跳转至内容
Merck
CN
登录查看公司和协议定价

About This Item

经验公式(希尔记法):
C26H22Cl2N4O3
分子量:
509.38
UNSPSC代码:
12352200
NACRES:
NA.77
技术服务
需要帮助?我们经验丰富的科学家团队随时乐意为您服务。
让我们为您提供帮助

方案

≥98% (HPLC)

质量水平

表单

solid

效能

3 nM IC50

制造商/商品名称

Calbiochem®

储存条件

OK to freeze
protect from light

颜色

off-white

溶解性

DMSO: 100 mg/mL

储存温度

−20°C

一般描述

A cell-permeable anilinoquinazoline derivative that acts as a highly potent, irreversible, paralog selective inhibitor of fibroblast growth factor receptor 4 kinase (FGFR4; IC50 = 3 nM; kinact/KI = 0.6 x 105 (mol/L) -1s-1). Acts by forming a covalent bond with Cys552 within the ATP-binding pocket of FGFR4. Has minimal effect on FGFR1, 2, and 3 (IC50 = 591 nM, 493 nM, and 150 nM respectively) and does not display any activity towards a panel of 455 other protein kinases. Suppresses FGFR4 signaling and phosphorylation of downstream components in MDA-MB-453 cells. Also shown to be a potent inhibitor of downstream signaling in Hep 3B hepatocellular carcinoma (HCC) cells expressing FGF19 and induces caspase 3 and 7 activity. Inhibits the growth of Hep 3B HCC xenografts in murine model (100 mg/kg, b.i.d; p.o. for 21 days). Displays desirable pharmacokinetic properties with moderate bioavailability (18%) and t1/2 = 2.3 h (~ 10 mg/kg, p.o.).

生化/生理作用

Cell permeable: yes
Primary Target
FGFR4
Reversible: no

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

重悬

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

其他说明

Hagel, M., et al. 2015. Cancer Discov.5, 424.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

储存分类代码

11 - Combustible Solids

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable


分析证书(COA)

输入产品批号来搜索 分析证书(COA) 。批号可以在产品标签上"批“ (Lot或Batch)字后找到。

已有该产品?

在文件库中查找您最近购买产品的文档。

访问文档库

我们的科学家团队拥有各种研究领域经验,包括生命科学、材料科学、化学合成、色谱、分析及许多其他领域.

联系客户支持