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OSI-906

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.

References PubMed ID::http://www.ncbi.nlm.nih.gov/pubmed/18951424

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

Appearance

Pale yellow powder

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.

GDC-0200