品牌	貨號	產(chǎn)品規(guī)格	價格(RMB)	庫存（上海）	北京	武漢	南京
源葉(MedMol)	S80135-5mg	99%	￥420.00元	9	-	-	-
源葉(MedMol)	S80135-10mg	99%	￥670.00元	10	-	-	-
源葉(MedMol)	S80135-50mg	99%	￥1950.00元	6	-	-	-

產(chǎn)品介紹

A66 is a highly specific and selective p110α inhibitor with an IC50 of 32 nM.

產(chǎn)品描述： A66 is a highly specific and selective p110α inhibitor with an IC50 of 32 nM.

靶點： 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：
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。

參考文獻

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A66 99%

(2S)-N1-(5-(2-tert-butylthiazol-4-yl)-4-methylthiazol-2-yl)pyrrolidine-1,2-dicarboxamide