BLZ945
发布者：信康 浏览次数：
产品名称:BLZ945CAS:953769-46-5别名：英文名：4-((2-(((1R,2R)-2-hydroxycyclohexyl)aMino)benzo[d]thiazol-6-yl)oxy)-N-MethylpicolinaMide
[] - 生物活性BLZ945是一种具有口服活性的，有效的选择性 CSF-1R抑制剂，IC50为1 nM，比其最接近的受体酪氨酸激酶同系物高出1000多倍的选择性。
- 体外研究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.
- 体内研究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. 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.
