中文名称: BLZ945
中文同义词: BLZ 945
CAS号: 953769-46-5
分子式: C20H22N4O3S
分子量: 398.47868
生物活性 BLZ945是一种具有口服活性的,**的选择性 CSF-1R抑制剂,IC50为1 nM,比其*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 inhibIT(http://www.maoyihang.com/sell/l_25/)s 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.
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