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Datasheet of BLZ945
Description: 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.
Chemical Information Catalog
DC8103
Purity of current batch:
>98%
Molecular Weight (MW)
398.48
Molecular Formula
C20H22N4O3S
CAS No.
953769-46-5
Solubility (25°C)
DMSO
Storage
Store at -20°C (desiccating conditions).
Handling: Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to 24 months. Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.