OSI-027 is a selective and potent dual inhibitor of mTORC1 and mTORC2 with IC50 of 22 nM and 65 nM, respectively. It shows more than 100-fold selectivity for mTOR relative to PI3Kα, PI3Kβ, PI3Kγ, and DNA-PK. It 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 shows robust antitumor activity in several different human xenograft models representing various histologies. In COLO 205 and GEO colon cancer xenograft models, OSI-027 showed superior efficacy compared with rapamycin. OSI-027 is currently in Phase I clinical trials in patients with advanced solid tumors or lymphoma.
CAS Number: 936890-98-1
Molecular Weight: 406.44
Chemical Name: (1r,4r)-4-(4-amino-5-(7-methoxy-1H-indol-2-yl)imidazo[5,1-f][1,2,4]triazin-7-yl)cyclohexanecarboxylic acid
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO up to 50 mM
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥360 days if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
OSI-027 was used at 1-10 µM in vitro and in cellular assays.
OSI-027 was orally dosed to mice at 50-65 mg/kg once per day.
- Vakana E, et al. Induction of autophagy by dual mTORC1-mTORC2 inhibition in BCR-ABL-expressing leukemic cells. (2010) Autophagy. 6(7):966-7.
- Carayol N,et al. Critical roles for mTORC2- and rapamycin-insensitive mTORC1-complexes in growth and survival of BCR-ABL-expressing leukemic cells. (2010) Proc Natl Acad Sci USA. 107(28):12469-74.
- Falcon BL, et al. Reduced VEGF production, angiogenesis, and vascular regrowth contribute to the antitumor properties of dual mTORC1/mTORC2 inhibitors. (2011) Cancer Res. 71(5):1573-83.
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