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Bcr-abl Inhibitor III, GNF-5-Calbiochem

品牌
Sigma-Aldrich
货号
197224
规格纯度
The Bcr-abl Inhibitor III, GNF-5 controls the biological activity of Bcr-abl. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.
参考价格
3352.28 *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:
Bcr-abl Inhibitor III, GNF-5-Calbiochem
N-(2-Hydroxyethyl)-3-(6-(4-(trifluoromethoxy)phenylamino)pyrimidin-4-yl)benzamide, Abl Inhibitor III
Abl Inhibitor III, N-(2-Hydroxyethyl)-3-(6-(4-(trifluoromethoxy)phenylamino)pyrimidin-4-yl)benzamide
产品介绍:

产品说明

一般描述

A cell-permeable GNF-2 (Cat. No. 197221) N-hydroxyethyl carboxamide analog that exhibits in vivo efficacy in suppressing the proliferation of Bcr-abl-expressing Ba/F3 (93% and 83% of no-treatment control, respectively, on days 5 and 7 post treatment; 100 mg/kg b.i.d.) and bone marrow cells (~75% of no-treatment control in both WBC counts and spleen weight on day 7 post treatment; 50 mg/kg b.i.d.) in murine xenograft models of leukemia. Similar to GNF-2, GNF-5 exerts its effect via an allosteric mechanism (IC50 = 0.22 µM against wild-type Abl) by targeting the myristate-binding pocket near the c-terminus of Abl kinase domain and thereby altering the conformational dynamics of the ATP-binding pocket. GNF-5 is ineffective toward the myristate-binding site mutant E505K and the ATP-binding site ‘gatekeeper’ mutant T315I.
A cell-permeable GNF-2 (Cat. No. 197221) N-hydroxyethyl carboxamide analog that exhibits in vivo efficacy in suppressing the proliferation of Bcr-abl-expressing Ba/F3 (93% and 83% of no-treatment control, respectively, on days 5 and 7 post treatment; 100 mg/kg b.i.d.) and bone marrow cells (~75% of no-treatment control in both WBC counts and spleen weight on day 7 post treatment; 50 mg/kg b.i.d.) in murine xenograft models of leukemia. Similar to GNF-2, GNF-5 exerts its effect via an allosteric mechanism (IC50 = 0.22 µM against wild-type Abl) by targeting the myristate-binding pocket near the c-terminus of Abl kinase domain and thereby altering the conformational dynamics of the ATP-binding pocket. GNF-5 is ineffective toward the myristate-binding site mutant E505K and the ATP-binding site ‘gatekeeper’ mutant T315I.

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 are stable for up to 6 months at -20°C.

其他说明

Zhang, J., et al. 2010. Nature463, 501.

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C20H17F3N4O3
分子量418.37

产品性质

质量水平100
测定≥97% (HPLC)
形式powder
manufacturer/tradenameCalbiochem®
储存条件OK to freeze
protect from light
颜色 off-white
溶解性DMSO: 50 mg/mL, clear, colorless
运输ambient
储存温度2-8℃

安全信息

储存分类代码11 - Combustible Solids
WGKWGK 3

Sigma-Aldrich

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