INK 128 (MLN0128)

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.

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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:

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Product Information

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  • Research Area
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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)

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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]
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)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)0.020.151.80.40.0810312
Body Surface Area (m2)0.0070.0250.150.050.020.50.240.6
Km factor361285201220
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 2015-05-23)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02417701 Not yet recruiting Recurrent Squamous Cell Lung Carcinoma|Stage IV Squamous Cell Lung Carcinoma National Cancer Institute (NCI) May 2015 Phase 2
NCT02417701 Not yet recruiting Recurrent Squamous Cell Lung Carcinoma|Stage IV Squamous Cell Lung Carcinoma National Cancer Institute (NCI) May 2015 Phase 2
NCT02412722 Recruiting Non-Hematologic Malignancy Millennium Pharmaceuticals, Inc. March 2015 Phase 1
NCT02412722 Recruiting Non-Hematologic Malignancy Millennium Pharmaceuticals, Inc. March 2015 Phase 1
NCT02327169 Recruiting Advanced Nonhematologic Malignancies Millennium Pharmaceuticals, Inc. February 2015 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
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 (<1 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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