OSI-906 inhibits IGF-1R and InsR, displaying anticancer chemotherapeutic activity; it is currently in clinical trials as a potential treatment for colorectal cancer. In animal models of ovarian cancer, OSI-906 inhibits tumor development and growth. This compound also decreases tumor growth in animal models of fibroblast tumors. OSI-906 inhibits cell proliferation in colorectal cancer, breast cancer, pancreatic cancer, and non-small cell lung cancer (NSCLC) cells.
| Cas No. | 867160-71-2 |
|---|---|
| Purity | ≥98% |
| Formula | C26H23N5O |
| Formula Wt. | 421.49 |
| IUPAC Name | cis-3-[8-Amino-1-(2-phenyl-7-quinolinyl)imidazo[1,5-a]pyrazin-3-yl]-1-methylcyclobutanol |
| Synonym | OSI906, Linsitinib |
| Solubility | DMSO 84 mg/mL (199.29 mM) Water Insoluble Ethanol Insoluble |
| Appearance | Pale yellow powder |
| Store Temp | -20°C |
|---|---|
| Ship Temp | Ambient |
| MSDS | |
|---|---|
| Info Sheet |
Bendell JC, Jones SF, Hart L, et al. A phase Ib study of linsitinib (OSI-906), a dual inhibitor of IGF-1R and IR tyrosine kinase, in combination with everolimus as treatment for patients with refractory metastatic colorectal cancer. Invest New Drugs. 2015 Feb;33(1):187-93. PMID: 25335932.
Rao W, Li H, Song F, et al. OVA66 increases cell growth, invasion and survival via regulation of IGF-1R-MAPK signaling in human cancer cells. Carcinogenesis. 2014 Jul;35(7):1573-81. PMID: 24667688.
Mulvihill MJ, Cooke A, Rosenfeld-Franklin M, et al. Discovery of OSI-906: a selective and orally efficacious dual inhibitor of the IGF-1 receptor and insulin receptor. Future Med Chem. 2009 Sep;1(6):1153-71. PMID: 21425998.
