| 產(chǎn)品描述： | A66 is a highly specific and selective p110α inhibitor with an IC50 of 32 nM. |
| 靶點(diǎn)： |
p110α:32 nM (IC50);p110α E545K:30 nM (IC50);p110α H1047R:43 nM (IC50);p110γ:3480 nM (IC50);PI3K-C2β:462 nM (IC50);PI4Kβ:236 nM (IC50);PI3K |
| 體內(nèi)研究： |
The optimal dosing strategy for xenograft studies is determined by investigating the drug pharmacokinetics after a dose of 10 mg/kg of body weight by intraperitoneal injection in CD-1 mice. Despite a short half-life of only 0.42 h, the large Cmax (8247 nM) of A66 S that is reached 30 min after dosing ensured that the AUC0-inf (area under the curve from zero time to infinity) (6809 nM?h) is similar to that of BEZ-235 (7333 nM?h), which has a longer half-life of 2.73 h. Furthermore, the A66 on SK-OV-3 tumour tissue is tested using a single dose of 100 mg/kg of body weight to determine whether a long-lasting effect of the drug could be achieved on target tissues. These studies show that A66 causes a profound reduction in the phosphorylation of Akt/PKB and p70 S6 kinase, but not of ERK (extracellular-signal-regulated kinase), at both 1 and 6 h after dosing. Levels of A66 in plasma are determined to be 21.1±1.2 μM and 9.1±1.1 μM at 1 and 6 h after drug injection, whereas levels of A66 in the tumor are 22.7±2.1 μM and 16.0±1.3 μM at the same time points |
| 參考文獻(xiàn)： |
1. Jamieson S, et al. A drug targeting only p110α can block phosphoinositide 3-kinase signalling and tumour growth in certain cell types. Biochem J, 2011, 438(1), 53-62. 2. Sun M, et al. Cancer-derived mutations in the regulatory subunit p85alpha of phosphoinositide 3-kinase function through the catalytic subunit p110alpha. Proc Natl Acad Sci U S A, 2010, 107(35), 15547-15552. |
| 溶解性： |
DMSO : 50 mg/mL (127.06 mM; Need ultrasonic) |
| 保存條件： |
-20℃ |
| 配置溶液濃度參考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.541 ml |
12.706 ml |
25.411 ml |
| 5 mM |
0.508 ml |
2.541 ml |
5.082 ml |
| 10 mM |
0.254 ml |
1.271 ml |
2.541 ml |
| 50 mM |
0.051 ml |
0.254 ml |
0.508 ml |
|
| 注意： |
部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。 |
上海工商
危險(xiǎn)品化學(xué)品經(jīng)營(yíng)許可證（不帶存儲(chǔ)）
營(yíng)業(yè)執(zhí)照(三證合一)
北京