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位置:首页 > 品牌 > Sigma-Aldrich > Trk Inhibitor III, GNF-5837-CAS 1033769-28-6-Calbiochem

Trk Inhibitor III, GNF-5837-CAS 1033769-28-6-Calbiochem

品牌
Sigma-Aldrich
CAS
1033769-28-6
货号
648451
规格纯度
The Trk Inhibitor III, GNF-5837 controls the biological activity of Trk. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.
参考价格
4137.78 *本价格含增值税费
促销
服务
  • 原厂保证
  • 包邮
  • 增值税票
数量
-+
产品名称:
1033769-28-6
Trk Inhibitor III, GNF-5837-CAS 1033769-28-6-Calbiochem
(Z)-1-(3-((3-((1H-Pyrrol-2-yl)methylene)-2-oxoindolin-6-yl)amino)-4-methylphenyl)-3-(2-fluoro-5-(trifluoromethyl)phenyl)urea
产品介绍:

产品说明

一般描述

An orally bioavailable oxindole compound that and acts as a potent, reversible and type II DFG-out inhibitor of pan-Trk activity (IC50 = 8 and 12 nM for TrkA and TrkB). Shown to target Trk (tropomyosin receptor kinase) ATP binding cleft and an immediately adjacent hydrophobic pocket. Preferentially arrests the proliferation of Ba/F3 cells fused with Tel-TrkA, Tel-TrkB and Tel-TrkC (IC50 = 11, 9 and 7 nM, respectively) and in Ba/F3 and RIE cells expressing both TrkA and NGF (IC50 = 42 and 17 nM, respectively) over Mo7e-c-Kit and Rat-A10-PDGFR (IC50 = 1 and 0.5 µM) and Ba/F3-Tel-KDR and wt-Ba/F3 cells (IC50 = 3.0 and 5.6 µM). Displays ~100-fold greater selectivity among a panel of 59 closely related kinases and in 33 cellular kinase assays. Weakly active against relevant cytochrome P450 isozymes and hERG channel, and exhibit adequate microsomal stability, pharmacokinetic profile and efficacy in mice and rats. Suppresses tumor growth in a mouse RIE-TrkAmNGF xenograft model (50 mg/kg, p.o.).

包装

10 mg in Glass bottle
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 6 months at -20°C.

其他说明

Albaugh, P., et al. 2012. ACS Med. Chem. Lett.3, In press.

法律信息

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

基本信息

经验(实验)分子式C28H21F4N5O2
分子量535.49
MDL编号MFCD24386809

产品性质

质量水平100
测定≥98% (HPLC)
形式powder
manufacturer/tradenameCalbiochem®
储存条件OK to freeze
protect from light
颜色 orange
溶解性DMSO: 50 mg/mL
运输ambient
储存温度2-8℃
SMILES stringO=C(NC1=C(C=CC(C(F)(F)F)=C1)F)NC2=CC(NC3=CC(NC/4=O)=C(C=C3)C4=C\C5=CC=CN5)=C(C)C=C2

安全信息

储存分类代码11 - Combustible Solids
WGKWGK 3
闪点(F)Not applicable
闪点(C)Not applicable

Sigma-Aldrich

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