OSI-027
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.
References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18951419
| Cas No. |
936890-98-1 |
|---|---|
| Purity |
≥98% |
| 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 |
| Appearance |
Pale yellow powder |
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.
