GSK2126458

产品名称：

1086062-66-9
GSK2126458
GSK 2126458
GSK-458
GSK2126458A
GSK-2126458
GSK 458
2,4-Difluoro-N-{2-(methyloxy)-5-[4-(4-pyridazinyl)-6-quinolinyl]-3-pyridinyl}benzenesulfonamide
GSK458
Omipalisib

产品介绍：

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