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Initial testing (Stage 1) of AT13387, an HSP90 inhibitor, by the pediatric preclinical testing program.

Publication ,  Journal Article
Kang, MH; Reynolds, CP; Houghton, PJ; Alexander, D; Morton, CL; Kolb, EA; Gorlick, R; Keir, ST; Carol, H; Lock, R; Maris, JM; Wozniak, A; Smith, MA
Published in: Pediatr Blood Cancer
July 15, 2012

AT13387, a non-geldanamycin inhibitor of heat-shock protein 90 (HSP90), was tested against the PPTP in vitro panel (1.0 nM to 10 µM) and against the PPTP in vivo panels (40 or 60 mg/kg) administered orally twice weekly. In vitro AT13387 showed a median EC(50) value of 41 nM and exhibited activity consistent with a cytotoxic effect. In vivo AT13387 induced significant differences in EFS distribution compared to controls in 17% evaluable solid tumor xenografts, but in none of the ALL xenografts. No objective tumor responses were observed. In vivo AT13387 demonstrated only modest single agent activity.

Duke Scholars

Published In

Pediatr Blood Cancer

DOI

EISSN

1545-5017

Publication Date

July 15, 2012

Volume

59

Issue

1

Start / End Page

185 / 188

Location

United States

Related Subject Headings

  • Xenograft Model Antitumor Assays
  • Oncology & Carcinogenesis
  • Neoplasms
  • Mice, SCID
  • Mice, Nude
  • Mice, Inbred BALB C
  • Mice
  • Isoindoles
  • Humans
  • HSP90 Heat-Shock Proteins
 

Citation

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Kang, M. H., Reynolds, C. P., Houghton, P. J., Alexander, D., Morton, C. L., Kolb, E. A., … Smith, M. A. (2012). Initial testing (Stage 1) of AT13387, an HSP90 inhibitor, by the pediatric preclinical testing program. Pediatr Blood Cancer, 59(1), 185–188. https://doi.org/10.1002/pbc.23154
Kang, Min H., C Patrick Reynolds, Peter J. Houghton, Denise Alexander, Christopher L. Morton, E Anders Kolb, Richard Gorlick, et al. “Initial testing (Stage 1) of AT13387, an HSP90 inhibitor, by the pediatric preclinical testing program.Pediatr Blood Cancer 59, no. 1 (July 15, 2012): 185–88. https://doi.org/10.1002/pbc.23154.
Kang MH, Reynolds CP, Houghton PJ, Alexander D, Morton CL, Kolb EA, et al. Initial testing (Stage 1) of AT13387, an HSP90 inhibitor, by the pediatric preclinical testing program. Pediatr Blood Cancer. 2012 Jul 15;59(1):185–8.
Kang, Min H., et al. “Initial testing (Stage 1) of AT13387, an HSP90 inhibitor, by the pediatric preclinical testing program.Pediatr Blood Cancer, vol. 59, no. 1, July 2012, pp. 185–88. Pubmed, doi:10.1002/pbc.23154.
Kang MH, Reynolds CP, Houghton PJ, Alexander D, Morton CL, Kolb EA, Gorlick R, Keir ST, Carol H, Lock R, Maris JM, Wozniak A, Smith MA. Initial testing (Stage 1) of AT13387, an HSP90 inhibitor, by the pediatric preclinical testing program. Pediatr Blood Cancer. 2012 Jul 15;59(1):185–188.
Journal cover image

Published In

Pediatr Blood Cancer

DOI

EISSN

1545-5017

Publication Date

July 15, 2012

Volume

59

Issue

1

Start / End Page

185 / 188

Location

United States

Related Subject Headings

  • Xenograft Model Antitumor Assays
  • Oncology & Carcinogenesis
  • Neoplasms
  • Mice, SCID
  • Mice, Nude
  • Mice, Inbred BALB C
  • Mice
  • Isoindoles
  • Humans
  • HSP90 Heat-Shock Proteins