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Pediatr Blood Cancer. 2012 Oct;59(4):749-52. doi: 10.1002/pbc.23364. Epub 2011 Nov 2.

Initial testing (stage 1) of SGI-1776, a PIM1 kinase inhibitor, by the pediatric preclinical testing program.

Author information

1
Children's Hospital of Philadelphia, Philadelphia, PA 19104-4318, USA.

Abstract

The PIM kinase inhibitor, SGI-1776, was tested against the PPTP in vitro (1.0 nM-10 µM) and in vivo panels (148 mg/kg daily × 5 days for 3 weeks). SGI-1776 exhibited cytotoxic activity in vitro with a median relative IC(50) of 3.1 µM. 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).

PMID:
22052829
PMCID:
PMC3276706
DOI:
10.1002/pbc.23364
[Indexed for MEDLINE]
Free PMC Article

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