellular carcinoma with distinct molecular traits and vulnerabilities.Cell death & disease.2022, 13(11): 1-15. 3. Zaccagnino A, Vynnytska-Myronovska B, Stöckle M, et al.An In Vitro Analysis of TKI-Based Sequence Therapy in Renal Cell Carcinoma Cell Lines.International Journal of Molecular Sciences.2023, 24(6): 5648.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

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：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 μL，一共给药动物10 只，您使用的配方为5% 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 μL DMSO (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：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：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。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 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：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Cabozantinib 849217-68-1 Angiogenesis Apoptosis Tyrosine Kinase/Adaptors VEGFR FLT TAM Receptor c-RET c-Met/HGFR c-Kit CD135 angiogenesis CD117 Tyro3 HT1080 卡博替尼 Fms like tyrosine kinase 3 Inhibitor Axl A431 antiangiogenic FLT3 BMS 907351 B16F10 cells SCFR inhibit BMS907351 XL-184 XL184 Vascular endothelial growth factor receptor Cluster of differentiation antigen 135 XL 184 BMS-907351 Mer inhibitor

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Cabozantinib

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

文献引用

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords