质量水平
检测方案
≥98% (HPLC)
形式
powder
颜色
white to beige
溶解性
DMSO: 2 mg/mL, clear
储存温度
2-8°C
SMILES字符串
FC(C=C1F)=CC=C1S(NC2=CC(C3=CC4=C(C5=CN=NC=C5)C=CN=C4C=C3)=CN=C2OC)(=O)=O
InChI
1S/C25H17F2N5O3S/c1-35-25-23(32-36(33,34)24-5-3-18(26)12-21(24)27)11-17(13-29-25)15-2-4-22-20(10-15)19(7-8-28-22)16-6-9-30-31-14-16/h2-14,32H,1H3
InChI key
CGBJSGAELGCMKE-UHFFFAOYSA-N
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).
警示用语：
Danger
危险声明
危险分类
Acute Tox. 4 Oral - Repr. 2 - STOT RE 1
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
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