Pexidartinib (PLX3397)
规格
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 级别 | Moligand™ |
| 包装 | 1ml |
产品信息
| 品牌 | 阿拉丁 |
| 浓度 | 10mM in DMSO |
| Cas编号 | 1029044-16-3(DMSO) |
| Action Type | 抑制剂 |
| Mechanism Of Action | 干细胞生长因子受体抑制剂 |
| 简短描述 | c-Kit Inhibitors |
| 英文简短描述 | c-Kit Inhibitors |
| 过滤标签 | Compound libraries |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 生化和生理学机理 | Pexidartinib (PLX3397) 是一种口服的强效突变靶向受体酪氨酸激酶抑制剂，可抑制 CSF-1R、Kit (c-Kit) 和 FLT3，其 IC50 分别为 20 nM、10 nM 和 160 nM。Pexidartinib (PLX3397) 可诱导细胞凋亡和坏死，具有抗肿瘤活性。第 3 阶段 |
| 描述 |
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| 英文描述 |
Information Pexidartinib (PLX3397) Pexidartinib (PLX3397) is an oral, potent mutil-targeted receptor tyrosine kinase inhibitor of CSF-1R , Kit (c-Kit) , and FLT3 with IC50 of 20 nM, 10 nM and 160 nM, respectively. Pexidartinib (PLX3397) induces apoptosis and necros In M-NFS-60, Bac1.2F5 and M-07e cells, Pexidartinib inhibits the CSF1-dependent proliferation with IC50 of 0.44 μM, 0.22 μMand 0.1 μM, respectively. In vivo In MMTV-PyMT mice, Pexidartinib (40 mg/kg, p.o.) significantly inhibits both steady-state and PTX-induced tumor infiltration by CD45+CD11b+Ly6C−Ly6G−F4/80+. Pexidartinib/PTX therapy also results in a significant reduction in CD31+ vessel density within mammary tumors, paralleling induction of apoptosis and necrosis. In C57 mice bearing GL261 tumors, Pexidartinib (p.o.) inhibits glioblastoma invasion. In cmo mice, PLX3397 significantly attenuates autoinflammatory disease by decreasing the erosive bone lesions in tails and paws and the levels of circulating MIP-1α. In mice bearing B16F10 melanomas, Pexidartinib (45 mg/kg, p.o.) enhances CD8-mediated immunotherapy of melanoma. cell lines：REF52 or PC3 cells Concentrations： Incubation Time： Powder Purity:≥98% |