Initial testing (stage 1) of the curaxin CBL0137 by the pediatric preclinical testing program.

ABSTRACT:

Background

CBL0137 is a novel drug that modulates FAcilitates Chromatin Transcription (FACT), resulting in simultaneous nuclear factor-κB suppression, heat shock factor 1 suppression and p53 activation. CBL0137 has demonstrated antitumor effects in animal models of several adult cancers and neuroblastoma.

Procedures

CBL0137 was tested against the Pediatric Preclinical Testing Program (PPTP) in vitro cell line panel at concentrations ranging from 1.0 nM to 10.0 μM and against the PPTP in vivo solid tumor xenograft and acute lymphocytic leukemia (ALL) panels at 50 mg/kg administered intravenously weekly for 4 weeks.

Results

The median relative IC₅₀ (rIC₅₀ ) value for the PPTP cell lines was 0.28 μM (range: 0.13-0.80 μM). There were no significant d

SUBMITTER: Lock R 

PROVIDER: S-EPMC5587189 | biostudies-literature | 2017 Apr

REPOSITORIES: biostudies-literature