产品描述
| 溶解性 | Soluble in DMSO or EtOH |
| 存贮条件 | 储存温度 2-8°C |
| 应用 | An inhibitor of c-Abl and Bcr-abl activity |
| 产品介绍 | GNF-2是一种高选择性，非ATP竞争性的Bcr-Abl抑制剂，对Flt3-ITD， Tel-PDGFR， TPR-MET和Tel-JAK1转化的肿瘤细胞没有作用活性。 |
| 备注 | GNF-2 is a highly selective non-ATP competitive inhibitor of Bcr-Abl, shows no activity to Flt3-ITD, Tel-PDGFR, TPR-MET and Tel-JAK1 transformed tumor cells. |
| 生化机理 | Bcr-abl Inhibitor is a cell-permeable pyrimidine compound that binds to and inhibits the c-Abl myristoyl binding pocket. Bcr-abl Inhibitor acts as an allosteric, non-ATP-competitive inhibitor of cellular Bcr-abl activity and Bcr-abl-dependent cellular functions. Bcr-abl Inhibitor exhibits little inhibitory effect against a panel of 63 kinases even at concentration as high as 10 μM, nor does it inhibit c-Abl or Bcr-abl in cell-free in vitro kinase assays. Bcr-abl inhibitor exhibits potent and selective antiproliferative activity toward Bcr-abl-expressing cells (IC50 = 138 nM, 194 nM, 268 nM and 273 nM in Ba/F3.p210, Ba/F3.p185Y253H, SUP-B15 and Ba/F3.p210E255V, and K562, respectively). |
| 别名 | GNF 2; 3-[6-[[4-(三氟甲氧基)苯基]氨基]-4-嘧啶基]苯甲酰胺;GNF 2;GNF2;Bcr-abl Inhibitor;3-[6-[[4-(Trifluoromethoxy)phenyl]amino]-4-pyrimidinyl]benzamide |
