INK 128 (MLN0128)
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.
Cited by 7 Publications
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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.
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|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.|
INK 128 exhibits an enzymatic inhibition activity against mTOR and more than 100-fold selectivity to PI3K kinases.  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. 
|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.  Daily, oral administration of INK 128 inhibits angiogenesis and tumor growth in multiplexenograft models. |
|In vitro||DMSO||62 mg/mL (200.43 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.
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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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