| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| B408114-1ml |
1ml |
现货  |
|
| 别名 | 巴非替尼（INNO-406） |
|---|---|
| 英文别名 | NS-187 | (S)-4-((3-(dimethylamino)pyrrolidin-1-yl)methyl)-N-(4-methyl-3-(4-(pyrimidin-5-yl)pyrimidin-2-ylamino)phenyl)-3-(trifluoromethyl)benzamide |
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | Bafetinib (INNO-406) |
| 生化机理 | 巴非替尼（INNO-406，NS-187）是一种强效、选择性的 Bcr-Abl/Lyn 双重抑制剂，在无细胞实验中的 IC50 为 5.8 nM/19 nM，不能抑制 T315I 突变体的磷酸化，对 PDGFR 和 c-Kit 的作用较弱。第二阶段 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 作用机制 | 酪氨酸蛋白激酶 Lyn 抑制剂 |
| 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。 Information Bafetinib (INNO-406, NS-187) is a potent and selective dualBcr-Abl/Lyninhibitor withIC50of 5.8 nM/19 nM in cell-free assays, does not inhibit the phosphorylation of the T315I mutant and is less potent to PDGFR and c-Kit. Phase 2. 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. In Bcr-Abl+ leukemia cell lines, Bafetinib induces both caspase-mediated and caspase-independent cell death by blocking the phosphorylation of Bcr-Abl. In vivo In Bcr-Abl–positive KU812 mouse model, Bafetinib (0.2 mg/kg/day) significantly inhibits tumor growth, and completely inhibits tumor growth without adverse effects at 20 mg/kg/day. For Balb/c mice, Bafetinib shows maximal tolerated dose of 200 mg/kg/d and bioavailability value (BA) of 32%. In a Central nervous system (CNS) leukemia model bearing Ba/F3/wt bcr-ablGFP, Ba/F3/Q252H, or Ba/F3/M351T cells, combination treatment of Bafetinib (60 mg/kg) and cyclosporine A (CsA) (50 mg/kg) leads to more significant inhibition of leukemia growth in the brain than either Bafetinib or CsA alone. cell lines： Concentrations：0-10 μM Incubation Time：72 hours Powder Purity:≥96% |
| IC50 | Abl, IC50: 5.8 nM |
|---|---|
| ALogP | 4.197 |
| hba_count | 5 |
| HBD Count | 2 |
| Rotatable Bond | 9 |
| 分子类型 | 小分子 |
|---|---|
| Canonical SMILES | CN(C)C1CCN(C1)CC2=CC=C(C=C2C(F)(F)F)C(=O)NC3=CC=C(C)C(=C3)NC4=NC=CC(=N4)C5=CN=CN=C5 |
| 分子量 | 576.62 |
| Reaxy-Rn | 26429538 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=26429538&ln= |
| 溶解性 | Solubility (25°C) In vitro DMSO: 47 mg/mL (198.9 mM); Ethanol: 47 mg/mL (198.9 mM); Water: Insoluble; |
|---|---|
| DMSO(mg / mL) Max Solubility | 100 |
| DMSO(mM) Max Solubility | 173.42 |
| Water(mg / mL) Max Solubility | <1 |
| Reaxy-Rn | 26429538 |
|---|---|
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=26429538&ln= |
| Concentration | 9-11（mmol/L） |
|---|---|
| Proton NMR spectrum | Conforms to Structure |
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