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

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

Pediatric blood & cancer (2014-03-26)
Hernan Carol, John M Maris, Min H Kang, C Patrick Reynolds, E Anders Kolb, Richard Gorlick, Stephen T Keir, Jianrong Wu, Raushan T Kurmasheva, Peter J Houghton, Malcolm A Smith, Richard B Lock, Dmitry Lyalin
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.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
L-Valine, from non-animal source, meets EP, JP, USP testing specifications, suitable for cell culture, 98.5-101.0%
Sigma-Aldrich
L-Valine, reagent grade, ≥98% (HPLC)
Supelco
L-Valine, certified reference material, TraceCERT®
Supelco
L-Valine, Pharmaceutical Secondary Standard; Certified Reference Material
Sigma-Aldrich
L-Valine, BioUltra, ≥99.5% (NT)
SAFC
L-Valine
Valine, European Pharmacopoeia (EP) Reference Standard