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Ki20227

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Chemical Structure| 623142-96-1 同义名 : -
CAS号 : 623142-96-1
货号 : A691021
分子式 : C24H24N4O5S
纯度 : 99%+
分子量 : 480.536
MDL号 : MFCD12024693
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：
生物活性
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
实验方案
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