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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.
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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 |
| 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 |
| 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 |
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RMC-4627 is a selective mTORC1 inhibitor that activates 4EBP1 and inhibits tumor growth. |
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| WYE-687 dihydrochloride
WYE-687 dihydrochloride is an ATP-competitive mTOR inhibitor with an IC50 of 7 nM. |
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