The PIM kinase inhibitor, SGI-1776, was tested against the PPTP in vitro (1.0nM-10μM) and in vivo panels (148mg/kg daily×5 days for 3 weeks). SGI-1776 exhibited cytotoxic activity in vitro with a median relative IC 50 of 3.1μM. SGI-1776 induced significant differences in EFS distribution in vivo in 9 of 31 solid tumor xenografts and in 1 of 8 of the evaluable ALL xenografts. SGI-1776 induced tumor growth inhibition meeting criteria for intermediate EFS T/C activity in 1 of 39 evaluable models. In contrast, SGI-1776 induced complete responses of subcutaneous MV4;11 (B myeloid leukemia). Pediatr Blood Cancer 2012;59:749-752.
- Developmental therapeutics
- Kinase inhibitors
- Preclinical testing
ASJC Scopus subject areas
- Pediatrics, Perinatology, and Child Health