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

Vandana Batra, John M. Maris, Min H. Kang, C. Patrick Reynolds, Peter J. Houghton, Denise Alexander, E. Anders Kolb, Richard Gorlick, Stephen T. Keir, Hernan Carol, Richard Lock, Catherine A. Billups, Malcolm A. Smith

Research output: Contribution to journalArticle

17 Scopus citations

Abstract

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.

Original languageEnglish (US)
Pages (from-to)749-752
Number of pages4
JournalPediatric Blood and Cancer
Volume59
Issue number4
DOIs
StatePublished - Oct 2012

Keywords

  • Developmental therapeutics
  • Kinase inhibitors
  • Preclinical testing

ASJC Scopus subject areas

  • Pediatrics, Perinatology, and Child Health
  • Hematology
  • Oncology

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    Batra, V., Maris, J. M., Kang, M. H., Reynolds, C. P., Houghton, P. J., Alexander, D., Kolb, E. A., Gorlick, R., Keir, S. T., Carol, H., Lock, R., Billups, C. A., & Smith, M. A. (2012). Initial testing (stage 1) of SGI-1776, a PIM1 kinase inhibitor, by the pediatric preclinical testing program. Pediatric Blood and Cancer, 59(4), 749-752. https://doi.org/10.1002/pbc.23364