Ki-20227 is a highly selective c-Fms tyrosine kinase (CSF1R) inhibitor with IC50 value of 2 nM, displaying 6 fold and > 100 fold selectivity over VEGFR2 (IC50=12 nM) and c-Kit/PDGFRβ (IC50=451/217 nM), respectively.
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描述 | It is found that macrophage colony-stimulating factor is important for the differentiation of osteoclasts, thus facilitating it to participate into the development of osteolysis in bone metastatic lesions. Ki20227 is an inhibitor of c-fms tyrosine kinase with IC50 values of 2nM, also showed inhibition against VEGFR2 with IC50 value of 12nM (measured by kinase activity). In cellular study, Ki20227 (>3nM) showed dose-dependent inhibition of M-CSF-dependent c-Fms phosphorylation in RAW264.7 cells cultured in medium supplemented with 0.1% FCS. Also it showed inhibitory activity against M-CSF-dependent and VEGF-dependent cell growth in M-NFS-60 (10-100nM) and HUVEC cells (300-3000nM). As macrophage colony-stimulating factor was important in osteolysis, inhibition of c-Fms kinase by Ki20227 at concentration of 100nM suppressed the development of TRAP-positive osteoclast-like cell formation. Oral administration of 50 mg/kg of Ki20227 daily for 20 days could markedly decrease the osteolytic lesion areas which caused by metastasizing A375 cells in nude rats. Once daily oral treatment with Ki20227 at 20 mg/kg for 28 days significantly reduced the TRAP-positive osteoclastic cells on the bone surface in the primary spongiosa in ovariectomized rats, which suggesting Ki20227 could also suppress TRAP-positive osteoclast-like cell development in a non-tumor-bearing rodent model[1]. |
作用机制 | Not found |
Dose | Nude rat[1] (p.o.): 10 mg/kg - 50 mg/kg |
Administration | p.o. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.08mL 0.42mL 0.21mL |
10.41mL 2.08mL 1.04mL |
20.81mL 4.16mL 2.08mL |
CAS号 | 623142-96-1 |
分子式 | C24H24N4O5S |
分子量 | 480.536 |
别名 | |
运输 | 蓝冰 |
存储条件 |
粉末 Sealed in dry,Store in freezer, under -20°C 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 |
DMSO: 60 mg/mL(124.86 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |