Brief Description

BLZ945 is an orally active, potent and selective CSF-1R inhibitor, which inhibits CSF-1R activity with an IC50 of 1nM and is more than 1000-fold selective against its closest receptor tyrosine kinase homologs c-KIT and Platelet-derived Growth Factor Receptor beta (PDGFRb) as well as more than 200 additional kinases, confirming the selectivity of the compound.
IC50 value: 1 nM
Target: CSF-1R inhibitor
in vitro: Treatment of bone marrow-derived macrophages (BMDMs) with BLZ945 inhibited CSF-1-dependent proliferation (EC50=67nM), and decreased CSF-1R phosphorylation, similar to CSF-1R antibody blockade. BLZ945 also reduced viability of CRL-2467 microglia, Ink4a/Arf/BMDMs (PDG genetic background), and NOD/SCID BMDMs. Importantly, BLZ945 treatment in culture did not affect proliferation of any PDG-derived tumor.
in vivo: BLZ945-treated TAMs retained CSF-1R expression in vivo, and there were no significant differences compared to vehicle-treated PDG gliomas. four human lines responded to BLZ945 in vivo, showing a clear histological response, and significantly reduced tumor growth and invasion. BLZ945 decreases primary mammary tumor growth but does not affect lung metastatic tumor burden in MMTV-PyMT mice.

Solubility

DMSO 50 mg/ml

Melting point

Boiling point

Density

Formula Weight:

Flash point

Storage conditions

Store at -20°C 2 years

Appearance:

White solid