产品说明
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) and in 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 |
产品性质
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 |