Mechanism of action: Colony stimulating factor-1 receptor (CSF-1R) tyrosine kinase inhibitor

Preclinical pharmacology

AZD6495 binds to CSF-1R with a potency of 6nM and has a cell IC50 of 5nM.

AZD6495 reduced tumour associated macrophage levels and demonstrated tumour growth inhibition in breast cancer xenografts (MDA-MB-231 orthotopic and MCF7 ER+ subcutaneous) at 100mg/kg BID (for 18 days and 14 days respectively). 70% pCSF1R inhibition (PD) was observed 2 hours post dose in MDA-MB-231 orthotopic xenografts. Decrease in angiogenesis was observed in MCF7 (but not MDA-MD-231) xenografts as measured by CD31 IHC tumour vessel density.

Additional Information

Gene information from the NCBi

This compound works on the following genes: