Sapanisertib (INK 128, MLN0128,TAK-228)

Catalog No.S2811

Sapanisertib (INK 128, MLN0128,TAK-228) Chemical Structure

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.

Size Price Stock Quantity  
In DMSO USD 221 In stock
USD 170 In stock
USD 270 In stock
USD 970 In stock
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Cited by 18 Publications

5 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,TAK-228) purchased from Selleck.

  • Antonino Maria Spart from University of Bologn. Sapanisertib (INK 128, MLN0128,TAK-228) purchased from Selleck.

  •  

    Bone marrow derived macrophages were pre-treated with 1nM INK128 for 1h prior to LPS treatment (100 ng/ml).  TNF-a production was analyzed 24h later. 

    Sapanisertib (INK 128, MLN0128,TAK-228) purchased from Selleck.

  • 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.

  • (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

Biological Activity

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.
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)
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  Mn2xR4VtdCCYaXHibYxqfHliQYPzZZk> MkDZNU0yODBibl2= NGW4TWQ4OiCq NXTDUHFTcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= NVjRUmd6OjR7N{G1OFQ>
PANC-1  NGSzS3ZE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MnO1OVAhdk1? NIDvbnYzPC17NjDo NXfVUHFYcW6qaXLpeJMh[2WubDD2bYFjcWyrdImgeIlu\SCmZYDlcoRmdnSueR?= MkXrNlQ6PzF3NES=
MIA PaCa-2 MVLD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MVKxMVExOCCwTR?= M2XLRVczKGh? MWXpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 NEHTNHIzPDl5MUW0OC=>
PANC-1  M3rJbmFxd3C2b4Ppd{BCe3OjeR?= MYOxNE0yODBibl2= NWrFfmZUPzJiaB?= Mo\1bY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= NH\tVngzPDl5MUW0OC=>
PANC-1  NVT1Xm5mTnWwY4Tpc44hSXO|YYm= MWCxNE82OCCwTR?= NXjRPWsyOjRiaB?= MUDkdoFu[XSrY3HscJkhcW6qaXLpeJMheGixc4Doc5J6dGG2aX;uJI9nKDSHLVLQNU1UPktzIDjtWG9TSzFiYXP0bZZifGmxbjDpcoRq[2G2b4LzLUBidmRiQXv0JIF1KFOncjC0O|MhMHSqZTDtWG9TSzJiYXP0bZZifGmxbjDpcoRq[2G2b4Kp NWDRdpFOOjR7N{G1OFQ>
PANC-1  NHe5UHpHfW6ldHnvckBCe3OjeR?= MV:1NEBvVQ>? MWq0PEBp MnO0[Il{enWydIOgZ4VtdCCleXPs[UBxem:pcnXzd4lwdg>? MnTtNlQ6PzF3NES=
PANC-1  M1jYbWZ2dmO2aX;uJGF{e2G7 NE\0XYQyOCCwTR?= NH;DSoE4OiCq MmDFbY5kemWjc3XzJIdmdWOrdHHibY5mKHOnboPpeIl3cXS7 NYPJN|c5OjR7N{G1OFQ>

... Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot
p-4EBP1 / 4EBP1 / p-S6 / S6 / p-Akt-S473 / p-Akt-T308 / Akt; 

PubMed: 25425103     


INK128 inhibits mTOR signaling in neuroblastoma cells. A panel of six neuroblastoma cell lines was treated with 0.2 μM INK128 for 0 hr, 4 hrs, and 6 hrs, lysed, subjected to SDS-PAGE and immunoblotted with indicated antibodies. β-Actin was detected as a l䲧疝Ỵ疞㧀疜膉痘 瘿뙠ෆᾰƌෆĀ

CD44 / Vimentin; 

PubMed: 29899840     


CD44 (high) SNU423 cells were treated with increasing concentrations of INK128 for 48 h. CD44, vimentin and downstream effectors of mTOR pathway were evaluated by immunoblotting. 

c-Jun; 

PubMed: 27462815     


Representative western blot of 293T cells after 24 h treatment with INK128. The results are representative of three independent experiments. 

p-mTOR(Ser2448) / mTOR / p-p70S6K(Thr389) / p70S6K / p-RPS / RPS6; 

PubMed: 25849580     


SUDHL-2 and SUDHL-4 cells were treated with either EtOH for 24 h, INK128 for 3 h at the concentrations as indicated, or 20 nM rapamycin (Rap.) for 3 h. Cell lysates were analyzed by western blotting for phosphorylation states and total levels of indicated䲧疝Ỵ疞㧀疜

FKBP1 / MARS / CDC25A / TCL1A; 

PubMed: 25849580     


SUDHL-2 and SUDHL-4 cells are treated with EtOH (20 mM) for 48 h or INK128 (40 nM) for 24 h. Protein levels of validated genes were analyzed by western blotting.

25425103 29899840 27462815 25849580
Growth inhibition assay
Cell viability ; 

PubMed: 25425103     


Six neuroblastoma cell lines were treated with the indicated concentrations of INK128 for 48 hrs. Cell viability was then measured by adding the mixture of 10 μL of CCK-8 and 190 μL of RPMI 1640 and reading the absorbance at 450 nm. Data were represented 䲧疝Ỵ疞㧀疜膉痘 瘿뙠ෆᾰƌෆĀ 㺣痖帉痖Ѐ瑖堘𢡄빢᎒ෆĀ鑸᎒彿堙奋堙巫堙᎒ﻺ᎒彿堙ﻮ᎒塚堙ﻺ

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

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

* 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.

Chemical Information

Molecular Weight 309.33
Formula

C15H15N7O
CAS No. 1224844-38-5
Storage powder
in solvent
Synonyms N/A

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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
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
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

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

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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID