半岛bd体育手机客户端 说明
生化/生理作用
GSK2126458 (GSK458) is an orally active, highly potent and selective ATP site inhibitor against phosphoinositide 3-kinase (PI3K p110α CI50 = 40 pM; p100 α/δ/γ/β Ki = 19/24/60/130 pM; p110α E542K/E545K/H1047R Ki = 8/8/9 pM), mTOR (mTORC1/C2 Ki = 180/300 pM) and DNA-PK (IC50 = 280 pM) with >10,000-fold selectivity over more than 240 other kinases evaluated. GSK458 inhibits cellular AKT pS473 and growth of breast cancer cells in cultures (pAKT/growth IC50 = 0.41/3 nM/T-47D and 0.18/2.4/BT-474) andin vivo(0.3-3 mg/kg, 5x per wk for 3 wks p.o. in mice).
基本信息
| 经验(实验)分子式 | C25H17F2N5O3S |
| 分子量 | 505.50 |
| MDL编号 | MFCD16038929 |
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 | FC(C=C1F)=CC=C1S(NC2=CC(C3=CC4=C(C5=CN=NC=C5)C=CN=C4C=C3)=CN=C2OC)(=O)=O |
安全信息
| 象形图 |   |
| 警示用语： | Danger |
| 危险声明 | H302 - H361fd - H372 |
| 预防措施声明 | P202 - P260 - P264 - P270 - P301 + P312 - P308 + P313 |
| 危险分类 | Acute Tox. 4 Oral - Repr. 2 - STOT RE 1 |
| 储存分类代码 | 6.1C - Combustible, acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects |
| WGK | WGK 3 |
| 闪点(F) | Not applicable |
| 闪点(C) | Not applicable |
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