Cabozantinib (BMS-907351)

目录号:S1119 别名: XL184 中文名称:卡博替尼

仅限科研使用

Cabozantinib (XL184, BMS-907351)是一种有效的VEGFR2抑制剂,在无细胞试验中IC50为0.035 nM,也能有效抑制c-Met、 Ret、 Kit、Flt-1/3/4、Tie2和AXL,IC50分别为1.3 nM,4 nM,4.6 nM,12 nM/11.3 nM/6 nM,14.3 nM 和 7 nM。Cabozantinib 在结肠癌细胞中可通过AKT/GSK-3β/NF-κB信号通路诱导PUMA依赖的凋亡。

Cabozantinib (BMS-907351) Chemical Structure

CAS: 849217-68-1

规格 价格 库存 购买数量
10mM (1mL in DMSO) RMB 1800.41 现货
RMB 902.82 现货
RMB 3837.48 现货
RMB 8176.22 现货
大包装 有超大折扣
大剂量询单有大折扣!

今日订购,明日送达 全国免运费 分装免费 分装成小规格产品(单支最小为1mg)
如1支10mg产品可分装为10支1mg产品

全国免费电话:400-668-6834   |   Email:info@selleck.cn

客户使用Selleck生产的Cabozantinib (BMS-907351)发表文献120篇:

产品安全说明书

VEGFR抑制剂选择性比较

相关VEGFR产品

生物活性

产品描述 Cabozantinib (XL184, BMS-907351)是一种有效的VEGFR2抑制剂,在无细胞试验中IC50为0.035 nM,也能有效抑制c-Met、 Ret、 Kit、Flt-1/3/4、Tie2和AXL,IC50分别为1.3 nM,4 nM,4.6 nM,12 nM/11.3 nM/6 nM,14.3 nM 和 7 nM。Cabozantinib 在结肠癌细胞中可通过AKT/GSK-3β/NF-κB信号通路诱导PUMA依赖的凋亡。
靶点
VEGFR2/KDR [1]
(Cell-free assay)
c-Met [1]
(Cell-free assay)
Axl [1]
(Cell-free assay)
0.035 nM 1.3 nM 7 nM
体外研究

XL184是多种受体酪氨酸激酶小分子抑制剂,尤其抑制c-Met 和VEGFR2。XL-184也有效作用于Ret, Kit, FLT1, FLT3, FLT4, Tie2, 和 AXL , IC50分别为 4 nM, 4.6 nM, 12 nM, 11.3 nM, 6 nM, 14.3 nM, 和7 nM。XL184微弱抑制 RON 和PDGFR-β,IC50分别为 124 nM和 234 nM,而对FGFR1则几乎没有抑制活性,IC50 为5.294 μM。[1] XL184低浓度(0.1-0.5 μM) 时处理MPNST细胞,也显著抑制组成型和诱导型Met磷酸化及其下游信号,且抑制 HGF诱导的MPNST细胞迁移和侵袭。XL184作用于细胞因子刺激的人脐静脉内皮细胞(HUVECs),也显著抑制Met和VEGFR2磷酸化。虽然XL184浓度为0.1 μM时不能抑制MPNST细胞生长,但是浓度为5-10 μM 时则能显著抑制MPNST细胞生长。[2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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Assay
Methods Test Index PMID
Western blot p-MET(Y1234/1235) / MET / p-EGFR(Y1068) / EGFR / p-Gab1(Y627) / Gab1 / p-AKT(S473) / p-ERK / p-EIF4E p-MET / p-ERK / p-AKT 29188469 29520051
Immunofluorescence α-tubulin 29520051
Growth inhibition assay Cell viability 23661005
体内研究 XL184按 30 mg/kg 剂量处理携带自发胰岛细胞瘤的RIP-Tag2 小鼠,扰乱 83%肿瘤血管, 降低周细胞和空基底膜袖,引起广泛瘤内缺氧和广泛的肿瘤细胞凋亡,且停药后延缓肿瘤血管再生长,与XL999相比更显著抑制VEGFR而不是c-Met,导致血管降低43%,说明抑制VEGFR,也抑制放大抑制血管新生的其他功能相关的受体酪氨酸激酶(RTK)。XL184也降低原发肿瘤的侵袭和减少转移。[1] XL184 每天按30 mg/kg剂量处理SCID小鼠,显著废除人 MPNST移植瘤生长和转移。[2] XL184 处理乳腺癌,肺癌胶质瘤模型,抑制肿瘤生长,这种作用存在剂量依赖性,降低肿瘤和内皮细胞增殖,促进凋亡。XL184按100 mg/kg 和 10 mg/kg剂量分别单独处理携带MDA-MB-231肿瘤的小鼠和携带C6肿瘤的大鼠,持续抑制肿瘤生长。[3]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

细胞实验: [2]
  • Cell lines: ST88-14, STS26T, 和MPNST724
  • Concentrations: 溶于DMSO,终浓度~10 μM
  • Incubation Time: 48小时
  • Method: 使用不同浓度XL184处理细胞48小时。通过MTS实验使用CellTiter96 Aqueous 非放射性细胞增殖实验试剂盒测定细胞生长。然后在 490 nm处测定吸光值。
动物实验:[1]
  • Animal Models: 携带自发胰岛肿瘤的RIP-TAG2转基因小鼠。
  • Dosages: ~60 mg/kg
  • Administration: 口服饲喂

溶解度(25°C)

体外

体内

从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
2% DMSO+30% PEG 300+5% Tween 80+ddH2O

5mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 501.51
化学式

C28H24FN3O5

CAS号 849217-68-1
储存条件 3年 -20°C 粉状
2年 -80°C 溶于溶剂

动物体内配方计算器(澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)

mg/kg g μL

第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)

% DMSO % % Tween 80 % ddH2O
%DMSO %

计算结果:

工作液浓度: mg/ml;

DMSO母液配制方法: mg 药物溶于μL DMSO溶液(母液浓度mg/mL,:如该浓度超过该批次药物DMSO溶解度,请先联系Selleck);

体内配方配制方法:μL DMSO母液,加入μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入μL ddH2O,混匀澄清。

体内配方配制方法:μL DMSO母液,加入μL Corn oil,混匀澄清。

注意:1. 首先保证母液是澄清的;
2.一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。

摩尔浓度计算器

质量 浓度 体积 分子量

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05048212 Not yet recruiting Drug: Nivolumab|Drug: Ipilimumab|Drug: Cabozantinib Brain Metastases|Renal Cell Carcinoma M.D. Anderson Cancer Center|Exelixis|Bristol-Myers Squibb February 28 2022 Phase 2
NCT05182164 Not yet recruiting Drug: Association of pembrolizumab + cabozantinib Soft Tissue Sarcoma Adult|Advanced Soft-tissue Sarcoma|Ewing Sarcoma|Osteosarcoma|Undifferentiated Pleomorphic Sarcoma Institut Bergonié|Ipsen|MSD France December 31 2021 Phase 2
NCT05100082 Recruiting Drug: Cabozantinib Hepatocellular Cancer Takeda November 17 2021 --
NCT05135975 Active not recruiting Drug: Cabozantinib Neuroblastoma|CNS Tumor|Sarcoma Nationwide Children''s Hospital|Exelixis October 18 2021 Phase 2
NCT05048901 Not yet recruiting Drug: Cabozantinib|Drug: Lanreotide Neuroendocrine TumorsGastroenteropancreatic National Health Research Institutes Taiwan|National Taiwan University Hospital|Taipei Veterans General Hospital Taiwan|Mackay Memorial Hospital|Tri-Service General Hospital|Changhua Christian Hospital|China Medical University Hospital|National Cheng-Kung University Hospital|Kaohsiung Medical University Chung-Ho Memorial Hospital September 30 2021 Phase 1|Phase 2

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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