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.

Sapanisertib (MLN0128) Chemical Structure

CAS No. 1224844-38-5

Selleck's Sapanisertib (MLN0128) has been cited by 97 publications

Purity & Quality Control

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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.
Targets
mTOR [3]
(Cell-free assay)
mTOR [3]
(Cell-free assay)
PI3Kα [3]
(Cell-free assay)
PI3Kγ [3]
(Cell-free assay)
PI3Kδ [3]
(Cell-free assay)
Click to View More Targets
1.4 nM(Ki) 1.4 nM(Ki) 219 nM 221 nM 230 nM
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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
PANC-1  MVjGeY5kfGmxbjDBd5NigQ>? NUCyb2dlOTBibl2= MXy3NkBp MX3pcoNz\WG|ZYOg[4Vu[2m2YXLpcoUhe2Wwc3n0bZZqfHl? MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDl5MUW0OEc,OjR7N{G1OFQ9N2F-
PANC-1  NHjhNFdHfW6ldHnvckBCe3OjeR?= M3zu[lUxKG6P MXO0PEBp NYPrc3c1\Gm|coXweJMh[2WubDDjfYNt\SCycn;ndoV{e2mxbh?= MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDl5MUW0OEc,OjR7N{G1OFQ9N2F-
PANC-1  NU\Pb3VXTnWwY4Tpc44hSXO|YYm= MUWxNE82OCCwTR?= NGXZSWszPCCq MUjkdoFu[XSrY3HscJkhcW6qaXLpeJMheGixc4Doc5J6dGG2aX;uJI9nKDSHLVLQNU1UPktzIDjtWG9TSzFiYXP0bZZifGmxbjDpcoRq[2G2b4LzLUBidmRiQXv0JIF1KFOncjC0O|MhMHSqZTDtWG9TSzJiYXP0bZZifGmxbjDpcoRq[2G2b4Kp MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDl5MUW0OEc,OjR7N{G1OFQ9N2F-
PANC-1  NVXhWoU3SXCxcITvd4l{KEG|c3H5 M{jKfFExNTFyMDDuUS=> M3jtU|czKGh? NITkT2RqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 M{nXNlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUexOVQ1Lz5{NEm3NVU1PDxxYU6=
MIA PaCa-2 MUTD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NVTZNWRQOS1zMECgcm0> MlTYO|IhcA>? MXrpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 NFmweJc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEm3NVU1PCd-MkS5O|E2PDR:L3G+
PANC-1  NXzIWlhjS2WubDDWbYFjcWyrdImgRZN{[Xl? MYm1NEBvVQ>? MYKyOE06PiCq NFTKOZlqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTD0bY1mKGSncHXu[IVvfGy7 NFjYbIM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEm3NVU1PCd-MkS5O|E2PDR:L3G+
PANC-1  NFvKVmxE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NGfOOJQyNTFyMDDuUS=> Mn:0O|IhcA>? MXPpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 NH\KO249[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEm3NVU1PCd-MkS5O|E2PDR:L3G+
TC32 MYXxTHRUKGG|c3H5 Mn\adWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFSFM{KgZ4VtdHN? NU\uNZFqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
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Saos-2 NEDVb3VyUFSVIHHzd4F6 NUX1bppEeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGPhc5MuOiClZXzsdy=> MmXtQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
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SK-N-SH Ml\YdWhVWyCjc4PhfS=> NYf0WGhPeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGPLMW4uW0hiY3XscJM> MlXPQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
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BT-12 MXLxTHRUKGG|c3H5 NV;Jd21seUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhSlRvMUKgZ4VtdHN? NWXnTJB7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
OHS-50 NI\VZ41yUFSVIHHzd4F6 MlLFdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKE:KUz21NEBk\Wyucx?= NX[3eHhwRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
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Assay
Methods Test Index PMID
Western blot FKBP1 / MARS / CDC25A / TCL1A ; p-mTOR(Ser2448) / mTOR / p-p70S6K(Thr389) / p70S6K / p-RPS / RPS6 ; c-Jun ; CD44 / Vimentin ; p-4EBP1 / 4EBP1 / p-S6 / S6 / p-Akt-S473 / p-Akt-T308 / Akt 25849580 27462815 29899840 25425103
Growth inhibition assay Cell viability 25425103
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
(Data is from Selleck tests instead of citations):
30% PEG400+0.5% Tween80+5% propylene glycol
For best results, use promptly after mixing.

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.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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.

Handling Instructions

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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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