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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2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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.
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  NUWwT4VrS2WubDDWbYFjcWyrdImgRZN{[Xl? NWnUNHJZOS1zMECgcm0> NH;vPVA4OiCq M1LOVYlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? NFP5UJUzPDl5MUW0OC=>
PANC-1  NWL1d25ES2WubDDWbYFjcWyrdImgRZN{[Xl? M4DQXlUxKG6P MX2yOE06PiCq NH;UUVlqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTD0bY1mKGSncHXu[IVvfGy7 NVu2b21JOjR7N{G1OFQ>
MIA PaCa-2 NUXSe4tqS2WubDDWbYFjcWyrdImgRZN{[Xl? Mnn1NU0yODBibl2= MV63NkBp Mni2bY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? MmHSNlQ6PzF3NES=
PANC-1  MlLPRZBweHSxc3nzJGF{e2G7 MXixNE0yODBibl2= MW[3NkBp NHq0SXFqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 MmjGNlQ6PzF3NES=
PANC-1  M4PFWmZ2dmO2aX;uJGF{e2G7 Mn;ENVAwPTBibl2= NI\LXmIzPCCq Mk\O[JJidWG2aXPhcIx6KGmwaHnibZR{KHCqb4PwbI9zgWyjdHnvckBw\iB2RT3CVFEuWz[NMTCocXRQWkNzIHHjeIl3[XSrb36gbY5lcWOjdH;yd{kh[W6mIFHreEBifCCVZYKgOFc{KCi2aHWgcXRQWkN{IHHjeIl3[XSrb36gbY5lcWOjdH;yLS=> MXKyOFk4OTV2NB?=
PANC-1  NVuxcoJyTnWwY4Tpc44hSXO|YYm= NWHScm57PTBibl2= NVTKUYwyPDhiaB?= MYfkbZNzfXC2czDj[YxtKGO7Y3zlJJBzd2e{ZYPzbY9v NXXOfXJOOjR7N{G1OFQ>
PANC-1  MV;GeY5kfGmxbjDBd5NigQ>? NGHs[FIyOCCwTR?= M1zQbVczKGh? MlLKbY5kemWjc3XzJIdmdWOrdHHibY5mKHOnboPpeIl3cXS7 MVuyOFk4OTV2NB?=

... 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]


Solubility (25°C)

In vitro DMSO 62 mg/mL (200.43 mM)
Ethanol 2 mg/mL (6.46 mM)
Water <1 mg/mL
In vivo 30% PEG400+0.5% Tween80+5% propylene glycol 30 mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* 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


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

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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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID