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Biological Activity:
Highly potent, orally efficacious and highly selective, dual ATP-competitive tyrosine kinase inhibitor of insulin-like growth factor-1 receptor (IGF-1R) (IC50: 35 nM) and insulin receptor (IR) (IC50: 75 nM).
References: online
MJ Mulvihill et al. Discovery of OSI-906: a selective and orally efficacious dual inhibitor of the IGF-1 receptor and insulin receptor. Fut. Med. Chem. 2009, 1(6), 1153-1171. [online]
CP Carden et al. Phase I study of intermittent dosing of OSI-906, a dual tyrosine kinase inhibitor of insulin-like growth factor-1 receptor (IGF-1R) and insulin receptor (IR) in patients with advanced solid tumors. J. Clin. Oncol. 2010, 28:15s (suppl; abstr 2530). [online]
V. M. Macaulay et al. Phase I study of OSI-906, dual tyrosine kinase inhibitor of insulin-like growth factor-1 receptor (IGF-1R) and insulin receptor (IR) in combination with erlotinib (E) in patients with advanced solid tumors. J. Clin. Oncol. 2010, 28:15s (suppl; abstr 3016). [online]
Chemical Name: cis-3-(8-amino-1-(2-phenylquinolin-7-yl)imidazo[1,5-a]pyrazin-3-yl)-1-methylcyclobutanol
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