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Cat. No. M2099
OSI-027 Structure
Size Price Availability Quantity
5mg USD 75  USD75 In stock
10mg USD 140  USD140 In stock
50mg USD 395  USD395 In stock
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Quality Control & Documentation
Biological Activity

OSI-027 is a potent, orally bioavailable mammalian target of rapamycin (mTOR) kinase inhibitor with potential antineoplastic activity. OSI-027 shows more than 100-fold selectivity for mTOR relative to PI3Kα, PI3Kβ, PI3Kγ and DNA-PK. OSI-027 inhibits phosphorylation of the mTORC1 substrates 4E-BP1 and S6K1 as well as the mTORC2 substrate AKT in diverse cancer models in vitro and in vivo. OSI-027 potently inhibits proliferation of several rapamycin-sensitive and -insensitive nonengineered and engineered cancer cell lines and also, induce cell death in tumor cell lines with activated PI3K-AKT signaling. In contrast to rapamycin, OSI-027 induced apoptosis in a variety of lymphoid cell lines and clinical samples, including specimens of B-cell acute lymphocytic leukemia (ALL), mantle cell lymphoma, marginal zone lymphoma and Sezary syndrome. Furthermore, OSI-027 shows superior efficacy compared with rapamycin in COLO 205 and GEO colon cancer xenograft models. OSI-027 is currently in phase I clinical trials in cancer patients.

Customer Product Validations & Biological Datas
Source Oncotarget (2015). Figure 2. OSI-027
Method Western blot
Cell Lines PDAC cell lines
Concentrations 5 and 10 μM
Incubation Time 48 and 72 h
Results Flow cytometry assay showed 5 μM OSI-027 induced cell cycle arrest in the G0/G1 phase in Panc-1, BxPC-3, and CFPAC-1 cells, whereas RAPA had little effect on cell cycle. Moreover, 10 μM OSI-027 further upregulated the proportion of cells arrested in G0/ G1 phase
Protocol (for reference only)
Cell Experiment
Cell lines MDA-MB-231, MDA MB 435, PC-3, OVCAR-3, A549, DU145, NCI-H2122, U 87 MG and ACHN cell lines
Preparation method For assays of cell proliferation, cells were seeded into 96-well plates and incubated for 3 days in the presence of OSI-027 or OXA-01 at various concentrations. Inhibition of cell growth was determined by luminescent quantification of intracellular ATP content using CellTiterGlo® (Promega). Proliferation on Day 0 vs. 72h was used to plot dose-response curves for IC50 calculations and to determine cell death.
Concentrations 0.1~1μM
Incubation time 72 h
Animal Experiment
Animal models nu/nu CD-1 mice bearing MDA-MB-231 xenograft model
Formulation 20% Trappsol
Dosages 25 or 65 mg/kg QD for 14 days
Administration orally
Chemical Information
Molecular Weight 406.44
Formula C21H22N6O3
CAS Number 936890-98-1
Solubility (25°C) DMSO 17 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.


[1] Gupta M, et al. Blood. Dual mTORC1/mTORC2 inhibition diminishes Akt activation and induces Puma-dependent apoptosis in lymphoid malignancies.

[2] Bhagwat SV, et al. Mol Cancer Ther. Preclinical characterization of OSI-027, a potent and selective inhibitor of mTORC1 and mTORC2: distinct from rapamycin.

[3] Altman JK, et al. Clin Cancer Res. Dual mTORC2/mTORC1 targeting results in potent suppressive effects on acute myeloid leukemia (AML) progenitors.

[4] Falcon BL, et al. Cancer Res. Reduced VEGF production, angiogenesis, and vascular regrowth contribute to the antitumor properties of dual mTORC1/mTORC2 inhibitors.

[5] Carayol N, et al. Proc Natl Acad Sci U S A. Critical roles for mTORC2- and rapamycin-insensitive mTORC1-complexes in growth and survival of BCR-ABL-expressing leukemic cells.

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Keywords: OSI-027 supplier, mTOR, inhibitors, activators

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