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

Publication ,  Journal Article
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 in: Pediatr Blood Cancer
October 2012

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).

Duke Scholars

Published In

Pediatr Blood Cancer

DOI

EISSN

1545-5017

Publication Date

October 2012

Volume

59

Issue

4

Start / End Page

749 / 752

Location

United States

Related Subject Headings

  • Xenograft Model Antitumor Assays
  • Pyridazines
  • Proto-Oncogene Proteins c-pim-1
  • Phosphoproteins
  • Oncology & Carcinogenesis
  • Neoplasms
  • Mice, SCID
  • Mice, Inbred NOD
  • Mice
  • Imidazoles
 

Citation

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MLA
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Batra, V., Maris, J. M., Kang, M. H., Reynolds, C. P., Houghton, P. J., Alexander, D., … Smith, M. A. (2012). Initial testing (stage 1) of SGI-1776, a PIM1 kinase inhibitor, by the pediatric preclinical testing program. Pediatr Blood Cancer, 59(4), 749–752. https://doi.org/10.1002/pbc.23364
Batra, Vandana, John M. Maris, Min H. Kang, C Patrick Reynolds, Peter J. Houghton, Denise Alexander, E Anders Kolb, et al. “Initial testing (stage 1) of SGI-1776, a PIM1 kinase inhibitor, by the pediatric preclinical testing program.Pediatr Blood Cancer 59, no. 4 (October 2012): 749–52. https://doi.org/10.1002/pbc.23364.
Batra V, Maris JM, Kang MH, Reynolds CP, Houghton PJ, Alexander D, et al. Initial testing (stage 1) of SGI-1776, a PIM1 kinase inhibitor, by the pediatric preclinical testing program. Pediatr Blood Cancer. 2012 Oct;59(4):749–52.
Batra, Vandana, et al. “Initial testing (stage 1) of SGI-1776, a PIM1 kinase inhibitor, by the pediatric preclinical testing program.Pediatr Blood Cancer, vol. 59, no. 4, Oct. 2012, pp. 749–52. Pubmed, doi:10.1002/pbc.23364.
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. Initial testing (stage 1) of SGI-1776, a PIM1 kinase inhibitor, by the pediatric preclinical testing program. Pediatr Blood Cancer. 2012 Oct;59(4):749–752.
Journal cover image

Published In

Pediatr Blood Cancer

DOI

EISSN

1545-5017

Publication Date

October 2012

Volume

59

Issue

4

Start / End Page

749 / 752

Location

United States

Related Subject Headings

  • Xenograft Model Antitumor Assays
  • Pyridazines
  • Proto-Oncogene Proteins c-pim-1
  • Phosphoproteins
  • Oncology & Carcinogenesis
  • Neoplasms
  • Mice, SCID
  • Mice, Inbred NOD
  • Mice
  • Imidazoles