Torin 2 |
رقم الكتالوجGC13858 |
Torin 2 هو مثبط mTOR مع EC50 من 0.25 نانومتر لتثبيط نشاط mTOR الخلوي ، ويعرض انتقائية 800 ضعف على PI3K (EC50: 200 نانومتر)يثبط Torin 2 أيضًا DNA-PK باستخدام IC50 بمقدار 0.5 نانومتر في الفحص الخالي من الخلايايمكن لـ Torin 2 قمع كلاً من mTORC1 و mTORC2
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Cas No.: 1223001-51-1
Sample solution is provided at 25 µL, 10mM.
Torin2 is a potent, selective and orally available inhibitor of mTOR with EC50 value of 0.25nM [1].
Torin2 is a highly potent and selective mTOR inhibitor. It is easier to produce than its lead compound Torin1 and displays improved pharmacokinetic properties. Torin2 is predicted to engage in hydrogen bonds with V2240 and Y2225 of a homology model of mTOR. It also form two hydrogen bonds between the aniline amino group of it with D2195 and D2357, making it more potent than Torin1. Besides that, Torin2 shows excellent overall selectivity and has strong binding to mTOR, CSNK1E, several PI3Ks, CSF1R and MKNK2. Torin2 exerts 800-fold cellular selectivity relative to inhibition of PI3K and other protein kinases. Moreover, Torin2 shows good bioavailability and exposure in vivo [1].
References:
[1] Liu Q, Wang J, Kang S A, et al. Discovery of 9-(6-Aminopyridin-3-yl)-1-(3-(trifluoromethyl) phenyl) benzo [h][1, 6] naphthyridin-2 (1 H)-one (Torin2) as a Potent, Selective, and Orally Available Mammalian Target of Rapamycin (mTOR) Inhibitor for Treatment of Cancer. Journal of medicinal chemistry, 2011, 54(5): 1473-1480.
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