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

Sapanisertib (Synonyms: INK-128; MLN0128)

Cat. No.: HY-13328 Purity: 99.06%
Handling Instructions

Sapanisertib (INK-128) 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
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 106 In-stock
Estimated Time of Arrival: December 31
5 mg USD 96 In-stock
Estimated Time of Arrival: December 31
10 mg USD 120 In-stock
Estimated Time of Arrival: December 31
50 mg USD 300 In-stock
Estimated Time of Arrival: December 31
100 mg USD 540 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 13 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Sapanisertib purchased from MCE. Usage Cited in: Nat Commun. 2017 Jun 8;8:15617.

    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 MCE. Usage Cited in: J Virol. 2014 Oct;88(20):11872-85.

    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.

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

    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 MCE. Usage Cited in: Oncogene. 2015 Mar 26;34(13):1729-35.

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

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    Description

    Sapanisertib (INK-128) 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].

    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].

    Clinical Trial
    Molecular Weight

    309.33

    Formula

    C₁₅H₁₅N₇O

    CAS No.

    1224844-38-5

    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 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 83.3 mg/mL (269.29 mM)

    *"≥" means soluble, but saturation unknown.

    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: ≥ 2.5 mg/mL (8.08 mM); Clear solution

    • 2.

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

      Solubility: ≥ 2.5 mg/mL (8.08 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (8.08 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    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

    Purity: 99.06%

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    Sapanisertib
    Cat. No.:
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