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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 the detailed information of BLZ945, the solubility of BLZ945 in water, the solubility of BLZ945 in DMSO, the solubility of BLZ945 in PBS buffer, the animal experiment (test) of BLZ945, the cell expriment (test) of BLZ945, the in vivo, in vitro and clinical trial test of BLZ945, the EC50, IC50,and affinity,of BLZ945, For the detailed information of BLZ945, the solubility of BLZ945 in water, the solubility of BLZ945 in DMSO, the solubility of BLZ945 in PBS buffer, the animal experiment (test) of BLZ945, the cell expriment (test) of BLZ945, the in vivo, in vitro and clinical trial test of BLZ945, the EC50, IC50,and affinity,of BLZ945, Please contact DC Chemicals. |
