切换导航

Cabozantinib malate (XL184)

现货
Catalog No.
B1401
MET和VEGF受体2抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 1,000.00
现货
5mg
¥ 700.00
现货
25mg
¥ 2,000.00
现货
100mg
¥ 6,800.00
现货

电话: 021-55669583

邮箱: sales@apexbio.cn

全球经销商

Background

Cabozantinib malate is a potent inhibitor of MET andVEGF receptor2 with IC50 values of 1.3nM and 0.035nM [1].

Cabozantinib is a pan-tyrosine kinase inhibitor and is developed as an oral treatment of various cancers including MTC, GBM, NSCLC, pancreatic carcinoma, breast and colon cancer. The targets of cabozantinib are MET, VEGFR-2, RET, FLT3, KIT, AXL as well as TEK. In cellular assays, cabozantinib inhibits the phosphorylation of MET, VEGFR2, KIT, FLT3 and AXL with IC50 values of 7.8, 1.9, 5.0, 7.5 and 42μM, respectively [1, 2].

As a pan-tyrosine kinase inhibitor, cabozantinib can affect many biological processes. Cabozantinib inhibits the tubule formation of HMVEC cells with IC50 value of 6.7nM. In B16F10 cells, cabozantinib inhibits HGF-inducedmigration and invasion with IC50 values of 31nM and 9nM, respectively. Moreover, cabozantinib shows anti-proliferation efficacy in a variety of tumors such as SNU-5, Hs746T, MDA-MB-231 and U87MG. It is also reported that the combination of cabozantinib and gefitinib can cause potent inhibition of the gefitinib-resistant HCC827GR6 cell line [1, 2].

References:
[1] Yakes F M, Chen J, Tan J, et al. Cabozantinib (XL184), a novel MET and VEGFR2 inhibitor, simultaneously suppresses metastasis, angiogenesis, and tumor growth. Molecular cancer therapeutics, 2011, 10(12): 2298-2308.
[2] Zhang Y, Guessous F, Kofman A, et al. XL-184, a MET, VEGFR-2 and RET kinase inhibitor for the treatment of thyroid cancer, glioblastoma multiforme and NSCLC. IDrugs, 2010, 13(2): 112.

Chemical Properties

StorageStore at -20°C
M.Wt635.59
Cas No.1140909-48-3
FormulaC32H30FN3O10
Solubility≥31.8mg/mL in DMSO
Chemical Name1-N-[4-(6,7-dimethoxyquinolin-4-yl)oxyphenyl]-1-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide;(2S)-2-hydroxybutanedioic acid
SDFDownload SDF
Canonical SMILESCOC1=CC2=C(C=CN=C2C=C1OC)OC3=CC=C(C=C3)NC(=O)C4(CC4)C(=O)NC5=CC=C(C=C5)F.C(C(C(=O)O)O)C(=O)O
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验 [1]:

细胞系

TT细胞

溶解方法

在DMSO中的溶解度>31.8mg/mL。为了获得更高的浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月

反应时间

13.7, 41, 123, 370, 1111, 3333nmol/L 作用1h

应用

Cabozantinib抑制了多种形式的致癌RET激酶活性,包括M918T 和Y791F突变体。并且它抑制了包含RET C634W激活突变的TT肿瘤细胞的增殖,该突变在MEN2A(多发性内分泌瘤2A)和家族性MTC(甲状腺髓样癌)中最常出现。

动物实验[2]:

动物模型

携带H441细胞移植瘤的雌性nu/nu小鼠

剂量

一次性100 mg/kg,口服

应用

在小鼠模型中,cabozantinib显著的改变了肿瘤的病理学表现,导致了肿瘤和内皮细胞增殖的降低,增加细胞凋亡,在乳房,肺,胶质瘤模型中剂量依赖性的抑制肿瘤生长。重要的是,在肿瘤转移的模型中,cabozantinib没有增加肺部肿瘤负荷。

注意事项

请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的,属于正常现象。

References:

[1]. Yakes F M, Chen J, et al. Cabozantinib (XL184), a novel MET and VEGFR2 inhibitor, simultaneously suppresses metastasis, angiogenesis, and tumor growth. Molecular cancer therapeutics, 2011, 10(12): 2298-2308.

[2]. Zhang Y, Guessous F, et al. XL-184, a MET, VEGFR-2 and RET kinase inhibitor for the treatment of thyroid cancer, glioblastoma multiforme and NSCLC. IDrugs, 2010, 13(2): 112.

质量控制

化学结构

Cabozantinib malate (XL184)

相关生物数据

Cabozantinib malate (XL184)

相关生物数据

Cabozantinib malate (XL184)