SGI-1776

Description: SGI-1776 is a novel, potent and ATP-competitive pan-inhibitor of the serine/threonine family of Pim kinase (an enzyme regulating cell survival) with potential antitumor activity. It inhibits Pim with an IC50 of 7 nM in a cell-free assay, and is 50- and 10-fold more selective for Pim2 and Pim3. Through extensive biomedical characterization, SGI-1776 exhibits specificity to the three isoforms of the Pim family, including Pim-1, Pim-2, and Pim-3. SGI-1776 was in phase I clinical trials for thetreatment of refractory prostate cancer and non-Hodgkin's lymphoma.However, the study was terminated in November 2010.

References: Blood. 2011 Jul 21; 118(3):693-702; Pediatr Blood Cancer. 2012 Oct; 59(4):749-52.

Synonym: SGI1776; SGI-1776; SGI 1776.

Chemical Name: N-((1-methylpiperidin-4-yl)methyl)-3-(4-(trifluoromethoxy)phenyl)imidazo[1, 2-b]pyridazin-6-amine.

InChi Key: SXLKQFDJPFXMGV-UHFFFAOYSA-N

InChi Code: InChI=1S/C20H22F3N5O/c1-27-10-8-14(9-11-27)12-24-18-6-7-19-25-13-17(28(19)26-18)15-2-4-16(5-3-15)29-20(21, 22)23/h2-7, 13-14H, 8-12H2, 1H3, (H, 24, 26)

SMILES Code: FC(F)(F)OC1=CC=C(C2=CN=C3C=CC(NCC4CCN(C)CC4)=NN32)C=C1