2. PI3K/Akt/mTOR Autophagy Apoptosis
  3. mTOR Autophagy Mitophagy Apoptosis
  4. Torkinib

Torkinib (PP242) est un inhibiteur de mTOR qui est sélectif et compétitif avec un IC50 de 8 nM. PP242 inhibe mTORC1 et mTORC2 avec des IC50s de 30 nM et 58 nM, respectivement.

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.

For research use only. We do not sell to patients.

Torkinib Chemical Structure

Torkinib Chemical Structure

CAS No. : 1092351-67-1

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 72 In-stock
Solution
10 mM * 1 mL in DMSO USD 72 In-stock
Solid
1 mg USD 31 In-stock
5 mg USD 66 In-stock
10 mg USD 86 In-stock
25 mg USD 158 In-stock
50 mg USD 220 In-stock
100 mg USD 350 In-stock
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Customer Review

Based on 22 publication(s) in Google Scholar

Torkinib Related Antibodies

Top Publications Citing Use of Products

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

    Total proteins in tumor tissues from nude mice were extracted and the expressions of RICTOR, p-AKT (Ser473), AKT, p-PRAS40 (Thr246), PRAS40, p-p70S6K (Thr389) and p70S6K were evaluated by Western blot (n=5). Values represent the mean±SD.

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

    ECa109 cells stably transfected with control shRNA or RICTOR shRNA were treated with RAD001 (10 μmol/L) or 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).

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    mTOR mTORC1 mTORC2

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    Description

    Torkinib (PP 242) is a selective and ATP-competitive mTOR inhibitor with an IC50 of 8 nM[1]. PP242 inhibits both mTORC1 and mTORC2 with IC50s of 30 nM and 58 nM, respectively[2].

    IC50 & Target[1][2]

    mTOR

    8 nM (IC50)

    mTORC1

    30 nM (IC50)

    mTORC2

    58 nM (IC50)

    p110δ

    100 nM (IC50)

    PDGFR

    410 nM (IC50)

    DNA-PK

    410 nM (IC50)

    p110γ

    1.3 μM (IC50)

    p110α

    2 μM (IC50)

    p110β

    2.2 μM (IC50)

    Hck

    1.2 μM (IC50)

    Scr

    1.4 μM (IC50)

    VEGFR2

    1.5 μM (IC50)

    Abl

    3.6 μM (IC50)

    EphB4

    3.4 μM (IC50)

    EGFR

    4.4 μM (IC50)

    Scr(T338I)

    5.1 μM (IC50)

    Autophagy

     

    Mitophagy

     

    In Vitro

    Torkinib (PP 242) potently inhibits mTOR (IC50=8 nM) but is much less active against other PI3K family members. Testing of Torkinib (PP 242) against 219 protein kinases reveals remarkable selectivity relative to the protein kinome: at a concentration 100-fold above its IC50 for mTOR, Torkinib (PP 242) inhibits only one kinase by more than 90% (Ret) and only three by more than 75% (PKCα, PKCβII and JAK2V617F)[1]. Torkinib (PP 242) has a dose-dependent effect on proliferation and at higher doses is much more effective than Rapamycin at blocking cell proliferation. The ability of Torkinib (PP 242) to block cell proliferation more efficiently than Rapamycin could be a result of its ability to inhibit mTORC1 and mTORC2, because Rapamycin can only inhibit mTORC1. In SIN1-/- mouse embryonic fibroblasts (MEFs), Rapamycin is also less effective at blocking cell proliferation than Torkinib. That Torkinib (PP 242) and Rapamycin exhibit very different anti-proliferative effects in SIN1-/- MEFs suggests that the two compounds differentially affect mTORC1[2].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Torkinib Related Antibodies
    In Vivo

    In fat and liver, Torkinib (PP 242) is able to completely inhibit the phosphorylation of Akt at S473 and T308, consistent with its effect on these phosphorylation sites observed in cell culture. Surprisingly, Torkinib (PP 242) is only partially able to inhibit the phosphorylation of Akt in skeletal muscle and is more effective at inhibiting the phosphorylation of T308 than S473, despite it's ability to fully inhibit the phosphorylation of 4EBP1 and S6. These results will be confirmed by in vivo dose-response experiments, but, consistent with the partial effect of Torkinib (PP 242) on pAkt in skeletal muscle, a muscle-specific knockout of the integral mTORC2 component rictor resulted in only a partial loss of Akt phosphorylation at S473. These results suggest that a kinase other than mTOR, such as DNA-PK, may contribute to phosphorylation of Akt in muscle[2].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    Molecular Weight

    308.34

    Formula

    C16H16N6O
    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    NC1=C2C(N(N=C2C3=CC4=C(N3)C=CC(O)=C4)C(C)C)=NC=N1
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    Solvent & Solubility
    In Vitro: 

    DMSO : 50 mg/mL (162.16 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.2432 mL 16.2159 mL 32.4317 mL
    5 mM 0.6486 mL 3.2432 mL 6.4863 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    Volume (start)

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (8.11 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (8.11 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 98.37%

    COA (253 KB) LCMS (270 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay
    [2]

    Wild-type and SIN1-/- MEFs are plated in 96-well plates at approximately 30% confluence and left overnight to adhere. The following day cells are treated with Torkinib (PP 242) (1 nM, 10 nM, 100 nM, 1 μM, and 10 μM), Rapamycin, or vehicle (0.1% DMSO). After 72 h of treatment, 10 μL of 440 μM resazurin sodium salt is added to each well, and after 18 h, the florescence intensity in each well is measured using a top-reading florescent plate reader with excitation at 530 nm and emission at 590 nm[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [2]

    Mice[2]
    Six-wk-old male C57BL/6 mice are fasted overnight prior to drug treatment. Torkinib (PP 242) (0.4 mg), Rapamycin (0.1 mg), or vehicle alone is injected IP. After 30 min for the Rapamycin-treated mouse or 10 min for the Torkinib (PP 242) and vehicle-treated mice, 250 mU of insulin in 100 μL of saline is injected IP. 15 min after the insulin injection, the mice are killed by CO2 asphyxiation followed by cervical dislocation. Tissues are harvested and frozen on liquid nitrogen in 200 μL of cap lysis buffer. The frozen tissue is thawed on ice, manually disrupted with a mortar and pestle, and then further processed with a micro tissue-homogenizer. Protein concentration of the cleared lysate is measured by Bradford assay and 5-10 μg of protein is analyzed by Western blot[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 3.2432 mL 16.2159 mL 32.4317 mL 81.0793 mL
    5 mM 0.6486 mL 3.2432 mL 6.4863 mL 16.2159 mL
    10 mM 0.3243 mL 1.6216 mL 3.2432 mL 8.1079 mL
    15 mM 0.2162 mL 1.0811 mL 2.1621 mL 5.4053 mL
    20 mM 0.1622 mL 0.8108 mL 1.6216 mL 4.0540 mL
    25 mM 0.1297 mL 0.6486 mL 1.2973 mL 3.2432 mL
    30 mM 0.1081 mL 0.5405 mL 1.0811 mL 2.7026 mL
    40 mM 0.0811 mL 0.4054 mL 0.8108 mL 2.0270 mL
    50 mM 0.0649 mL 0.3243 mL 0.6486 mL 1.6216 mL
    60 mM 0.0541 mL 0.2703 mL 0.5405 mL 1.3513 mL
    80 mM 0.0405 mL 0.2027 mL 0.4054 mL 1.0135 mL
    100 mM 0.0324 mL 0.1622 mL 0.3243 mL 0.8108 mL
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    Torkinib Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Torkinib1092351-67-1PP 242PP242PP-242mTORAutophagyMitophagyApoptosisMammalian target of RapamycinMitochondrial AutophagyInhibitorinhibitorinhibit

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