您的位置：首页 > 产品中心 > Bcr-abl Inhibitor III, GNF-5-Calbiochem
Bcr-abl Inhibitor III, GNF-5-Calbiochem
| 产品编号： | 4155250 |
| 规格： | 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. |
| 包装规格： | 10 MG |
| 产品类别： | 进口试剂 |
| 品牌： | Sigma-Aldrich |
| 优惠价： | 立即咨询 |
产品别名
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
基本信息
| Empirical Formula【经验(实验)分子式】 | C20H17F3N4O3 |
| Molecular weight | 418.37 |
| General description【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. |
| Warning【警告】 | Toxicity: Standard Handling (A) |
| Reconstitution【重悬】 | Following reconstitution, aliquot and freeze (-20°C). Stock solutions are are stable for up to 6 months at -20°C. |
| Other Notes【其他说明】 | Zhang, J., et al. 2010. Nature463, 501. |
| Legal Information【法律信息】 | CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany |
产品性质
| Quality Level【质量水平】 | 100 |
| Assay【测定】 | ≥97% (HPLC) |
| form【形式】 | powder |
| manufacturer/tradename | Calbiochem® |
| storage condition【储存条件】 | OK to freeze protect from light |
| color【颜色】 | off-white |
| solubility【溶解性】 | DMSO: 50 mg/mL, clear, colorless |
| shipped in【运输】 | ambient |
| storage temp.【储存温度】 | 2-8℃ |
| packaging【包装】 | 10 mg in Glass bottle Packaged under inert gas |
安全信息
| Storage Class Code【储存分类代码】 | 11 - Combustible Solids |
| WGK | WGK 3 |
