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Sapanisertib (MLN0128)
Catalog No.S2811 Synonyms: INK 128,TAK-228
For research use only.
Sapanisertib (MLN0128, INK 128, TAK-228) 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.
CAS No. 1224844-38-5
Selleck's Sapanisertib (MLN0128) has been cited by 97 publications
Purity & Quality Control
Choose Selective mTOR Inhibitors
Related Compound Libraries
Other mTOR Products
Biological Activity
| Description | Sapanisertib (MLN0128, INK 128, TAK-228) 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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| Targets |
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| 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] |
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| Cell Data |
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| Assay |
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| 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] |
Protocol (from reference)
Solubility (25°C)
|
In vitro |
DMSO |
62 mg/mL
(200.43 mM) |
| Ethanol |
2 mg/mL
(6.46 mM) |
|
| Water |
Insoluble
|
|
|
In vivo |
Add solvents to the product individually and in order |
30 mg/mL |
Chemical Information
| Molecular Weight | 309.33 | ||
|---|---|---|---|
| Formula | C15H15N7O |
||
| CAS No. | 1224844-38-5 | ||
| Storage | 3 years | -20°C | powder |
| 2 years | -80°C | in solvent | |
| Smiles | CC(C)N1C2=NC=NC(=C2C(=N1)C3=CC4=C(C=C3)OC(=N4)N)N | ||
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
mg/kg
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.
Clinical Trial Information
| NCT Number | Recruitment | Interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|---|
| NCT04250545 | Recruiting | Drug: Sapanisertib|Drug: Telaglenastat Hydrochloride | Leptomeningeal Neoplasm|Metastatic Lung Non-Small Cell Carcinoma|Metastatic Malignant Neoplasm in the Brain|Recurrent Lung Non-Small Cell Carcinoma|Stage IV Lung Cancer AJCC v8|Stage IVA Lung Cancer AJCC v8|Stage IVB Lung Cancer AJCC v8 | National Cancer Institute (NCI) | November 9 2020 | Phase 1 |
| NCT02575339 | Active not recruiting | Drug: MLN0128|Drug: MLN0128 (RP2D)|Drug: Sorafenib | Hepatocellular Carcinoma|Liver Cancer|HCC | Kathy Miller|Millennium Pharmaceuticals Inc.|Big Ten Cancer Research Consortium | July 2016 | Phase 1|Phase 2 |
| NCT02719691 | Completed | Drug: Alisertib|Drug: MLN0128 | Metastatic Breast Cancer|Solid Tumors | University of Colorado Denver | May 13 2016 | Phase 1 |
| NCT02514824 | Completed | Drug: MLN0128 | Merkel Cell Carcinoma | Dana-Farber Cancer Institute|Millennium Pharmaceuticals Inc. | October 2015 | Phase 1|Phase 2 |
| NCT02244463 | Active not recruiting | Drug: MLN0128 | Anaplastic Thyroid Cancer|Thyroid Cancer | Dana-Farber Cancer Institute|Millennium Pharmaceuticals Inc. | July 2015 | Phase 2 |
(data from https://clinicaltrials.gov, updated on 2022-01-17)
Tech Support
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.
Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.
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Frequently Asked Questions
Question 1:
What is the recommendation method to formulate S2811 INK 128 (MLN0128) for oral administration?
Answer:
You can try this vehicle for oral administration: 30% PEG400+0.5% Tween80 +5% Propylene glycol.
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