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

Journal Article

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.

Full Text

Duke Authors

Cited Authors

  • 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 Date

  • April 2017

Published In

Volume / Issue

  • 64 / 4

PubMed ID

  • 27786412

Electronic International Standard Serial Number (EISSN)

  • 1545-5017

International Standard Serial Number (ISSN)

  • 1545-5009

Digital Object Identifier (DOI)

  • 10.1002/pbc.26304

Language

  • eng