INK 128 (MLN0128)

Catalog No.S2811
5 5 3 Product Use Citation

INK 128 (MLN0128) 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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In DMSO USD 221 In stock
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INK 128 (MLN0128) Chemical Structure

INK 128 (MLN0128) Chemical Structure
Molecular Weight: 309.33

Validation & Quality Control

Customer Product Validation(3)

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
  • 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; >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 [1] mTOR [3] PI3Kα [3] PI3Kγ [3] PI3Kδ [3] PI3Kβ [3]
IC50 1 nM 1.4 nM(Ki) 219 nM 221 nM 230 nM 5293 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]
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]
Features

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

SpeciesBaboonDogMonkeyRabbitGuinea pigRatHamsterMouse
Weight (kg)121031.80.40.150.080.02
Body Surface Area (m2)0.60.50.240.150.050.0250.020.007
Km factor202012128653
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

References

[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 http://clinicaltrials.gov, updated on 2015-04-11)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02412722 Recruiting Non-Hematologic Malignancy Millennium Pharmaceuticals, Inc. March 2015 Phase 1
NCT02327169 Recruiting Advanced Nonhematologic Malignancies Millennium Pharmaceuticals, Inc. February 2015 Phase 1
NCT02244463 Not yet recruiting Anaplastic Thyroid Cancer|Thyroid Cancer Dana-Farber Cancer Institute|Millennium Pharmaceuticals,  ...more Dana-Farber Cancer Institute|Millennium Pharmaceuticals, Inc. October 2014 Phase 2
NCT02197572 Recruiting Advanced Solid Tumors Millennium Pharmaceuticals, Inc. September 2014 Phase 1
NCT02159989 Suspended Adult Solid Neoplasm|Gastrin-Producing Neuroendocrine Tumor|Pancreatic Glucagonoma|Pancreatic Insulinoma|Pancreatic Polypeptide Tumor|Recurrent Ova  ...more Adult Solid Neoplasm|Gastrin-Producing Neuroendocrine Tumor|Pancreatic Glucagonoma|Pancreatic Insulinoma|Pancreatic Polypeptide Tumor|Recurrent Ovarian Carcinoma|Recurrent Ovarian Germ Cell Tumor|Recurrent Pancreatic Neuroendocrine Carcinoma|Somatostatin-Producing Neuroendocrine Tumor|Stage IIIA Ovarian Cancer|Stage IIIA Ovarian Germ Cell Tumor|Stage IIIB Ovarian Cancer|Stage IIIB Ovarian Germ Cell Tumor|Stage IIIC Ovarian Cancer|Stage IIIC Ovarian Germ Cell Tumor|Stage IV Ovarian Cancer|Stage IV Ovarian Germ Cell Tumor National Cancer Institute (NCI) June 2014 Phase 1

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Chemical Information

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

C15H15N7O

CAS No. 1224844-38-5
Storage 3 years -20℃Powder
6 months-80℃in solvent (DMSO, water, etc.)
Synonyms
Solubility (25°C) * In vitro DMSO 62 mg/mL (200.43 mM)
Water <1 mg/mL (<1 mM)
Ethanol 2 mg/mL (6.46 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 Product Validation (3)


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Rating
Source Biochem Biophys Res Commun 2013 440(4), 701-6. INK 128 (MLN0128) purchased from Selleck
Method CCK-8 cell viability assay
Cell Lines Hep-2, SCC-9 cells
Concentrations 0.1 uM
Incubation Time 72 h
Results It found that AZD8055 was more potent than mTORC1 inhibitor rapamycin and Akt/mTOR dual inhibitor LY 294002 in killing of Hep-2 (D) and SCC-9 (E) cells. AZD2014 and INK-128, two other mTORC1/mTORC2 dual inhibitors, were also shown to inhibit the survival of Hep-2 and SCC-9 cells (D and E).

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Rating
Source Antonino Maria Spart from University of Bologn. 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.

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

Product Use Citation (3)

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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