半岛bd体育手机客户端 说明
生化/生理作用
ALW-II-41-27 is an RG-25 (RG25) structural analog that exhibits enhanced type II kinase inhibitor activity against ephrin type-A receptor 2/EphA2/ECK (IC50 = 11 nM vs 770 nM with NG25) by targeting the ATP-binding pocket and an allosteric site next to the “DFG” motif. ALW-II-41-27 inhibits constitutive and ephrin A1-induced EphA2 tyrosine phosphorylation (0.1-1 μM; H358), effectively suppressing EphA2-dependent cancer survivalin vitro(0.1-1 μM for 72 hrs; NSCLC) and xenograft tumor growth in micein vivo(15-30 mg/kg b.i.d. i.p.; H358 NSCLC & A375 melanoma). Note: ALW-II-41-27 and RG-25 (RG25) display very similar kinase-targeting profiles with EphA2 being a notable exception, RG25 can therefore serve as a control for ALW-II-41-27 when probing EphA2-mediated cellular functions.
基本信息
| 经验(实验)分子式 | C32H32F3N5O2S |
| 分子量 | 607.69 |
| MDL编号 | MFCD25372028 |
半岛bd体育手机客户端 性质
| 质量水平 | 100 |
| 测定 | ≥98% (HPLC) |
| 形式 | powder |
| 颜色 | white to beige |
| 溶解性 | DMSO: 2 mg/mL, clear |
| 储存温度 | 2-8℃ |
| SMILES string | O=C(NC1=CC=C(CN2CCN(CC)CC2)C(C(F)(F)F)=C1)C3=CC=C(C)C(NC(C4=CC(C5=CC=CS5)=CN=C4)=O)=C3 |
安全信息
| 储存分类代码 | 11 - Combustible Solids |
| WGK | WGK 3 |
| 闪点(F) | Not applicable |
| 闪点(C) | Not applicable |
Sigma-Aldrich
m.cnreagent.com
