Sapanisertib (INK 128, MLN0128)
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
3 Customer Reviews
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) 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
Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
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Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT01058707||Active not recruiting||Advanced Solid Malignancies||Millennium Pharmaceuticals Inc.|Takeda||January 4 2010||Phase 1|
|NCT02724020||Active not recruiting||Clear-cell Metastatic Renal Cell Carcinoma||Millennium Pharmaceuticals Inc.|Takeda||June 30 2016||Phase 2|
|NCT01351350||Completed||Advanced Solid Malignancies|Hematologic Malignancies||Millennium Pharmaceuticals Inc.|Takeda||February 28 2011||Phase 1|
|NCT02987959||Recruiting||Soft-tissue Sarcoma||Fox Chase Cancer Center||February 21 2017||Phase 2|
|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|
|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.