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

INK-128 (Synonyms: Sapanisertib; MLN0128)

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

INK-128 is a potent and selective mTOR inhibitor with IC50 of 1 nM, > 200-fold less potent to class I PI3K isoforms, superior in blocking mTORC1/2 and sensitive to pro-invasion genes.

For research use only. We do not sell to patients.
INK-128 Chemical Structure

INK-128 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 $88 In-stock
5 mg $80 In-stock
10 mg $100 In-stock
50 mg $250 In-stock
100 mg $450 In-stock
200 mg   Get quote  
500 mg   Get quote  

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    INK-128 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.

    INK-128 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.

    INK-128 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.

    INK-128 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.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    INK-128 is a potent and selective mTOR inhibitor with IC50 of 1 nM, > 200-fold less potent to class I PI3K isoforms, superior in blocking mTORC1/2 and sensitive to pro-invasion genes.

    IC50 & Target

    IC50: 1 nM (mTOR)

    In Vitro

    INK-128 exhibits an enzymatic inhibition activity against mTOR and more than 100-fold selectivity to PI3K kinases[1]. INK128 selectively decreases the expression of YB1, MTA1, vimentin and CD44 at the protein but not transcript level in PC3 cells. INK128 decreases the invasive potential of PC3 prostate cancer cells. Furthermore, INK128 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, 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. INK128 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
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    References
    Preparing Stock Solutions
    Concentration Volume 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.
    Kinase Assay
    [2]

    mTOR activity is assayed using LanthaScreen Kinase kit reagents. PI(3)K α, β, γ and δ activity are assayed using the PI(3)K HTRF assay kit. The concentration of INK128 necessary to achieve inhibition of enzyme activity by 50% (IC50) is calculated using concentrations ranging from 20 μM to 0.1 nM (12-point curve). IC50 values are determined using a nonlinear regression model. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    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 INK128 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]

    INK128 is formulated in 5% polyvinylpropyline, 15% NMP, 80% water.

    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. INK128 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
    Molecular Weight

    309.33

    Formula

    C₁₅H₁₅N₇O

    CAS No.

    1224844-38-5

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    10 mM in DMSO

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

    Purity: 99.06%

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    Product Name:
    INK-128
    Cat. No.:
    HY-13328
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