Torin 2

Torin 2

Catalog Number:
L002370150APE
Mfr. No.:
APE-B1640
Price:
$294
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      • Overview
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          Background

          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].

          [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.

      • Properties
        • Alternative Name
          9-(6-aminopyridin-3-yl)-1-[3-(trifluoromethyl)phenyl]benzo[h][1,6]naphthyridin-2-one
          CAS Number
          1223001-51-1
          Molecular Formula
          C24H15F3N4O
          Molecular Weight
          432.41
          Appearance
          A solid
          Purity
          99.37%
          Solubility
          ≥21.6 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH
          Storage
          Store at -20°C

          * For Research Use Only

      • Reference
        • 1. Ming Liu, Jinyi Zhang, et al. "WAVE2 suppresses mTOR activation to maintain T cell homeostasis and prevent autoimmunity." Science. 2021 Mar 26;371(6536):eaaz4544. PMID:33766857
          2. Tariqul Islam AFM, Scavello M, et al. "Caffeine inhibits PI3K and mTORC2 in Dictyostelium and differentially affects multiple other cAMP chemoattractant signaling effectors." Mol Cell Biochem. 2019 Jul;457(1-2):157-168. PMID:30879206

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