Sapanisertib (INK 128, MLN0128)


Sapanisertib (INK 128, MLN0128)化学構造


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.

サイズ 価格(税別)  
JPY 36686.00
JPY 28220.00
JPY 44820.00
JPY 161020.00


  • 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) purchased from Selleck.

    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.

  • (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) purchased from Selleck.

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




製品説明 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.
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

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 Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
PANC-1  MXzD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NEf0cW8yNTFyMDDuUS=> M1\SWVczKGh? MVzpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 MoqxNlQ6PzF3NES=
PANC-1  MVnD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M1TZb|UxKG6P NXTm[Y5lOjRvOU[gbC=> M1ziTYlvcGmkaYTzJINmdGxidnnhZoltcXS7IITpcYUh\GWyZX7k[Y51dHl? NH\TeGgzPDl5MUW0OC=>
MIA PaCa-2 M1G4bWNmdGxiVnnhZoltcXS7IFHzd4F6 Mof6NU0yODBibl2= MV63NkBp NUHQ[GMzcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= MlzaNlQ6PzF3NES=
PANC-1  MoCwRZBweHSxc3nzJGF{e2G7 MUOxNE0yODBibl2= MUC3NkBp MWPpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 MnfmNlQ6PzF3NES=
PANC-1  M2TsRmZ2dmO2aX;uJGF{e2G7 MmDtNVAwPTBibl2= M{DINFI1KGh? M{LMfYRz[W2jdHnjZYxtgSCrbnjpZol1eyCyaH;zdIhwenmuYYTpc44hd2ZiNFWtRnAyNVN4S{GgLI1VV1KFMTDhZ5RqfmG2aX;uJIlv\GmlYYTvdpMqKGGwZDDBb5Qh[XRiU3XyJFQ4OyBqdHjlJI1VV1KFMjDhZ5RqfmG2aX;uJIlv\GmlYYTvdkk> MmLmNlQ6PzF3NES=
PANC-1  MUDGeY5kfGmxbjDBd5NigQ>? M17NZ|UxKG6P MWK0PEBp NYPuR|No\Gm|coXweJMh[2WubDDjfYNt\SCycn;ndoV{e2mxbh?= M1viZlI1QTdzNUS0
PANC-1  MXfGeY5kfGmxbjDBd5NigQ>? NUL4ZZgxOTBibl2= Mnz0O|IhcA>? MXnpcoNz\WG|ZYOg[4Vu[2m2YXLpcoUhe2Wwc3n0bZZqfHl? MXiyOFk4OTV2NB?=


体内試験 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]


溶解度 (25°C)

体外 DMSO 62 mg/mL (200.43 mM)
Ethanol 2 mg/mL (6.46 mM)
Water Insoluble
体内 左から(NMPから)右の順に溶剤を製品に加えます(文献ではなく、Selleckの実験によるデータ):
30% PEG400+0.5% Tween80+5% propylene glycol
30 mg/mL

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程で起きる正常な現象ですからご安心ください。


分子量 309.33


CAS No. 1224844-38-5
in solvent
別名 N/A





質量 (g) = 濃度 (mol/L) x 体積 (L) x 分子量 (g/mol)


  • 質量





開始濃度 x 開始体積 = 最終濃度 x 最終体積


この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 入力 出力 )

  • C1



  • 連続希釈剤

  • 計算結果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):




チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2


質量 濃度 体積 分子量


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
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
NCT02719691 Recruiting Metastatic Breast Cancer|Solid Tumors University of Colorado Denver May 13 2016 Phase 1
NCT02725268 Recruiting Endometrial Neoplasms Millennium Pharmaceuticals Inc.|European Network of Translational Research in Ovarian Cancer - EUTROC|European Network of Individualized Treatment in Endometrial Cancer - ENITEC|Takeda April 1 2016 Phase 2
NCT02514824 Active not recruiting Merkel Cell Carcinoma Dana-Farber Cancer Institute|Millennium Pharmaceuticals Inc. October 2015 Phase 1|Phase 2



Handling Instructions


  • * 必須


  • 質問1:

    What is the recommendation method to formulate S2811 INK 128 (MLN0128) for oral administration?

  • 回答:

    You can try this vehicle for oral administration: 30% PEG400+0.5% Tween80 +5% Propylene glycol.


mTOR Inhibitors with Unique Features


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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID