产品描述
| 溶解性 | DMSO 115 mg/mL Water <1 mg/mL Ethanol <1 mg/mL |
| 存贮条件 | 储存温度-20°C |
| 产品介绍 | Bafetinib (INNO-406)是一种有效的，选择性的，Bcr-Abl/Lyn双重抑制剂，IC50为5.8 nM/19 nM，对T315I突变型的磷酸化没有抑制作用，对PDGFR和c-Kit的作用效果稍弱。 |
| 生化机理 | Bafetinib (1-10 μM) concentration dependently inhibits PAR2-TRPV4 coupling. In TRPV4 HEKs, 10 μM Bafetinib significantly inhibits the coupling response to SLIGRL and trypsin compared with vehicle control. Bafetinib inhibits the signalling pathway leading to TRPV4 channel opening, downstream of PAR2 activation, most likely by blocking the activation of a tyrosine kinase. Bafetinib blocks WT Bcr-Abl autophosphorylation and its downstream kinase activity with IC50 of 11 nM and 22 nM in K562 and 293T cells, respectively. Bafetinib suppresses the growth of the Bcr-Abl-positive cell lines including K562, KU812, and BaF3/wt cells potently without effects on the proliferation of the Bcr-Abl-negative U937 cell line. Moreover, Bafetinib exhibits a dose-dependent antiproliferative effect against Bcr-Abl point mutant cell lines, such as BaF3/E255K cells |
| 别名 | NS-187;巴非替尼; N-[3-([4,5'-联嘧啶]-2-基氨基)-4-甲基苯基]-4-[[(3S)-3-(二甲基氨基)-1-吡咯烷基]甲基]-3-(三氟甲基)苯甲酰胺;NS-187;N-[3-([4,5'-bipyrimidin]-2-ylamino)-4-methylphenyl]-4-[[(3S)-3-(dimethylamino)-1-pyrrolidinyl]methyl]-3-(trifluoromethyl)benzamide |
