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Initial testing of VS-4718, a novel inhibitor of focal adhesion kinase (FAK), against pediatric tumor models by the Pediatric Preclinical Testing Program.

Publication ,  Journal Article
Kurmasheva, RT; Gorlick, R; Kolb, EA; Keir, ST; Maris, JM; Lock, RB; Carol, H; Kang, M; Reynolds, CP; Wu, J; Houghton, PJ; Smith, MA
Published in: Pediatr Blood Cancer
April 2017

VS-4718, a novel inhibitor of focal adhesion kinase (FAK), was tested against the Pediatric Preclinical Testing Program's (PPTP's) in vitro cell line panel and showed a median relative IC50 of 1.22 μM. VS-4718 was tested in vivo against the PPTP xenograft models using a dose of 50 mg/kg administered by the oral route twice daily for 21 days. VS-4718 induced significant differences in an event-free survival distribution compared with control in 18 of 36 of the evaluable solid tumor xenografts and in 0 of 8 acute lymphoblastic leukemia (ALL) xenografts, but no xenograft lines showed tumor regression. Future plans include further evaluation of the role of FAK inhibition in combination with ABL kinase inhibitors for Ph+ ALL.

Duke Scholars

Published In

Pediatr Blood Cancer

DOI

EISSN

1545-5017

Publication Date

April 2017

Volume

64

Issue

4

Location

United States

Related Subject Headings

  • Xenograft Model Antitumor Assays
  • Tumor Cells, Cultured
  • Oncology & Carcinogenesis
  • Neoplasms, Experimental
  • Mice, SCID
  • Mice, Nude
  • Mice, Inbred BALB C
  • Mice
  • Humans
  • Focal Adhesion Protein-Tyrosine Kinases
 

Citation

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Kurmasheva, R. T., Gorlick, R., Kolb, E. A., Keir, S. T., Maris, J. M., Lock, R. B., … Smith, M. A. (2017). Initial testing of VS-4718, a novel inhibitor of focal adhesion kinase (FAK), against pediatric tumor models by the Pediatric Preclinical Testing Program. Pediatr Blood Cancer, 64(4). https://doi.org/10.1002/pbc.26304
Kurmasheva, Raushan T., Richard Gorlick, E Anders Kolb, Stephen T. Keir, John M. Maris, Richard B. Lock, Hernan Carol, et al. “Initial testing of VS-4718, a novel inhibitor of focal adhesion kinase (FAK), against pediatric tumor models by the Pediatric Preclinical Testing Program.Pediatr Blood Cancer 64, no. 4 (April 2017). https://doi.org/10.1002/pbc.26304.
Kurmasheva RT, Gorlick R, Kolb EA, Keir ST, Maris JM, Lock RB, et al. Initial testing of VS-4718, a novel inhibitor of focal adhesion kinase (FAK), against pediatric tumor models by the Pediatric Preclinical Testing Program. Pediatr Blood Cancer. 2017 Apr;64(4).
Kurmasheva, Raushan T., et al. “Initial testing of VS-4718, a novel inhibitor of focal adhesion kinase (FAK), against pediatric tumor models by the Pediatric Preclinical Testing Program.Pediatr Blood Cancer, vol. 64, no. 4, Apr. 2017. Pubmed, doi:10.1002/pbc.26304.
Kurmasheva RT, Gorlick R, Kolb EA, Keir ST, Maris JM, Lock RB, Carol H, Kang M, Reynolds CP, Wu J, Houghton PJ, Smith MA. Initial testing of VS-4718, a novel inhibitor of focal adhesion kinase (FAK), against pediatric tumor models by the Pediatric Preclinical Testing Program. Pediatr Blood Cancer. 2017 Apr;64(4).
Journal cover image

Published In

Pediatr Blood Cancer

DOI

EISSN

1545-5017

Publication Date

April 2017

Volume

64

Issue

4

Location

United States

Related Subject Headings

  • Xenograft Model Antitumor Assays
  • Tumor Cells, Cultured
  • Oncology & Carcinogenesis
  • Neoplasms, Experimental
  • Mice, SCID
  • Mice, Nude
  • Mice, Inbred BALB C
  • Mice
  • Humans
  • Focal Adhesion Protein-Tyrosine Kinases