 COA |
MSDS |
 HPLC |
NMR |
| CAS No: | 953769-46-5 |
| Molecular formula(MF) | C20H22N4O3S |
| Molecular Weight(MW): | 398.48 |
| Alias |
| In vitro | DMSO | 79 mg/mL (198.25 mM) |
|---|---|---|
| Ethanol | 3 mg/mL warmed (7.52 mM) | |
| Water | <1 mg/mL | |
| In vivo | 4% DMSO+30% PEG 300+ddH2O | 2.5mg/mL |
| Description | BLZ945 is an orally active, potent and selective CSF-1R inhibitor with IC50 of 1 nM, >1000-fold selective against its closest receptor tyrosine kinase homologs. | ||
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| Targets |
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| In vitro |
In bone marrow-derived macrophages (BMDMs), BLZ945 specifically inhibits CSF-1-dependent proliferation with EC50 of 67nM, and decreases CSF-1R phosphorylation. BLZ945 blocks the reciprocal effects between macrophages and glioma cells on the survival, proliferation and/ or polarization of each other to promote tumorigenesis. [1] |
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| In vivo | In glioma-bearing mice, BLZ945 blocks tumor progression and significantly improves survival via CSF-1R inhibition. BLZ945 also inhibits orthotopic tumor growth of patient-derived proneural tumor spheres and cell lines in vivo. [1] BLZ945 (200 mg/kg, p.o.) decreases the growth of malignant cells in both mouse mammary tumor virus-driven polyomavirus middle T antigen (MMTV-PyMT) model of mammary carcinogenesis and keratin 14-expressing human papillomavirus type 16 (K14-HPV-16) transgenic model of cervical carcinogenesis. [2] |