INK 128 (MLN0128)

Catalog No.S2811

INK 128 (MLN0128) Chemical Structure

Molecular Weight(MW): 309.33

INK 128 (MLN0128) is a potent and selective mTOR inhibitor with IC50 of 1 nM in cell-free assays; >200-fold less potent to class I PI3K isoforms, superior in blocking mTORC1/2 and sensitive to pro-invasion genes (vs Rapamycin). Phase 1.

Size Price Stock Quantity  
In DMSO USD 221 In stock
USD 170 In stock
USD 270 In stock
USD 970 In stock
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3 Customer Reviews

  • Hep-2 (D) or SCC-9 (E) cells were treated with PI3K/Akt and mTOR dual inhibitor LY 294002 (LY, 1 umol/L), mTORC1 inhibitor rapamycin (0.5 umol/L), mTORC1/2 dual inhibitor AZD2014 (0.1 uM), INK-128 (0.1 uM) or AZD8055 (0.1 uM) for 72 h, cell viability was analyzed. The mean of three independent experiments performed in triplicate was shown. Statistical significance was analyzed by ANOVA. *p < 0.01 vs Control. **p < 0.01 vs. AZD8055 group.

    Biochem Biophys Res Commun 2013 440(4), 701-6. INK 128 (MLN0128) purchased from Selleck.

    Antonino Maria Spart from University of Bologn. INK 128 (MLN0128) purchased from Selleck.

  •  

    Bone marrow derived macrophages were pre-treated with 1nM INK128 for 1h prior to LPS treatment (100 ng/ml).  TNF-a production was analyzed 24h later. 

    INK 128 (MLN0128) purchased from Selleck.

Purity & Quality Control

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Biological Activity

Description INK 128 (MLN0128) is a potent and selective mTOR inhibitor with IC50 of 1 nM in cell-free assays; >200-fold less potent to class I PI3K isoforms, superior in blocking mTORC1/2 and sensitive to pro-invasion genes (vs Rapamycin). Phase 1.
Targets
mTOR [3]
(Cell-free assay)
mTOR [3]
(Cell-free assay)
PI3Kα [3]
(Cell-free assay)
PI3Kγ [3]
(Cell-free assay)
PI3Kδ [3]
(Cell-free assay)
1.4 nM(Ki) 1.4 nM(Ki) 219 nM 221 nM 230 nM
In vitro

INK 128 exhibits an enzymatic inhibition activity against mTOR and more than 100-fold selectivity to PI3K kinases. [1] As TORC1/2 inhibitor, INK 128 inhibits both the phosphorylation of S6 and 4EBP1, the downstream substrates of TORC1, and selectively inhibits AKT phosphorylation at Ser473, the downstream substrate of TORC2. Furthermore, INK 128 also shows potent inhibition effects on cell lines resistant to rapamycin and pan-PI3K inhibitors. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
PANC-1  NWfxT2FZS2WubDDWbYFjcWyrdImgRZN{[Xl? NIHWPZQyNTFyMDDuUS=> MVe3NkBp MnjCbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? Mn[wNlQ6PzF3NES=
PANC-1  NVSzT3ZTS2WubDDWbYFjcWyrdImgRZN{[Xl? NVjofmpPPTBibl2= M1;ZXFI1NTl4IHi= MUPpcohq[mm2czDj[YxtKH[rYXLpcIl1gSC2aX3lJIRmeGWwZHXueIx6 NFrlc|czPDl5MUW0OC=>
MIA PaCa-2 M{OxSmNmdGxiVnnhZoltcXS7IFHzd4F6 MYqxMVExOCCwTR?= M4PvclczKGh? MojvbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? MlTiNlQ6PzF3NES=
PANC-1  M323RWFxd3C2b4Ppd{BCe3OjeR?= M{S3UFExNTFyMDDuUS=> M3LQflczKGh? M{PjTYlv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm= M{\G[|I1QTdzNUS0
PANC-1  M4HvNmZ2dmO2aX;uJGF{e2G7 MWOxNE82OCCwTR?= M4\LbFI1KGh? NVPyOZB[\HKjbXH0bYNidGy7IHnubIljcXS|IIDoc5NxcG:{eXzheIlwdiCxZjC0SU1DWDFvU{\LNUApdVSRUlOxJIFkfGm4YYTpc44hcW6maXPheI9zeyliYX7kJGFsfCCjdDDT[ZIhPDd|IDj0bIUhdVSRUlOyJIFkfGm4YYTpc44hcW6maXPheI9zMQ>? NV;0U5ZVOjR7N{G1OFQ>
PANC-1  MX\GeY5kfGmxbjDBd5NigQ>? NYKyUYFPPTBibl2= MUi0PEBp MoDh[Il{enWydIOgZ4VtdCCleXPs[UBxem:pcnXzd4lwdg>? MoTPNlQ6PzF3NES=
PANC-1  NVv4ZVFiTnWwY4Tpc44hSXO|YYm= NYPwOIQyOTBibl2= MmfkO|IhcA>? M3z5e4lv[3KnYYPld{Bo\W2laYThZolv\SC|ZX7zbZRqfmm2eR?= NITxWmkzPDl5MUW0OC=>

... Click to View More Cell Line Experimental Data

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] Daily, oral administration of INK 128 inhibits angiogenesis and tumor growth in multiplexenograft models. [2]

Protocol

Solubility (25°C)

In vitro DMSO 62 mg/mL (200.43 mM)
Ethanol 2 mg/mL (6.46 mM)
Water Insoluble
In vivo Add solvents individually and in order:
30% PEG400+0.5% Tween80+5% propylene glycol
30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 309.33
Formula

C15H15N7O

CAS No. 1224844-38-5
Storage powder
Synonyms N/A

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

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

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

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Molecular Weight Calculator

Molecular Weight Calculator

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Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
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Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02724020 Recruiting Clear-cell Metastatic Renal Cell Carcinoma Millennium Pharmaceuticals, Inc.|Takeda September 2016 Phase 2
NCT02575339 Recruiting Hepatocellular Carcinoma|Liver Cancer|HCC Bert ONeil, MD|Hoosier Cancer Research Network|Millennium Pharmaceuticals, Inc.|Big Ten Cancer Research Consortium July 2016 Phase 1|Phase 2
NCT02756364 Recruiting Breast Neoplasms Millennium Pharmaceuticals, Inc.|Takeda June 2016 Phase 2
NCT02725268 Recruiting Endometrial Neoplasms Millennium Pharmaceuticals, Inc.|European Network of Translational Research in Ovarian Cancer - EUTROC|European Network of Individualized Treatment in Endometrial Cancer - ENITEC|Takeda June 2016 Phase 2
NCT02719691 Recruiting Metastatic Breast Cancer|Solid Tumors University of Colorado, Denver May 2016 Phase 1
NCT02514824 Recruiting Merkel Cell Carcinoma Dana-Farber Cancer Institute|Millennium Pharmaceuticals, Inc. October 2015 Phase 1|Phase 2

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Frequently Asked Questions

  • Question 1:

    What is the recommendation method to formulate S2811 INK 128 (MLN0128) for oral administration?

  • Answer:

    You can try this vehicle for oral administration: 30% PEG400+0.5% Tween80 +5% Propylene glycol.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID