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GW2580 {[allProObj[0].p_purity_real_show]}

货号:A161762 Ambeed 开学季,买赠积分,赢豪礼

GW2580 is a selective CSF-1R inhibitor for c-FMS with IC50 of 30 nM, 150- to 500-fold selective compared to b-Raf, CDK4, c-KIT, c-SRC, EGFR, ERBB2/4, ERK2, FLT-3, GSK3, ITK, JAK2 etc.

GW2580 化学结构 CAS号:870483-87-7
GW2580 化学结构
CAS号:870483-87-7
GW2580 3D分子结构
CAS号:870483-87-7
GW2580 化学结构 CAS号:870483-87-7
GW2580 3D分子结构 CAS号:870483-87-7
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GW2580 纯度/质量文件 产品仅供科研

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GW2580 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]

GW2580 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
HUVEC Growth inhibition assay Growth inhibition of VEGF-stimulated HUVEC after 3 days by spectrophotometry 16249345

GW2580 动物研究

Dose Rat: 7.5 mg/kg - 75 mg/kg[2] (p.o., b.i.d) Mice: 160 mg/kg[3] (p.o.)
Administration p.o.

GW2580 实验方案

计算器
存储液制备 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

GW2580 技术信息

CAS号870483-87-7
分子式C20H22N4O3
分子量 366.414
别名
运输蓝冰
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

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