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.
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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 (mg) = Concentration (mM) × Volume (mL) × 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:
Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2
Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
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||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02575339||Active not recruiting||Drug: MLN0128|Drug: MLN0128 (RP2D)|Drug: Sorafenib||Hepatocellular Carcinoma|Liver Cancer|HCC||Bert O''Neil MD|Millennium Pharmaceuticals Inc.|Big Ten Cancer Research Consortium||July 2016||Phase 1|Phase 2|
|NCT02719691||Recruiting||Drug: Alisertib|Drug: MLN0128||Metastatic Breast Cancer|Solid Tumors||University of Colorado Denver||May 13 2016||Phase 1|
|NCT02244463||Recruiting||Drug: MLN0128||Anaplastic Thyroid Cancer|Thyroid Cancer||Dana-Farber Cancer Institute|Millennium Pharmaceuticals Inc.||July 2015||Phase 2|
|NCT02197572||Completed||Drug: MLN0128||Advanced Solid Tumors||Millennium Pharmaceuticals Inc.|Takeda||September 15 2014||Phase 1|
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.