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Cabozantinib hydrochloride

产品编号 T5164 CAS 1817759-42-4

别名: XL184, Cabozantinib hydrochloride (849217-68-1(free base)), BMS-907351, 盐酸卡博替尼

Cabozantinib hydrochloride (XL184) 是一种有效的泛酪氨酸激酶抑制剂，可抑制 VEGFR2、c-Met、Kit、Axl 和 Flt4（IC50：0.035、1.3、4.6、7 和 6 nM）。

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Cabozantinib hydrochloride Chemical Structure

Cabozantinib hydrochloride, CAS 1817759-42-4

规格	价格/CNY	货期
1 mg	￥ 248	现货
2 mg	￥ 350	现货
5 mg	￥ 620	现货
10 mg	￥ 960	现货
25 mg	￥ 1,670	现货
50 mg	￥ 2,520	现货
100 mg	￥ 3,560	现货
200 mg	￥ 5,130	现货
500 mg	￥ 7,860	现货

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其他形式的 Cabozantinib hydrochloride:

Cabozantinib
现货
Cabozantinib S-malate
现货

选择批次

纯度: 97.09%

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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 hydrochloride (XL184) is a potent pan-tyrosine kinases inhibitor that inhibits VEGFR2, c-Met, Kit, Axl, and Flt4 (IC50s: 0.035, 1.3, 4.6, 7 and 6 nM).
靶点活性	RORα:172 nM (Ki), RORγ:111 nM (Ki)
体外活性	SR1001 binds specifically to the ligand-binding domains of RORα and RORγt, inducing a conformational change within the ligand-binding domain, resulting in suppression of the receptors' transcriptional activity. SR1001 inhibited the development of murine T(H)17 cells. Furthermore, SR1001 inhibited the expression of cytokines when added to differentiated murine or human T(H)17 cells [1]. Treatment with the RORγT inhibitor SR1001 to abrogate Th17 cell function reduced Th17-dependent learned helplessness [2].
体内活性	After myelin oligodendrocyte glycoprotein (MOG35–55) immunization at day 0, experimental autoimmune encephalomyelitis (EAE) mice were treated with SR1001 (25 mg/kg, b.i.d. i.p.) for the duration of the study. Further analysis of spinal cords from mice harvested at day 18 post-immunization revealed that SR1001 repressed Il17a mRNA expression by ~60%, as well as reduced Il21, and Il22 mRNA expression [1]. When these mice were injected with SR1001, the circadian rhythm of CS expression was eliminated [3].
细胞实验	CD4+ T cells were isolated as described previously and in the Supplementary Materials. CD4+ T cells cultured with splenic feeder cells were activated with 2.5 μg/mL of anti-CD3 (clone 145–11), and differentiated to Th17 cells by addition of IL-6 (20 ng/mL; Peprotech), TGFβ (5 ng/mL), anti-IL-4 (10 μg/mL; clone 11B11, UAB core facility) and anti-IFNγ (10 μg/mL; clone XMG1.2, UAB core facility). After 5 days of differentiation toward Th17 cells, cells were recovered after histopaque gradient purification and resuspended in PBS. An aliquot of cells was used to evaluate the percent of Th17 cells (~40%) and ~10–20×106 undifferentiated CD4+ T or Th17 cells were injected in 500 μL PBS by tail vein 48 h prior to behavioral testing. Where indicated, mice were injected intraperitoneally with 100 μg anti-IL-17A, or 125 μg SR1001 daily beginning 1 day before Th17 cell transfer, and this was continued throughout the experiment. As controls, mice were injected i.v. with ~10–20×106 CD4+ T cells to evaluate the effect of non-differentiated cells, or with 500 μL PBS to mimic the stress of tail vein i.v. injection 48 h prior to behavioral testing. Intracellular cytokine staining was carried out as described previously and in the Supplementary Information [2].
动物实验	For circadian gene expression experiments male C57BL6 mice (8–10 weeks of age) were either maintained on a L:D (12h∶12h) cycle or on constant darkness (1 day). At the circadian time (CT) 0 animals were administered a single dose of 25 mg/kg SR1001 (i.p.) and groups of animals (n?=?6) were sacrificed at CT0, CT6, CT12, and CT18. Gene expression was determined by real-time qPCR. Gene expression was normalized to Cyclophin b in all experiments [3].

别名	XL184, Cabozantinib hydrochloride (849217-68-1(free base)), BMS-907351, 盐酸卡博替尼
分子量	537.96
分子式	C28H25ClFN3O5
CAS No.	1817759-42-4

存储

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

溶解度

DMSO: 5.38 mg/mL (10 mM), Sonication is recommended.

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	1.8589 mL	9.2944 mL	18.5887 mL	46.4719 mL
	5 mM	0.3718 mL	1.8589 mL	3.7177 mL	9.2944 mL
	10 mM	0.1859 mL	0.9294 mL	1.8589 mL	4.6472 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

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浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

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参考文献

1. Yakes FM, et al. Cabozantinib (XL184), a novel MET and VEGFR2 inhibitor, simultaneously suppresses metastasis, angiogenesis, and tumor growth. Mol Cancer Ther, 2011, 10(12), 2298-2308. 2. Torres KE, et al. Activated MET is a molecular prognosticator and potential therapeutic target for malignant peripheral nerve sheath tumors.Clin Cancer Res. 2011 Jun 15;17(12):3943-55. 3. You WK, et al. VEGF and c-Met blockade amplify angiogenesis inhibition in pancreatic islet cancer. Cancer Res, 2011, 71(14), 4758-4768.

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 hydrochloride 1817759-42-4 Angiogenesis Metabolism Tyrosine Kinase/Adaptors VEGFR FLT c-Met/HGFR TAM Receptor c-Kit ROR inhibit CD135 Mer Fms like tyrosine kinase 3 Inhibitor XL184 SCFR BMS 907351 Axl XL 184 Cluster of differentiation antigen 135 XL-184 Vascular endothelial growth factor receptor Cabozantinib hydrochloride (849217-68-1(free base)) angiogenesis CD117 BMS-907351 BMS907351 FLT3 HT1080 Cabozantinib Hydrochloride A431 antiangiogenic Apoptosis Tyro3 Cabozantinib 盐酸卡博替尼 B16F10 cells inhibitor

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Cabozantinib hydrochloride

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