AT13148 是一种ATP 竞争性AGC 激酶口服抑制剂，能够抑制 Akt1/Akt2/Akt3、p70S6K、PKA 和 ROCKI/ROCKII 的活性，IC50值分别为 38/402/50、8、3 和 6 nM/4 nM。
产品描述
AT13148 is an oral-active and ATP-competitive, multi-AGC kinase inhibitor for Akt1/2/3, p70S6K, PKA, and ROCKI/II.
体外活性
在人肿瘤异种移植物模型中,口服AT13148（50 mg/kg）能够抑制AKT 和p70S6K AGC激酶,表现出抗肿瘤活性.
体内活性
在PTEN缺陷型MES-SA细胞中,AT13148能够抑制AKT 和 p70S6K信号。对于PI3K-AKT-mTOR 或 RAS-RAF通路反常的癌细胞系（GI50=1.5-3.8 μM）,AT13148能够抑制多重AGC激酶,从而抑制癌细胞增殖。
激酶实验
In vitro kinase assays: AT13148 is assayed against 40 kinases and the percentage inhibition at 10 μM of AT13148 is determined. Individual IC50 values are measured for selected kinases using ATP concentrations equivalent to the Km for each enzyme.
细胞实验
Cytotoxicity is determined using a 72 h Alamar Blue assay or a 96 h SRB assay. (Only for Reference)
Cas No.
1056901-62-2
分子式
C17H16ClN3O
分子量
313.78
储存和溶解度
Ethanol:<1 mgml
H2O:<1 mgml
DMSO:58 mg/mL (184.8 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years
