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

Publication ,  Journal Article
Carol, H; Maris, JM; Kang, MH; Reynolds, CP; Kolb, EA; Gorlick, R; Keir, ST; Wu, J; Kurmasheva, RT; Houghton, PJ; Smith, MA; Lock, RB; Lyalin, D
Published in: Pediatr Blood Cancer
August 2014

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.

Duke Scholars

Published In

Pediatr Blood Cancer

DOI

EISSN

1545-5017

Publication Date

August 2014

Volume

61

Issue

8

Start / End Page

1493 / 1496

Location

United States

Related Subject Headings

  • Xenograft Model Antitumor Assays
  • Valine
  • Tetrahydronaphthalenes
  • Receptors, Notch
  • Oncology & Carcinogenesis
  • Neoplasms, Experimental
  • Neoplasm Proteins
  • Mice, SCID
  • Mice, Nude
  • Mice, Inbred BALB C
 

Citation

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Carol, H., Maris, J. M., Kang, M. H., Reynolds, C. P., Kolb, E. A., Gorlick, R., … Lyalin, D. (2014). Initial testing (stage 1) of the notch inhibitor PF-03084014, by the pediatric preclinical testing program. Pediatr Blood Cancer, 61(8), 1493–1496. https://doi.org/10.1002/pbc.25026
Carol, Hernan, John M. Maris, Min H. Kang, C Patrick Reynolds, E Anders Kolb, Richard Gorlick, Stephen T. Keir, et al. “Initial testing (stage 1) of the notch inhibitor PF-03084014, by the pediatric preclinical testing program.Pediatr Blood Cancer 61, no. 8 (August 2014): 1493–96. https://doi.org/10.1002/pbc.25026.
Carol H, Maris JM, Kang MH, Reynolds CP, Kolb EA, Gorlick R, et al. Initial testing (stage 1) of the notch inhibitor PF-03084014, by the pediatric preclinical testing program. Pediatr Blood Cancer. 2014 Aug;61(8):1493–6.
Carol, Hernan, et al. “Initial testing (stage 1) of the notch inhibitor PF-03084014, by the pediatric preclinical testing program.Pediatr Blood Cancer, vol. 61, no. 8, Aug. 2014, pp. 1493–96. Pubmed, doi:10.1002/pbc.25026.
Carol H, Maris JM, Kang MH, Reynolds CP, Kolb EA, Gorlick R, Keir ST, Wu J, Kurmasheva RT, Houghton PJ, Smith MA, Lock RB, Lyalin D. Initial testing (stage 1) of the notch inhibitor PF-03084014, by the pediatric preclinical testing program. Pediatr Blood Cancer. 2014 Aug;61(8):1493–1496.
Journal cover image

Published In

Pediatr Blood Cancer

DOI

EISSN

1545-5017

Publication Date

August 2014

Volume

61

Issue

8

Start / End Page

1493 / 1496

Location

United States

Related Subject Headings

  • Xenograft Model Antitumor Assays
  • Valine
  • Tetrahydronaphthalenes
  • Receptors, Notch
  • Oncology & Carcinogenesis
  • Neoplasms, Experimental
  • Neoplasm Proteins
  • Mice, SCID
  • Mice, Nude
  • Mice, Inbred BALB C