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Torkinib

(Synonyms: PP 242)
30 Cited Publications
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Based on 30 publication(s) in Google Scholar

Torkinib (PP 242) is a selective and ATP-competitive mTOR inhibitor with an IC50 of 8 nM. PP242 inhibits both mTORC1 and mTORC2 with IC50s of 30 nM and 58 nM, respectively.

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  • Pureté: 99.03%
  • CAS No.: 1092351-67-1
  • Formule: C16H16N6O
  • Masse moléculaire:308.34
  • Stockage:
    Powder   -20°C, 3 years , 4°C, 2 years ; In solvent   -80°C, 1 year , -20°C, 6 months
  • Torkinib Chemical Structure
    Torkinib Chemical Structure
  • Experimental Validation Results for Torkinib
  • Experimental Validation Results for Torkinib
  • Experimental Validation Results for Torkinib
  • Experimental Validation Results for Torkinib
  • Experimental Validation Results for Torkinib
  • Experimental Validation Results for Torkinib
  • Experimental Validation Results for Torkinib
  • Experimental Validation Results for Torkinib
CAS No.: 1092351-67-1
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  • Torkinib Chemical Structure
    Torkinib Chemical Structure
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    Torkinib purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2020 Jun;10(6):1004-1019. [Abstract]

    Customer Validation
     ECa109 cells stably transfected with control shRNA or RICTOR shRNA were treated with RAD001 (10 μmol/L) or Torkinib (PP242, 2 μmol/L) for 48 h, and total proteins were extracted to analysis the expression of RICTOR, p-AKT (Ser473), AKT, p-PRAS40 (Thr246), PRAS40, p-p70S6K and p70S6K by Western blot (n=5).

  • 1/16

    Torkinib purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2020 Jun;10(6):1004-1019. [Abstract]

    Customer Validation
     ECa109 and EC9706 cells were treated with Torkinib (PP242) for 24 or 48 h, respectively, and the cell viability was assessed by CCK-8 assay (n = 5).

  • 1/16

    Torkinib purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2020 Jun;10(6):1004-1019. [Abstract]

    Customer Validation
     After ECa109 and EC9706 cells were treated with Torkinib (PP242) (0, 1 and 4 μmol/L) for 24 h or at the same concentration (4 μmol/L of PP242) for different time, total proteins were extracted to analyze the expression of p-AKT (Ser473), AKT, p-p70S6K and p70S6K by Western blot (n = 5). The results showed that PP242 decreased the expression of p-AKT (Ser473) and p-p70S6K (Thr389) in dose- and time-dependent manners.

  • 1/16

    Torkinib purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2020 Jun;10(6):1004-1019. [Abstract]

    Customer Validation
     ECa109 RICTOR-KD cells or control cells were treated with RAD001 (10 μmol/L) or Torkinib (PP242) (2 μmol/L) for 48 h, and then the cell migration was assessed by transwell migration assay (n = 3). Scale bar = 100 μm.

  • 1/16

    Torkinib purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2020 Jun;10(6):1004-1019. [Abstract]

    Customer Validation
     ECa109 RICTOR-KD cells or control cells were treated with RAD001 (20 μmol/L) or Torkinib (PP242) (4 μmol/L) for 48 h, and then cell apoptosis was assessed by flow cytometry (n = 3).

  • 1/16

    Torkinib purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2020 Jun;10(6):1004-1019. [Abstract]

    Customer Validation
     ECa109 RICTOR-KD cells or control cells were treated with RAD001 (10 μmol/L) or PP242 (2 μmol/L ) for 48 h, and then the cell cycle were assessed by flow cytometer (n = 3).

  • 1/16

    Torkinib purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2020 Jun;10(6):1004-1019. [Abstract]

    Customer Validation
     Stable knockdown of RICTOR inhibited tumor growth and potentiated the antitumor effect of Torkinib (PP242) in nude mice. Nude mice bearing tumors derived from ECa109 RICTOR-KD cells or control cells were treated by Torkinib (PP242) (5 mg/kg every other day, i.p.) for 14 days (n = 5). Tumor growth curves were graphed with the tumor volume of each mouse measured and recorded every day (n = 5).

  • 1/16

    Torkinib purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2020 Jun;10(6):1004-1019. [Abstract]

    Customer Validation
     Nude mice bearing tumors derived from ECa109 RICTOR-KD cells or control cells were treated by Torkinib (PP242) (5 mg/kg every other day, i.p.) for 14 days (n = 5). Paraffin-embedded tumor was used to analyze the cell apoptosis as well as livers and kidneys of mice were used to evaluate the potential hepatorenal toxicity by H&E staining (n = 5). Scale bar = 100 μm.

  • Torkinib