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

INK-128 (Synonyms: Sapanisertib; MLN0128)

Cat. No.: HY-13328 Purity: 99.55%
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   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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Top Publications Citing Use of Products
  • 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
Sponsor Condition Start Date Phase
Millennium Pharmaceuticals Inc Advanced solid tumor 2013-07-31 Phase 1
Millennium Pharmaceuticals Inc Advanced solid tumor 2011-03-31 Phase 1
Millennium Pharmaceuticals Inc Macroglobulinemia 2010-11-30 Phase 1
Millennium Pharmaceuticals Inc Non-Hodgkin lymphoma 2010-11-30 Phase 1
Millennium Pharmaceuticals Inc Multiple myeloma 2010-11-30 Phase 1
Millennium Pharmaceuticals Inc Advanced solid tumor 2010-01-31 Phase 1
References
Preparing Stock Solutions
Concentration Volume (DMSO) 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
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.

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).

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.

References
M.Wt

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

Purity: 99.55%

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