2. PI3K/Akt/mTOR Autophagy
  3. mTOR Autophagy
  4. Sapanisertib

Sapanisertib  (Synonyms: INK-128; MLN0128; TAK-228)

Cat. No.: HY-13328 Purity: 99.64%
COA Handling Instructions

Molarity Calculator

Sapanisertib (INK-128; MLN0128; TAK-228) is an orally available, ATP-dependent mTOR1/2 inhibitor with an IC50 of 1 nM for mTOR kinase.

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

Sapanisertib Chemical Structure

Sapanisertib Chemical Structure

CAS No. : 1224844-38-5

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 106 In-stock
Solution
10 mM * 1 mL in DMSO USD 106 In-stock
Solid
1 mg USD 31 In-stock
5 mg USD 96 In-stock
10 mg USD 120 In-stock
50 mg USD 300 In-stock
100 mg USD 540 In-stock
200 mg   Get quote  
500 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 40 publication(s) in Google Scholar

Sapanisertib Related Antibodies

Top Publications Citing Use of Products

36 Publications Citing Use of MCE Sapanisertib

WB
IF

    Sapanisertib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2017 Jun 8;8:15617.  [Abstract]

    Immunoblot analysis of KRAS protein levels in parental (P) and resistant derivatives (R1 and R2) following 4 h treatment with the corresponding inhibitors Rapamycin, AZD2014, MLN0128, BEZ235 and 4EGI-1. Images are cropped for clarity from the same exposure of the same membrane.

    Sapanisertib purchased from MedChemExpress. Usage Cited in: Oncogene. 2015 Mar 26;34(13):1729-35.  [Abstract]

    INK-128 ablates phosphorylation of the mTORC1 substrates, 4E-BP1 and S6K.

    Sapanisertib purchased from MedChemExpress. Usage Cited in: J Virol. 2014 Oct;88(20):11872-85.  [Abstract]

    Confocal analysis of MTA1 (red) and β-catenin (green) expression in CNE-1-LMP2A cells treated with Rapamycin (50 nM) or INK-128 (200 nM) for 24 h. The scale bar represents 10 μm. Immunofluorescence analysis of MTA1 and β-catenin expression reveals that MTA1 is decreased and β-catenin is maintained in the cytoplasm when the cells are treated with INK-128.

    Sapanisertib purchased from MedChemExpress. Usage Cited in: J Virol. 2014 Oct;88(20):11872-85.  [Abstract]

    Representative Western blot from two independent experiments of p-Akt, p-mTOR, mTOR, p-4EBP1, 4EBP1, eIF4E, c-myc, and MTA1 genes in CNE-1-LMP2A cells treated with Rapamycin (50 nM) or INK-128 (200 nM) for 24 h. The quantification of the Western blot signals are analyzed.

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    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Sapanisertib (INK-128; MLN0128; TAK-228) is an orally available, ATP-dependent mTOR1/2 inhibitor with an IC50 of 1 nM for mTOR kinase.

    IC50 & Target[2]

    mTOR

    1 nM (IC50)

    mTORC1

     

    mTORC2

     

    PI3Kα

    219 nM (IC50)

    PI3Kγ

    221 nM (IC50)

    PI3Kδ

    230 nM (IC50)

    PI3Kβ

    5.293 μM (IC50)

    Autophagy

     

    In Vitro

    Sapanisertib (INK-128) exhibits an enzymatic inhibition activity against mTOR and more than 100-fold selectivity to PI3K kinases[1].
    Sapanisertib (INK-128) selectively decreases the expression of YB1, MTA1, vimentin and CD44 at the protein but not transcript level in PC3 cells. Sapanisertib (INK-128) decreases the invasive potential of PC3 prostate cancer cells. Furthermore, Sapanisertib (INK-128) inhibits cancer cell migration starting at 6 h of treatment, precisely correlating with when decreases in the expression of pro-invasion genes are evident, but preceding any changes in the cell cycle or overall global protein synthesis[2].

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

    Sapanisertib Related Antibodies
    In Vivo

    In a ZR-75-1 breast cancer xenograft model, Sapanisertib (INK-128) shows tumor growth inhibition efficacy at a dose of 0.3 mg/kg/day[1].
    4EBP1 and p70S6K1/2 phosphorylation is completely restored to wild-type levels after treatment with INK128 in PtenL/L mice. Sapanisertib (INK-128) treatment results in a 50% decrease in prostatic intraepithelial neoplasia (PIN) lesions in PtenL/L mice and induces programmed cell death in multiple cancer cell lines in mice[2].

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

    309.33

    Formula

    C15H15N7O
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    NC1=NC=NC2=C1C(C3=CC4=C(C=C3)OC(N)=N4)=NN2C(C)C
    Shipping

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

    DMSO : 55 mg/mL (177.80 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 3.2328 mL 16.1640 mL 32.3279 mL
    5 mM 0.6466 mL 3.2328 mL 6.4656 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
    =
    Concentration
    ×
    Volume
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    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    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: ≥ 2.08 mg/mL (6.72 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (6.72 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: 99.66%

    COA (256 KB) HNMR (266 KB) LCMS (97 KB)

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

    PC3 cells are treated with the appropriate drug for 48 h, and proliferation is measured using CellTiter-Glo Luminescent reagent. The concentration of Sapanisertib (INK-128) necessary to achieve inhibition of cell growth by 50% (IC50) is calculated using concentrations ranging from 20.0 μM to 0.1 nM (12-point curve).

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

    Nude mice are inoculated subcutaneously in the right subscapular region with 5×106 MDA-MB-361 cells. After tumours reach a size of 150-200 mm3, mice are randomLy assigned into vehicle control or treatment groups. Sapanisertib (INK-128) is formulated in 5% polyvinylpropyline, 15% NMP, 80% water and administered by oral gavage at 0.3 mg/kg and 1 mg/kg daily.

    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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 3.2328 mL 16.1640 mL 32.3279 mL 80.8198 mL
    5 mM 0.6466 mL 3.2328 mL 6.4656 mL 16.1640 mL
    10 mM 0.3233 mL 1.6164 mL 3.2328 mL 8.0820 mL
    15 mM 0.2155 mL 1.0776 mL 2.1552 mL 5.3880 mL
    20 mM 0.1616 mL 0.8082 mL 1.6164 mL 4.0410 mL
    25 mM 0.1293 mL 0.6466 mL 1.2931 mL 3.2328 mL
    30 mM 0.1078 mL 0.5388 mL 1.0776 mL 2.6940 mL
    40 mM 0.0808 mL 0.4041 mL 0.8082 mL 2.0205 mL
    50 mM 0.0647 mL 0.3233 mL 0.6466 mL 1.6164 mL
    60 mM 0.0539 mL 0.2694 mL 0.5388 mL 1.3470 mL
    80 mM 0.0404 mL 0.2020 mL 0.4041 mL 1.0102 mL
    100 mM 0.0323 mL 0.1616 mL 0.3233 mL 0.8082 mL
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    Sapanisertib 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:

    Sapanisertib1224844-38-5INK-128 MLN0128 TAK-228INK128INK 128MLN0128MLN 0128MLN-0128TAK228TAK 228TAK-228mTORAutophagyMammalian target of RapamycinInhibitorinhibitorinhibit

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