INK 128 (MLN0128)

Catalog No.S2811

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.

Price Stock Quantity  
USD 221 In stock
USD 170 In stock
USD 270 In stock
USD 970 In stock
Bulk Inquiry

Massive Discount Available

Free Overnight Delivery on all orders over $ 500.

INK 128 (MLN0128) Chemical Structure

INK 128 (MLN0128) Chemical Structure
Molecular Weight: 309.33

Validation & Quality Control

3 customer reviews :

Quality Control & MSDS

Related Compound Libraries

INK 128 (MLN0128) is available in the following compound libraries:

mTOR Inhibitors with Unique Features

Product Information

  • Compare mTOR Inhibitors
    Compare mTOR Products
  • Research Area
  • Inhibition Profile
  • Combination Therapy
    Combination Therapy

Product Description

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)

 View  More

IC50 1.4 nM(Ki) 1.4 nM(Ki) 219 nM 221 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 LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
PANC-1 M3vtTWNmdGxiVnnhZoltcXS7IFHzd4F6MYqxMVExOCCwTR?=NEfXRmY4OiCqNHjITINqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7NIL4ZVMzPDl5MUW0OC=>
PANC-1 NHHQNG5E\WyuIG\pZYJqdGm2eTDBd5NigQ>?MVK1NEBvVQ>?M360WVI1NTl4IHi=M4DD[4lvcGmkaYTzJINmdGxidnnhZoltcXS7IITpcYUh\GWyZX7k[Y51dHl?NIXqXo4zPDl5MUW0OC=>
MIA PaCa-2MXvD[YxtKF[rYXLpcIl1gSCDc4PhfS=>NH;rUWMyNTFyMDDuUS=>NIXOdXI4OiCqM4HoW4lvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl?M{XXUVI1QTdzNUS0
PANC-1 MWHBdI9xfG:|aYOgRZN{[Xl?M{DST|ExNTFyMDDuUS=>M3;6U|czKGh?NISzR4FqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5M3;xdlI1QTdzNUS0
PANC-1 NEf2NIVHfW6ldHnvckBCe3OjeR?=MnnINVAwPTBibl2=Mn3TNlQhcA>?MX;kdoFu[XSrY3HscJkhcW6qaXLpeJMheGixc4Doc5J6dGG2aX;uJI9nKDSHLVLQNU1UPktzIDjtWG9TSzFiYXP0bZZifGmxbjDpcoRq[2G2b4LzLUBidmRiQXv0JIF1KFOncjC0O|MhMHSqZTDtWG9TSzJiYXP0bZZifGmxbjDpcoRq[2G2b4KpMVmyOFk4OTV2NB?=
PANC-1 MYDGeY5kfGmxbjDBd5NigQ>?NWXzW5B4PTBibl2=M2TDXVQ5KGh?MVfkbZNzfXC2czDj[YxtKGO7Y3zlJJBzd2e{ZYPzbY9vMmniNlQ6PzF3NES=
PANC-1 MmOxSpVv[3Srb36gRZN{[Xl?MmOxNVAhdk1?Mor2O|IhcA>?NXjLelVWcW6lcnXhd4V{KGenbXPpeIFjcW6nIIPlcpNqfGm4aYT5MoDxNlQ6PzF3NES=

... 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]

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)
Body Surface Area (m2)0.0070.0250.
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)


[1] Liu A, et al. Drug Discovery Today: Therapeutic Strategies. 2009, 6(2), 47-55.

[2] Jessen K, et al. Mol Cancer Ther. 2009, 8(12), Meeting Abstract Supplement.

view more

Clinical Trial Information( data from, updated on 2016-07-30)

NCT Number Recruitment Conditions Sponsor
Start Date Phases
NCT02575339 Recruiting Hepatocellular Carcinoma|Liver Cancer|HCC Bert ONeil, MD|Hoosier Cancer Research Network|Millennium  ...more Bert ONeil, MD|Hoosier Cancer Research Network|Millennium Pharmaceuticals, Inc.|Big Ten Cancer Research Consortium July 2016 Phase 1|Phase 2
NCT02756364 Not yet recruiting Breast Neoplasms Millennium Pharmaceuticals, Inc. June 2016 Phase 2
NCT02725268 Recruiting Endometrial Neoplasms Millennium Pharmaceuticals, Inc.|European Network of Tran  ...more Millennium Pharmaceuticals, Inc.|European Network of Translational Research in Ovarian Cancer - EUTROC|European Network of Individualized Treatment in Endometrial Cancer - ENITEC June 2016 Phase 2
NCT02724020 Recruiting Clear-cell Metastatic Renal Cell Carcinoma Millennium Pharmaceuticals, Inc. June 2016 Phase 2
NCT02719691 Recruiting Metastatic Breast Cancer|Solid Tumors University of Colorado, Denver May 2016 Phase 1

view more

Chemical Information

Download INK 128 (MLN0128) SDF
Molecular Weight (MW) 309.33


CAS No. 1224844-38-5
Storage 3 years -20℃powder
2 years -80℃in solvent
Synonyms N/A
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 Name 3-(2-aminobenzo[d]oxazol-5-yl)-1-isopropyl-1H-pyrazolo[3,4-d]pyrimidin-4-amine

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.

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.

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

If you have any other enquiries, please leave a message.

* Indicates a Required Field

Related mTOR Products

  • MHY1485

    MHY1485 is a potent, and cell-permeable mTOR activator, and also potently inhibits autophagy.

  • CHIR-99021 (CT99021)

    CHIR-99021 (CT99021) is a GSK-3α and GSK-3β inhibitor with IC50 of 10 nM and 6.7 nM, respectively.

  • Dorsomorphin

    Dorsomorphin is a potent, reversible, selective AMPK inhibitor with Ki of 109 nM in cell-free assays, exhibiting no significant inhibition of several structurally related kinases including ZAPK, SYK, PKCθ, PKA, and JAK3. Also inhibits type I BMP receptor activity.

  • Rapamycin (Sirolimus)

    Rapamycin (Sirolimus) is a specific mTOR inhibitor with IC50 of ~0.1 nM HEK293 cells.

  • Everolimus (RAD001)

    Everolimus (RAD001) is an mTOR inhibitor of FKBP12 with IC50 of 1.6-2.4 nM in a cell-free assay.

  • AZD8055

    AZD8055 is a novel ATP-competitive mTOR inhibitor with IC50 of 0.8 nM in MDA-MB-468 cells with excellent selectivity (∼1,000-fold) against PI3K isoforms and ATM/DNA-PK. Phase 1.

    Features:First drug to inhibit both types of mTOR protein.

  • Torin 1

    Torin 1 is a potent inhibitor of mTORC1/2 with IC50 of 2 nM/10 nM in cell-free assays; exhibits 1000-fold selectivity for mTOR than PI3K.

  • Temsirolimus (CCI-779, NSC 683864)

    Temsirolimus (CCI-779, NSC 683864) is a specific mTOR inhibitor with IC50 of 1.76 μM in a cell-free assay.

  • Tacrolimus (FK506)

    Tacrolimus (FK506) is a 23-membered macrolide lactone, it reduces peptidyl-prolyl isomerase activity in T cells by binding to the immunophilin FKBP12 (FK506 binding protein) creating a new complex.

  • KU-0063794

    KU-0063794 is a potent and highly specific dual-mTOR inhibitor of mTORC1 and mTORC2 with IC50 of ~10 nM in cell-free assays; no effect on PI3Ks.

Recently Viewed Items

Tags: buy INK 128 (MLN0128) | INK 128 (MLN0128) supplier | purchase INK 128 (MLN0128) | INK 128 (MLN0128) cost | INK 128 (MLN0128) manufacturer | order INK 128 (MLN0128) | INK 128 (MLN0128) distributor
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Contact Us