中文名称: | GW2580 促销 | ||||
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英文名称: | GW2580 | ||||
别名: | 5-[[3-Methoxy-4-[(4-methoxyphenyl)methoxy]phenyl]methyl]-2,4-Pyrimidinediamine | ||||
CAS No: | 870483-87-7 | 分子式: | C20H22N4O3 | 分子量: | 366.41 |
CAS No: | 870483-87-7 | ||||
分子式: | C20H22N4O3 | ||||
分子量: | 366.41 |
基本信息
产品编号:G10045 |
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产品名称:GW2580 |
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CAS: |
870483-87-7 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式: |
溶于液体 |
-80℃ |
六个月 |
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分子量 |
366.41 |
-20℃ |
一个月 |
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化学名: |
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Solubility (25°C) |
体外 |
DMSO |
36mg/mL (98.25mM) |
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Ethanol |
Insoluble |
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Water |
Insoluble |
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体内(现配现用) |
5% DMSO+30% PEG 300+5% Tween 80+ddH2O |
5mg/mL |
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<1mg/ml表示微溶或不溶。 |
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普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 |
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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;⼀旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 |
制备储备液
浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
1mM |
2.7292mL |
13.6459mL |
27.2918mL |
5mM |
0.5458mL |
2.7292mL |
5.4584mL |
10mM |
0.2729mL |
1.3646mL |
2.7292mL |
50mM |
0.0546mL |
0.2729mL |
0.5458mL |
生物活性
产品描述 |
一种CFMS激酶活性抑制剂,IC50:30nM。 |
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靶点/IC50 |
IC50: 60nM (c-FMS) |
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体外研究 |
GW2580 completely inhibits the growth of CSF-1-dependent mouse myeloid M-NFS-60 cells at 0.7μM. GW2580 at 0.8-1μM.completely blocks the ability of CSF-1 to induce the growth of mouse M-NFS60 myeloid cells and human monocytes.GW2580 causes a 30-40% inhibition of PTH-induced calcium release at 0.1-0.3μM, with higher concentrations of 1, 3, and 10μM completely inhibiting the PTH response.GW2580 inhibits CSF1R phosphorylation in RAW264.7 murine macrophages stimulated with 10 ng/mL with IC50 of.approximately 10nM.GW2580 also inhibits TRKA activity with IC50 of 0.88μM. |
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体内研究 |
GW2580 (Oral administration; 20 and 80mg/kg) produces a dose-related decrease in the number of tumor cells, with the 80mg/kg dose completely blocking tumor growth.GW2580 (Oral administration; 20 and 80mg/kg) has gave maximal plasma concentrations of 1.4 and 5.6μM, respectively.GW2580 (50mg/kg; twice a day from days 0 to 21, 7 to 21, or 14 to 21) inhibits joint connective tissue and bone destruction in a 21-day adjuvant arthritis model. |
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Animal Model: |
Female C3H/HEN mice or female CD-1 nude mice weighing 22-26g |
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Dosage: |
20 and 80mg/kg |
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Administration: |
Oral administration |
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Result: |
Produced a dose-related decrease in the number of tumor cells, with the 80mg/kg dose completely blocking tumor growth. |
Animal Model: |
Produced a dose-related decrease in the number of tumor cells, with the 80mg/kg dose completely blocking tumor growth. |
Dosage: |
20 and 80mg/kg (Pharmacokinetic Study) |
Administration: |
Oral administration |
Result: |
Had gave maximal plasma concentrations of 1.4 and 5.6μM, respectively. |
推荐实验方法(仅供参考)
激酶实验: |
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cFMS酪氨酸激酶实验 |
10μM 酶, 100μM ATP,和 5mM MgCl2在50mM Tris HCL中在室温下温育90分钟,通过自磷酸化而使酶激活。使用圆底聚苯乙烯96孔板,在Biomek 2000上进行酶反应,反应体积为45μL。每孔加入溶于1μL DMSO的化合物或只加入DMSO,孔中有含50mM Mops(3-[N-Morpholino] 丙磺酸)的30μL 1.5×底物反应混合物,pH 7.5, 15mM MgCl2, 6μM 肽底物, 生物素-EAIYAPFAKKK-NH2 7.5mM DTT, 75mM NaCl, 10μM ATP, 和 0.5μCi(1 Ci = 37 GBq)[33P-γ] ATP。加入15μL 稀释的酶溶液开始反应,最终酶浓度为20nM。EDTA加入到对照孔中。反应进行40分钟,加入等体积的0.5%磷酸终止反应,75μL转移到已用 100μL 0.5%的磷酸预湿的96孔磷酸纤维素过滤板上。实验板在Millipore过滤板真空歧管上过滤,然后使用磷酸溶液洗涤三次,随后加入40μL闪烁液。实验板进行密封,然后使用Packard Topcount NXT闪烁计数器进行计数。 |
细胞实验: |
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细胞系 |
MCSF依赖性小鼠骨髓M-NFS-60细胞系 |
浓度 |
~20μM |
处理时间 |
3天 |
方法 |
细胞自旋减慢后,按2×106细胞/mL置于培养基中饥饿处理24小时,一天后开始细胞生长实验。进行M-NSF60 细胞生长实验的培养基缺乏MCSF。实验第二天,溶于DMSO 的10 mM GW2580稀释至20μM ,与0.2%DMSO在含10%血清的培养基中,连续稀释,获得一个10点浓度曲线。M-NFS-60 细胞按0.5×106细胞/mL再悬浮于含10%血清和20ng/mL小鼠MCSF的培养基中。细胞(50μL)加到含抑制剂(50μL)的孔中,3天后,每孔加入,10μL WST-1 试剂。温育4小时后,在440nm处测定吸光度,计算含全培养基和饥饿培养基的孔中的细胞生长差异。 |
动物实验: |
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动物模型 |
携带骨髓癌移植瘤 M-NFS-60的小鼠 |
剂量 |
80mg/kg |
给药处理 |
口服处理,每天两次 |
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液,使用的计算公式为:
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为:C1V1 = C2V2 ( 输入 输出 )