AZD8055 (mTOR inhibitor)

Preclinical pharmacology

AZD8055 is a potent, selective inhibitor of mTOR kinase, thus, targeting both mTORC1 (rapamycin-sensitive) and mTORC2 (rapamycin insensitive) complexes.  AZD8055 is specific against mTOR (IC50 value of 0.8 ± 0.2 nM using an immunoprecipitate of full length mTOR from HeLa cells as basis for an ELISA-based kinase assay).  AZD8055 was inactive in a counter screen against 260 kinases.

AZD8055 inhibited downstream targets of both mTORC1 (phosphorylation of S6 at serine 235/236) and mTORC2 (phosphorylation of AKT at serine 473) in several in vitro models in a dose- and time-dependent manner.  Oral treatment of mice bearing U87-MG human glioma xenografts twice daily with 2.5, 5, and 10 mg/kg/day AZD8055 for 10 days resulted in a dose-dependent tumour growth inhibition of 33%, 48% and 77%, respectively.  All doses were well tolerated.  The growth inhibitory effect of once daily administration with 10 and 20 mg/kg of AZD8055 for 10 days was 57 and 85%, respectively.  This tumour growth inhibitory effect was observed in a number of xenograft models tested in vivo.  Furthermore, the antitumour activity in vivo was in good agreement with growth inhibition observed in cell lines in vitro.

Additional Information

Clinical trials for this compound

See all of the clinical trials currently associated with this compound:

Publications for this compound

Find out more about this compound by reading related publications: