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Pediatr Blood Cancer. 2014 Aug;61(8):1493-6. doi: 10.1002/pbc.25026. Epub 2014 Mar 24.

Initial testing (stage 1) of the notch inhibitor PF-03084014, by the pediatric preclinical testing program.

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1
Children's Cancer Institute Australia for Medical Research, Randwick, NSW, Australia.

Erratum in

  • Pediatr Blood Cancer. 2014 Sep;61(9):1716. Lyalin, Dmitry [added].

Abstract

PF-03084014, a γ-secretase inhibitor, was tested against the PPTP in vitro cell line panel (1.0 nM to 10 μM) and against the in vivo xenograft panels (administered orally twice daily on Days 1-7 and 15-21). PF-03084014 demonstrated limited in vitro activity, with no cell line achieving ≥50% inhibition. PF-03084014 induced significant differences in EFS distribution in 14 of 35 (40%) solid tumor xenografts, and 1 of 9 ALL xenografts (which lacked a NOTCH1 mutation), but objective responses were not observed. PF-03084014 demonstrated limited single agent activity in vitro and in vivo against the pediatric preclinical models studied.

KEYWORDS:

developmental therapeutics; notch inhibitors; preclinical testing

PMID:
24664981
PMCID:
PMC4225044
DOI:
10.1002/pbc.25026
[Indexed for MEDLINE]
Free PMC Article
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