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OSI-027 is an inhibitor of mTORC1/2 that exhibits anticancer chemotherapeutic activity. In vitro, OSI0027 inhibits phosphorylation of downstream target Akt, inhibiting cell proliferation in breast cancer cells. OSI-027 also induces apoptosis in several lymphoid cell lines including mantle cell lymphoma, acute lymphocytic leukemia (ALL), and others. In animal models of cancer, this compound inhibits tumor growth.
| Cas No. | 936890-98-1 |
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| Purity | ≥99% |
| Formula | C21H22N6O3 |
| Formula Wt. | 406.44 |
| IUPAC Name | 4-[(5Z)-4-amino-5-(7-methoxyindol-2-ylidene)-1H-imidazo[5,1-f][1,2,4]triazin-7-yl]cyclohexane-1-carboxylic acid |
| Solubility | DMSO 18 mg/mL (44.28 mM) Water Insoluble Ethanol Insoluble |
| Appearance | Pale yellow powder |
| Store Temp | 4°C |
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| Ship Temp | Ambient |
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| Info Sheet | |
| Brochures |
Li H, Lin J, Wang X, et al. Targeting of mTORC2 prevents cell migration and promotes apoptosis in breast cancer. Breast Cancer Res Treat. 2012 Aug;134(3):1057-66. PMID: 22476852.
Gupta M, Hendrickson AE, Yun SS, et al. Dual mTORC1/mTORC2 inhibition diminishes Akt activation and induces Puma-dependent apoptosis in lymphoid malignancies. Blood. 2012 Jan 12;119(2):476-87. PMID: 22080480.
Falcon BL, Barr S, Gokhale PC, et al. Reduced VEGF production, angiogenesis, and vascular regrowth contribute to the antitumor properties of dual mTORC1/mTORC2 inhibitors. Cancer Res. 2011 Mar 1;71(5):1573-83. PMID: 21363918.
Vakana E, Sassano A, Platanias LC. Induction of autophagy by dual mTORC1-mTORC2 inhibition in BCR-ABL-expressing leukemic cells. Autophagy. 2010 Oct;6(7):966-7. PMID: 20699667.