INK 128 (MLN0128)

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 (vs Rapamycin). Phase 1.

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INK 128 (MLN0128) Chemical Structure

INK 128 (MLN0128) Chemical Structure
Molecular Weight: 309.33

Validation & Quality Control

Customer Reviews(2)

Quality Control & MSDS

Related Compound Libraries

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

mTOR Inhibitors with Unique Features

Product Information

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  • Research Area
  • Combination Therapy
    Combination Therapy

Product Description

Biological Activity

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 (vs Rapamycin). Phase 1.
Targets mTOR mTOR PI3Kα PI3Kγ PI3Kδ PI3Kβ
IC50 1 nM [1] 1.4 nM [3](Ki) 219 nM [3] 221 nM [3] 230 nM [3] 5293 nM [3]
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]
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(Only for Reference)



[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.

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Clinical Trial Information( data from

NCT Number Recruitment Conditions Sponsor
Start Date Phases
NCT01058707 Recruiting Advanced Solid Malignancies Millennium Pharmaceuticals, Inc. 2010-01 Phase 1
NCT01118689 Completed Relapsed Multiple Myeloma|Refractory Multiple Myeloma|Waldenstrom Macroglobulinemia Millennium Pharmaceuticals, Inc. 2010-11 Phase 1
NCT01351350 Active, not recruiting Advanced Solid Malignancies|Hematologic Malignancies Millennium Pharmaceuticals, Inc. 2011-03 Phase 1
NCT02133183 Not yet recruiting Adult Giant Cell Glioblastoma|Adult Glioblastoma|Adult Gliosarcoma|Recurrent Adult Brain Tumor National Cancer Institute (NCI) 2014-05

Chemical Information

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


CAS No. 1224844-38-5
Storage 3 years -20℃Powder
6 months-80℃in DMSO
Solubility (25°C) * In vitro DMSO 62 mg/mL (200 mM)
Water <1 mg/mL (<1 mM)
Ethanol 2 mg/mL (6 mM)
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

Research Area

Customer Reviews (2)

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Source Antonino Maria Spartà from University of Bologna. INK 128 (MLN0128) purchased from Selleck
Method Western Blot/MTT
Cell Lines Molt-4 leukemia cell
Concentrations 1.9 μM
Incubation Time 48 h
Results PI3K Inhibitor INK-128 was able to block Molt-4 leukemia cell line proliferation after 48 h with a measured IC50 of around 1.9 mM. Apoptosis induction assessed by western blot, demonstrated a limited cleavage of Caspase 7.

Click to enlarge
Source INK 128 (MLN0128) purchased from Selleck
Method ELISA
Cell Lines Bone marrow derived macrophages
Concentrations 1 nM
Incubation Time 1 h

Product Citations (2)

Tech Support & FAQs

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.

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