Sapanisertib (INK 128, MLN0128,TAK-228)
Molecular Weight(MW): 309.33
Sapanisertib (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 9 Publications
5 Customer Reviews
Blockade of PD-1 in combination with INK128 inhibits liver cancer cell proliferation and clone formation in vitro in immunocompetent mice. (A) Representative pictures show the clone formation of different administered groups in SMMC7721 PD-1 OE cells. (B) Histogram showing mean number of cloned formed 6 SD in each group. P < 0.05. (C) Optical density values 6 SD of Cell Counting Kit 8 assay in different administered groups in SMMC7721 PD-1 OE cells. (D,E) Flow-cytometric assessment of cell death with percent of annexin V1/7-aminoactinomycin D1 cells, mean 6 SEM. (F,G) Tumor growth kinetics (mean±SD) of different administered groups versus corresponding control in C57BL/6 mice subcutaneously implanted with PD-1 OE or vector-control Hepa1-6 cells. *P < 0.5; **P < 0.01; ***P < 0.001; #, not significant. Abbreviations: 7-AAD, 7-aminoactinomycin D; CCK8, Cell Counting Kit 8; NS, not significant; OD, optical density.
Hepatology, 2017, 66(6):1920-1933. Sapanisertib (INK 128, MLN0128,TAK-228) purchased from Selleck.
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. Sapanisertib (INK 128, MLN0128,TAK-228) purchased from Selleck.
(A–C), BMDMs were pretreated with or without INK128 (10, 20, or 30 nM) for 1 h and primed with LPS for 3 h. The cells were then stimulated with or without ATP. (A) Western blot analysis of IL-1β and cleaved caspase-1 in the supernatants and western blot analysis of NLRP3, pro-caspase-1 and pro-IL-1β in the lysates.
Acta Biochim Biophys Sin (Shanghai), 2018, doi: 10.1093/abbs/gmy088. Sapanisertib (INK 128, MLN0128,TAK-228) purchased from Selleck.
Purity & Quality Control
Choose Selective mTOR Inhibitors
|Description||Sapanisertib (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||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
30% PEG400+0.5% Tween80+5% propylene glycol
For best results, use promptly after mixing.
* 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.
Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).
Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
Molecular Weight Calculator
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02575339||Active not recruiting||Hepatocellular Carcinoma|Liver Cancer|HCC||Bert O''Neil MD|Millennium Pharmaceuticals Inc.|Big Ten Cancer Research Consortium||July 2016||Phase 1|Phase 2|
|NCT02756364||Active not recruiting||Breast Neoplasms||Millennium Pharmaceuticals Inc.|Takeda||June 1 2016||Phase 2|
|NCT02724020||Active not recruiting||Clear-cell Metastatic Renal Cell Carcinoma||Millennium Pharmaceuticals Inc.|Takeda||June 30 2016||Phase 2|
|NCT02719691||Recruiting||Metastatic Breast Cancer|Solid Tumors||University of Colorado Denver||May 13 2016||Phase 1|
|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||April 1 2016||Phase 2|
|NCT02514824||Active not recruiting||Merkel Cell Carcinoma||Dana-Farber Cancer Institute|Millennium Pharmaceuticals Inc.||October 2015||Phase 1|Phase 2|
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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Frequently Asked Questions
What is the recommendation method to formulate S2811 INK 128 (MLN0128) for oral administration?
You can try this vehicle for oral administration: 30% PEG400+0.5% Tween80 +5% Propylene glycol.