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

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

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Solid + Solvent
10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 106 In-stock
Solid
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10 mg USD 120 In-stock
50 mg USD 300 In-stock
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Customer Review

Based on 32 publication(s) in Google Scholar

Sapanisertib Related Antibodies

Top Publications Citing Use of Products

    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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    • References

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    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

    Appearance

    Solid

    Formula

    C15H15N7O
    CAS No.
    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)

    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
    10 mM 0.3233 mL 1.6164 mL 3.2328 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 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

    • 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

    • 3.

      Add each solvent one by one:  10% DMSO    90% Corn Oil

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

    *All of the co-solvents are available by MedChemExpress (MCE).
    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
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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.

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    Keywords:

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

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