T-8448 Torin 2, Free Base, >99%

Synonyms : [mTOR Inhibitor XII]

  • Size
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  • 5 mg
  • 69
  • 65
  • 56
  • 10,300
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  • 10 mg
  • 96
  • 90
  • 78
  • 14,300
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  • 25 mg
  • 198
  • 186
  • 162
  • 29,500
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  • 50 mg
  • 315
  • 297
  • 258
  • 46,900
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  • 100 mg
  • 543
  • 512
  • 445
  • 80,800
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  • 250 mg
  • 830
  • 782
  • 680
  • 123,600
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  • M.W. 432.40
  • C24H15F3N4O
  • [1223001-51-1]

Storage: Store at or below -20 ºC. Solubility: Soluble in DMSO. Disposal: A.

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  • Torin 2 is a highly potent and selective ATP-competitive mammalian target of rapamycin (mTOR) kinase inhibitor. Torin 2 inhibited cellular mTOR activity with an IC50 of 0.25 nM and exhibited 800-fold selectivity over PI3K (IC50 = 200 nM) and over 100-fold binding selectivity over 440 other protein kinases. Liu Q., et al. "Discovery of 9-(6-aminopyridin-3-yl)-1-(3-(trifluoromethyl)phenyl)benzo[h][1,6]naphthyridin-2(1H)-one (Torin2) as a potent, selective, and orally available mammalian target of rapamycin (mTOR) inhibitor for treatment of cancer." J. Med. Chem. 54: 1473-1480 (2011).
  • In addition to mTOR, torin 2 also exhibited potent biochemical and cellular activity against phosphatidylinositol-3 kinase-like (PI3K-like) kinase family kinases including ATM (IC50 = 28 nM), ATR (IC50 = 35 nM), and DNA-PK (IC50 = 118 nM), the inhibition of which sensitized cells to irradiation. Treatment with torin 2 for 24 hours resulted in strong growth inhibition of cancer cells in vitro. Single-agent treatment with torin 2 in vivo did not show significant efficacy against KRAS-driven lung tumors, but the combination of torin 2 with mitogen-activated protein/extracellular signal-regulated kinase inhibitor AZD6244 (selumetinib, please see Cat. No. S-4490, Selumetinib, Free Base) demonstrated a significant growth inhibition. Liu Q., et al. "Characterization of Torin2, an ATP-competitive inhibitor of mTOR, ATM, and ATR." Cancer Res. 73: 2574-2586 (2013).
  • Torin 1 and torin 2 are potent antimalarials. Hanson K.K., et al. "Torins are potent antimalarials that block replenishment of Plasmodium liver stage parasitophorous vacuole membrane proteins." Proc. Natl. Acad. Sci. USA 110: E2838-E2847 (2013).
  • Sold for laboratory or manufacturing purposes only; not for human, veterinary, food, or household use.
  • This product is offered for R&D use in accordance with (i) 35 USC 271(e)+A13(1) in the U.S.; (ii) Section 69.1 of Japanese Patent Law in Japan; (iii) Section 11, No. 2 of the German Patent Act of 1981 in Germany; (iv) Section 60, Paragraph 5b of the U.K. Patents Act of 1977 in the U.K.; (v) Sections 55.2(1) and 55.2(6) and other common law exemptions of Canadian patent law; (vi) Section 68B of the Patents Act of 1953 in New Zealand together with the amendment of same by the Statutes Amendment Bill of 2002; (vii) such related legislation and/or case law as may be or become applicable in the aforementioned countries; and (viii) such similar laws and rules as may apply in various other countries.
  • Not available in some countries; not available to some institutions; not available for some uses.
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