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OXA-01
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
OXA-01图片
CAS NO:936889-68-8
包装与价格：
包装价格(元)
1mg电议
5mg电议
10mg电议
25mg电议

产品介绍
OXA-01 是一种有效的 mTORC1 和 mTORC2 抑制剂，IC50 值分别为 29 nM 和 7 nM。
Cas No.936889-68-8
化学名trans-4-[8-amino-1-(7-chloro-1H-indol-2-yl)imidazo[1,5-a]pyrazin-3-yl]-cyclohexanecarboxylic acid
Canonical SMILESOC([C@H]1CC[C@H](C2=NC(C3=CC4=C(C(Cl)=CC=C4)N3)=C5N2C=CN=C5N)CC1)=O
分子式C21H20CIN5O2
分子量409.9
溶解度≤3mg/ml in DMSO;1mg/ml in dimethyl formamide
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

OXA-01 is an ATP-competitive and selective inhibitor of both mTORC1 and mTORC2 with IC50 values of 29 nM and 7 nM, respectively [1].

The mammalian target of rapamycin (mTOR) is a serine/threonine kinase and exists in two complexes, mTORC1 and mTORC2. MTORC1 activation through PI3K and Akt controls cell growth and mTORC2 phosphorylates Akt, SGK1, and PKC to control cell survival and cytoskeletal organization [1].

OXA-01 is a dual inhibitor of mTORC1 and mTORC2, and inhibited mTOR kinase with IC50 value of 11 nM. In cell-based assays, OXA-01 inhibited mTOR signaling of phospho-4E-BP1 with IC50 value of 1.1 μM [1].

In GEO colorectal xenograft model, the median plasma concentration of OXA-01 was 25.6 μM at 1 hour and 13.2 μM at 8 hours, and OXA-01 slowed tumor growth. In RIP-Tag2 pancreatic neuroendocrine tumors, OXA-01 reduced Akt, 4E-BP1 and S6K phosphorylation. OXA-01 also decreased cellular proliferation and increased apoptosis. OXA-01 reduced VEGF production, which was associated with decreased tumor angiogenesis [1].

Reference:
[1].  Falcon BL, Barr S, Gokhale PC, et al. Reduced VEGF production, angiogenesis, and vascular regrowth contribute to the antitumor properties of dual mTORC1/mTORC2 inhibitors. Cancer Res. 2011 Mar 1;71(5):1573-83.