Evaluation of entinostat alone and in combination with standard-of-care cytotoxic agents against rhabdomyosarcoma xenograft models.

ABSTRACT:

Background

Entinostat, a selective class I histone deacetylase inhibitor, has been reported to enhance the activity of cytotoxic agents and suppress expression of PAX3-FOXO1 in alveolar rhabdomyosarcoma (ARMS).

Procedures

Entinostat was tested against three rhabdomyosarcoma cell lines using 96-hour drug exposure. Entinostat alone or in binary combination with vincristine, actinomycin D or cyclophosphamide was tested in ARMS and two embryonal rhabdomyosarcoma (ERMS) xenograft models. Tumor growth was measured at weekly intervals. Drug-induced changes in acetylated histone H3(K9) and entinostat pharmacokinetics were determined.

Results

In vitro, the IC₅₀ concentration of entinostat ranged from 280 to 1300 nM. In vivo, entinostat significantly inhibited the gr

SUBMITTER: Kurmasheva RT 

PROVIDER: S-EPMC6685061 | biostudies-literature | 2019 Aug

REPOSITORIES: biostudies-literature