|5-[3-甲氧基-4-(4-甲氧基苄氧基)苄基]嘧啶-2,4-二胺|CsnPharm

CAS No.: 870483-87-7

5-(3-Methoxy-4-((4-methoxybenzyl)oxy)benzyl)pyrimidine-2,4-diamine Catalog No. CSN12714

Synonyms: SC-203877

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.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 c-FMS

IC50:30nM
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

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
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

更多
动物研究
剂量
Rat: 7.5 mg/kg - 75 mg/kg^[2] (p.o., b.i.d) Mice: 160 mg/kg^[3] (p.o.)

给药途径
p.o.

动物研究
剂量	Rat: 7.5 mg/kg - 75 mg/kg^[2] (p.o., b.i.d) Mice: 160 mg/kg^[3] (p.o.)
给药途径	p.o.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.7292 mL
- 13.6458 mL
- 27.2916 mL
- 5 mM
- 0.5458 mL
- 2.7292 mL
- 5.4583 mL
- 10 mM
- 0.2729 mL
- 1.3646 mL
- 2.7292 mL

技术信息

CAS号

870483-87-7

储存条件

粉末: Keep in dark place,Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C20H22N4O3

运输

蓝冰

分子量

366.41

别名

SC-203877

溶解度

DMSO	25.0 mg/mL (68.2 mM) warming
Water	insoluble

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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5-(3-Methoxy-4-((4-methoxybenzyl)oxy)benzyl)pyrimidine-2,4-diamine Catalog No. CSN12714

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