产品说明书
GW2580
 |
同义名 : | - |
| CAS号 : | 870483-87-7 | |
| 货号 : | A161762 | |
| 分子式 : | C20H22N4O3 | |
| 纯度 : | 98% | |
| 分子量 : | 366.414 | |
| MDL号 : | MFCD12024701 | |
| 存储条件： |
粉末 Keep in dark place,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: 35 mg/mL(95.52 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： |
IP 2% DMSO+2% Tween80+30% PEG300+water 0.5 mg/mL clear PO 0.5% CMC-Na 57 mg/mL suspension |
| 生物活性 | |||
|---|---|---|---|
| 描述 | GW2580 is a selective inhibitor of CSF-1R with IC50 value of 60nM for cFMS kinase (measured by kinase activity), 150- to 500-fold selective compared to the other kinase tested including BRAF, CDK4, cKIT, cSRC, EGFR, ERBB2, ERBB4, ERK2, FLT-3, GSK3, ITK, JAK2, JNK3, MK2, P38, PDGFR-β, PDHK4, PKA, PKCα, PKCβI, PKCζ, SYK, TIE2 and VEGFR2, as well as mouse LCK kinases. Complete inhibition of CSF-1-dependent growth of mouse myeloid M-NFS-60 cells can be observed at 0.7μM by GW2580. Treatment with GW2580 at 1μM inhibited CSF-1-, GMCSF- and LPS-induced human monocytes growth by 100%, 80% and 50%, respectively. This can be also confirmed in vivo as oral dosed mice with GW2580 at 40mg/kg before CSF-1-priming dose completely blocked the ability of MCSF to increase LPS-induced IL-6 production, but slightly increased LPS-induced IL-6 production before vehicle-priming dose. It showed that oral dose with GW2580 at 20 and 80mg/kg, BID, before thioglycolate injection for 4 days could inhibit thioglycolate-induced macrophage Influx into the peritoneal cavity in vivo. Oral administration of GW2580 at 20 and 80mg/kg, BID, at 1h before i.p. injection of M-NFS-60 cells, produced a dose-related decrease in the number of tumor cells in mice on 4 days later[1]. | ||
| 作用机制 | GW2580 acts as a competitive inhibitor of ATP binding to the cFMS kinase.[1] | ||
| 细胞研究 | |||||
|---|---|---|---|---|---|
| 细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
| human BT474 cells | Growth inhibition assay | Growth inhibition of serum-stimulated human BT474 cells after 3 days by spectrophotometry, IC50=21 μM | 16249345 | ||
| human HN5 cells | Growth inhibition assay | Growth inhibition of serum-stimulated human HN5 cells after 3 days by spectrophotometry, IC50=29 μM | 16249345 | ||
| human PBMC | Function assay | Inhibition of LPS-induced IL6 production in human PBMC by ELISA, EC50=1.89 μM | 23095041 | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
|
1 mM 5 mM 10 mM |
2.73mL 0.55mL 0.27mL |
13.65mL 2.73mL 1.36mL |
27.29mL 5.46mL 2.73mL |
