2015年6月1日星期一

BLZ945|BLZ-945,CSF1R inhibitor|DC Chemicals

BLZ945|BLZ-945,CSF1R inhibitor|DC Chemicals
BLZ945 is a highly selective and brain-penetrant inhibitor of CSF1R with IC50 of 1 nM; >3200-fold higher than its affinity for other kinases.

Catlog: DC8103| Product name: BLZ945| Cas: 953769-46-5| Other names: BLZ-945,BLZ 945| Molecule Formula: C20H22N4O3S| MW: 398.48. Purity: >98%

Price: 100mg: 750 USD; 250mg: 1300 USD; 1000mg: 2500 USD

BLZ945 is a highly selective and brain-penetrant inhibitor of CSF1R with IC50 of 1 nM; >3200-fold higher than its affinity for other kinases.
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.

For research and scientific purpose only, not for human use.

没有评论:

发表评论