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Cabozantinib S-malate

产品编号 T1797 CAS 1140909-48-3

别名: 苹果酸卡博替尼, Cabozantinib, 卡博替尼苹果酸盐, XL184, Cabozantinib Malate

Cabozantinib S-malate (XL184) 是一种多受体酪氨酸激酶抑制剂，抑制VEGFR2，c-Met，Kit，Axl 和Flt3的IC50分别为0.035，1.3，4.6，7 和 11.3 nM。

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Cabozantinib S-malate Chemical Structure

Cabozantinib S-malate, CAS 1140909-48-3

规格	价格/CNY	货期
5 mg	￥ 329	现货
10 mg	￥ 475	现货
25 mg	￥ 653	现货
50 mg	￥ 883	现货
100 mg	￥ 1,310	现货
200 mg	￥ 2,270	现货
500 mg	￥ 3,850	现货
1 mL * 10 mM (in DMSO)	￥ 659	现货

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其他形式的 Cabozantinib S-malate:

Cabozantinib
现货
Cabozantinib hydrochloride
现货

选择批次

纯度: 100%

纯度: 98.87%

纯度: 98%

更多批次查询请联系客服

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 S-malate (XL184) is the s-malate salt form of cabozantinib, an orally bioavailable, small molecule receptor tyrosine kinase (RTK) inhibitor with potential antineoplastic activity.
靶点活性	VEGFR2/KDR:0.035 nM, c-Met:1.3 nM
体外活性	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]
体内活性	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]
激酶实验	The inhibition profile of cabozantinib against a broad panel of 270 human kinases is determined using luciferase-coupled chemiluminescence,?33P-phosphoryl transfer, or AlphaScreen technology. Recombinant human full-length, glutathione?S-transferase tag, or histidine tag fusion proteins are used, and half maximal inhibitory concentration (IC50) values are 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 is evaluated using the AlphaScreen Assay by determining the IC50?values over a range of ATP concentrations.
细胞实验	Cells are exposed to various concentrations of Cabozantinib for 48 hours. Cell growth is determined by MTS assays using CellTiter96 Aqueous Non-Radioactive Cell Proliferation Assay kit. Absorbance is measured at a wavelength of 490 nm, and the absorbance values of treated cells are presented as a percentage of the absorbance of untreated cells. (Only for Reference)

别名	苹果酸卡博替尼, Cabozantinib, 卡博替尼苹果酸盐, XL184, Cabozantinib Malate
分子量	635.59
分子式	C32H30FN3O10
CAS No.	1140909-48-3

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 (146.3 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	1.5733 mL	7.8667 mL	15.7334 mL	39.3335 mL
	5 mM	0.3147 mL	1.5733 mL	3.1467 mL	7.8667 mL
	10 mM	0.1573 mL	0.7867 mL	1.5733 mL	3.9334 mL
	20 mM	0.0787 mL	0.3933 mL	0.7867 mL	1.9667 mL
	50 mM	0.0315 mL	0.1573 mL	0.3147 mL	0.7867 mL
	100 mM	0.0157 mL	0.0787 mL	0.1573 mL	0.3933 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. You WK, et al. Cancer Res, 2011, 71(14), 4758-4768. 2. Torres KE, et al. Clin Cancer Res, 2011, 17(12), 3943-3955. 3. Yakes FM, et al. Mol Cancer Ther, 2011, 10(12), 2298-2308.

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 S-malate 1140909-48-3 Angiogenesis Apoptosis Tyrosine Kinase/Adaptors c-Met/HGFR VEGFR TAM Receptor c-Kit 苹果酸卡博替尼 Vascular endothelial growth factor receptor Cabozantinib BMS 907351 Inhibitor XL-184 BMS907351 Cabozantinib S malate 卡博替尼苹果酸盐 Cabozantinib Smalate inhibit XL 184 XL184 Cabozantinib Malate BMS-907351 inhibitor

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Cabozantinib S-malate

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

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