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

Journal Article

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).

Full Text

Duke Authors

Cited Authors

  • Batra, V; Maris, JM; Kang, MH; Reynolds, CP; Houghton, PJ; Alexander, D; Kolb, EA; Gorlick, R; Keir, ST; Carol, H; Lock, R; Billups, CA; Smith, MA

Published Date

  • October 2012

Published In

Volume / Issue

  • 59 / 4

Start / End Page

  • 749 - 752

PubMed ID

  • 22052829

Electronic International Standard Serial Number (EISSN)

  • 1545-5017

Digital Object Identifier (DOI)

  • 10.1002/pbc.23364

Language

  • eng

Conference Location

  • United States