OSI-027

For research use only.

Catalog No.S2624 Synonyms: ASP4786

23 publications

OSI-027 Chemical Structure

Molecular Weight(MW): 406.44

OSI-027 is a selective and potent dual inhibitor of mTORC1 and mTORC2 with IC50 of 22 nM and 65 nM in cell-free assays, and more than 100-fold selectivity observed for mTOR than PI3Kα, PI3Kβ, PI3Kγ or DNA-PK. Phase 1.

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10mM (1mL in DMSO) USD 200 In stock
USD 120 In stock
USD 210 In stock
USD 570 In stock
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Selleck's OSI-027 has been cited by 23 publications

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Choose Selective mTOR Inhibitors

Biological Activity

Description OSI-027 is a selective and potent dual inhibitor of mTORC1 and mTORC2 with IC50 of 22 nM and 65 nM in cell-free assays, and more than 100-fold selectivity observed for mTOR than PI3Kα, PI3Kβ, PI3Kγ or DNA-PK. Phase 1.
Targets
mTOR [4]
(Cell-free assay)
mTORC1 [1]
(Cell-free assay)
mTORC2 [1]
(Cell-free assay)
PI3Kγ [4]
(Cell-free assay)
4 nM 22 nM 65 nM 0.42 μM
In vitro

OSI-027 shows the selective and ATP competitive inhibition activities against mTORC1 and mTORC2 with IC50 of 22 nM and 65 nM, respectively. In addition, OSI-027 inhibits mTOR signaling of phospho-4E-BP1 with an IC50 of 1 μM in cell-based assays. [1] OSI-027 exhibits anti-proliferative activities against several acute leukemia cell lines of myeloid/megakaryocytic origin in a dose-dependent manner, including U937, KG-1, KBM-3B, ML-1, HL-60, and MEG-01 cells. [2] A recent study shows that inhibition of mTORC1/2 by OSI-027 effectively suppresses phosphorylation of Akt (S473) and cell proliferation in breast cancer cells. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human SQ20B cells M{HVZmN6fG:2b4jpZ4l1gSCjc4PhfS=> MlH5O|IhcA>? Mm[2R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gV3EzOEJiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME2xMlMh|ryP NEHCWFAzPDR2NUOxNS=>
human Caki1 cells MVXDfZRwfG:6aXPpeJkh[XO|YYm= NFrZV|U4OiCq MY\DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDDZYtqOSClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUGuPUDPxE1? M4r3V|I1PDR3M{Gx
human SKHEP1 cells NWT0cYZZS3m2b4TvfIlkcXS7IHHzd4F6 NH:zcHE4OiCq MYPDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTT2hGWDFiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME2zMlIh|ryP NX;NWXZ3OjR2NEWzNVE>
human DU145 cells MWnDfZRwfG:6aXPpeJkh[XO|YYm= M3e5ZlczKGh? MnLzR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gSHUyPDViY3XscJMh[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME20MlEh|ryP NUK2[3d5OjR2NEWzNVE>
human HCT116 cells M3OwZmN6fG:2b4jpZ4l1gSCjc4PhfS=> NVfY[FZ{PzJiaB?= Mn3PR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTGNVOTF4IHPlcIx{KGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUC9OU43KM7:TR?= MXyyOFQ1PTNzMR?=
human ColoR cells NGe0WoNEgXSxdH;4bYNqfHliYYPzZZk> MonTO|IhcA>? NIDNbWJEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBEd2yxUjDj[YxteyCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVUvQCEQvF2= NH;6bFMzPDR2NUOxNS=>
human COLO205 cells NHvHTndEgXSxdH;4bYNqfHliYYPzZZk> NWL0SohvPzJiaB?= NGLCbVJEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBEV0yRMkC1JINmdGy|IHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:PS56IN88US=> MVuyOFQ1PTNzMR?=
human OVCAR3 cells M{nBTmN6fG:2b4jpZ4l1gSCjc4PhfS=> MlHkO|IhcA>? NF7jPWVEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBQXkODUkOgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF05NjFizszN NUXhOHlLOjR2NEWzNVE>
human HOP62 cells NUfBOIxQS3m2b4TvfIlkcXS7IHHzd4F6 MnqzO|IhcA>? NXrrN2lqS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUE:SNkKgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF01OSEQvF2= M{DtdVI1PDR3M{Gx
human COLO205 cells M2PYfGN6fG:2b4jpZ4l1gSCjc4PhfS=> MkjIO|IhcA>? NGnrXmdEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBEV0yRMkC1JINmdGy|IHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[Xl? MlPwNlQ5OzZyN{C=
human HOP62 cells MUTDfZRwfG:6aXPpeJkh[XO|YYm= M3LicFczKGh? NUjPfFNiS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUE:SNkKgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigQ>? M3roVVI1QDN4MEew

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-mTOR / mTOR / p-AKT / AKT / p-P70S6K / P70S6K / p-4EBP1 / 4EBP1 ; 

PubMed: 26026051     


Immunoblot analysis of mTORC1 and mTORC2 signaling in Huh-7 cells treated with 4 µmol/L rapamycin (Rapa) or various concentrations of OSI-027 for 8 hours.

26026051
Immunofluorescence
LC3; 

PubMed: 24610825     


U937 cells were treated with OSI-027 for 24 hours and after collection were stained with anti-DAPI (blue) or anti-LC3 (green) and signals were detected by confocal microscopy. Merged panels indicate areas of overlapping images of the two fluorescing signals.

24610825
Growth inhibition assay
Cell viability; 

PubMed: 25823922     


(A) U937, (B) MM6, (C) Kasumi-1 cells were plated in 96 well plates and treated with BYL-719 and OSI-027 alone and in combination, as indicated, for 72 hours. Viability was assessed using a WST-1 assay. Data are expressed as percentage of vehicle-treated cells (control). Shown are means and standard errors of five (A) or four (B and C) independent experiments.

25823922
In vivo In GEO colorectal xenograft, OSI-027 (65 mg/kg) inhibits both mTORC1 and mTORC2 effectors, including 4E-BP1, Akt, and S6 phosphorylation. Furthermore, mTORC1 and mTORC2 inhibition together by OSI-027 potently inhibits tumor growth more than mTORC1 inhibition by rapamycin. [1]

Protocol

Kinase Assay:

[1]

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Biochemical assays:

mTORC1 and mTORC2 inhibition is assayed using native enzyme complex immunoprecipitated from HeLa lysates at 1 mM ATP. To prepare whole cell lysates from HeLa cells, 25 g cell pellet is lysed in 60 mL of ice-cold buffer A [40 mM HEPES (pH 7.5), 120 mM NaCl, 1 mM EDTA, 10 mM sodium pyrophosphate, 10 mM glycerophosphate, 50 mM NaF, 0.5 mM orthovanadate, and EDTA-free protease inhibitors containing 0.3% CHAPS] for 30 minutes on a magnetic stirrer in a cold room. After clearing of the lysates by centrifugation at 13,000 g for 10 minutes, Protein G-coated 384-well plates are incubated with 0.25 μg of mTOR antibody in 15 μL of buffer A for 1 hour at 4 °C. To each well, 40 μg of HeLa cell lysate in 15 μL of buffer A is added and incubated overnight at 4 °C to immunoprecipitate mTOR complexes. Plates are washed 3 times with buffer A and twice with immunoprecipitation wash buffer [Buffer B: 50 mM HEPES (pH 7.5) and 150 mM NaCl]. OSI-027 is added at 10 μM concentration to each well and DMSO is added to the control wells. The reaction is started by adding 150 ng of His-tagged 4E-BP1 as a substrate in the presence or absence of 100 μM ATP to each well in 25 μL of freshly prepared kinase buffer [Buffer C: 20 mM HEPES (pH 7.5), 10 mM MgCl2, 4 mM MnCl2, 10 mM β-mercaptoethanol, and 200 μM vanadate] and incubated at room temperature (RT) for 30 minutes. The reaction is stopped by transferring 25 μL of reaction mixture from each well to corresponding wells of fresh Ni-chelate-coated plates and incubated overnight at 4 °C followed by 2 hours at 37 °C. To detect phosphorylation of 4E-BP1, the plates are washed once with TBST (Tris-buffered saline containing 0.1% Tween-20) containing 5% skim milk powder. To each well, 25 μL of 1:1,000 diluted phospho-4E-BP1 antibodies in TBST containing 5% skim milk are added and incubated for 1 hour at RT. The plates are washed once with TBST and then 25 μL of anti-rabbit HRP (diluted 1:10,000) in TBST containing 5% skim milk is added. The plates are incubated for 1 hour at RT and washed 5 times with TBST. For detection of phospho-4E-BP1, 25 μL of chemiluminescent reagents A+B is added and chemiluminescence is measured using an Analyst plate reader.
Cell Research:

[2]

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  • Cell lines: U937, KG-1, KBM-3B, ML-1, HL-60, and MEG-01
  • Concentrations: 0-10 μM
  • Incubation Time: 72 hours
  • Method:

    Inhibition of proliferation is measured using the Cell Titer Glo Assay , as noted in figure legends. To generate dose–response curves, cell lines are seeded at a density of 5,000 cells per well in a 96-well plate. After 24 hours of plating, cells are dosed with varying concentrations of either OSI-027 or rapamycin. The signal for Cell Titer Glo Assay is determined 72 hours after dosing and normalized to that of vehicle-treated controls. Inhibition of proliferation, relative to vehicle-treated controls, is expressed as a fraction of 1 and graphed using PRISM software.


    (Only for Reference)
Animal Research:

[1]

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  • Animal Models: GEO colorectal cells are injected s.c. into the right flank of nu/nu CD-1 mice.
  • Dosages: ≤65 mg/kg
  • Administration: Administered via gavage.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 18 mg/mL (44.28 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
1% DMSO+30% polyethylene glycol+1% Tween 80
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 406.44
Formula

C21H22N6O3

CAS No. 936890-98-1
Storage powder
in solvent
Synonyms ASP4786
Smiles COC1=CC=CC2=C1[NH]C(=C2)C3=C4[N](N=CN=C4N)C(=N3)C5CCC(CC5)C(O)=O

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID