OSI-906 (Linsitinib)

Description: Linsitinib (formerly OSI-906; OSI 906) is a firs-in-class, ATP-competitive and orally bioavailable dual inhibitor of and insulin receptor (IR) and insulin-like growth factor-1 receptor (IGF-1R) with potential antitumor activity. It inhibits IGF-1R with an IC50 of 35 nM in cell-free assays; shows modest potency against InsR with IC50 of 75 nM, and has no activity against other kinases such as Abl, ALK, BTK, EGFR, FGFR1/2, PKA etc.

References: Future Med Chem. 2009 Sep; 1(6):1153-71; Clin Cancer Res. 2011 May 15; 17(10):3332-40.

Synonym: OSI906; Linsitinib; OSI-906; OSI 906;

Chemical Name: (1r, 3r)-3-(8-amino-1-(2-phenylquinolin-7-yl)imidazo[1, 5-a]pyrazin-3-yl)-1-methylcyclobutanol.

InChi Key: PKCDDUHJAFVJJB-KQODVJPSSA-N

InChi Code: InChI=1S/C26H23N5O/c1-26(32)14-19(15-26)25-30-22(23-24(27)28-11-12-31(23)25)18-8-7-17-9-10-20(29-21(17)13-18)16-5-3-2-4-6-16/h2-13, 19, 32H, 14-15H2, 1H3, (H2, 27, 28)/t19-, 26-

SMILES Code: O[C]1(C)C[CH](C2=NC(C3=CC=C4C=CC(C5=CC=CC=C5)=NC4=C3)=C6C(N)=NC=CN62)C1