Powder: -20°C for 3 years | In solvent: -80°C for 1 year
FRAX486 HCL(1232030-35-1 free base) 是一种有效的 p21 活化激酶 (PAK) 抑制剂,对 PAK1、PAK2、PAK3 和 PAK4 的 IC50 值分别为 14、33、39 和 575 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 263 | 现货 | ||
2 mg | ¥ 369 | 现货 | ||
5 mg | ¥ 585 | 现货 | ||
10 mg | ¥ 989 | 现货 | ||
25 mg | ¥ 1,530 | 现货 | ||
50 mg | ¥ 2,320 | 现货 | ||
100 mg | ¥ 3,480 | 现货 | ||
200 mg | ¥ 4,930 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 997 | 现货 |
产品描述 | FRAX486 HCL is a potent p21-activated kinase (PAK) inhibitor with IC50 values of 14, 33, 39 and 575 nM for PAK1, PAK2, PAK3 and PAK4 respectively. |
靶点活性 | PAK3:39 nM, PAK2:33 nM, PAK1:14 nM, PAK4:575 nM |
体外活性 | In WPMY-1 cells, FRAX486 induces concentration-dependent (1-10 μM) degeneration of actin filaments. This was paralleled by attenuation of proliferation rate, being observed from 1 to 10 μM FRAX486. Cytotoxicity of FRAX486 in WPMY-1 cells is time- and concentration-dependent. In WPMY-1 cells, effects of FRAX486 on actin organization, survival, and proliferation occurred already at concentrations of 1-5 μM. In these concentrations, full inhibition of PAK1-3 may be expected, while PAK4 may be inhibited only partially[2]. |
体内活性 | FRAX486 crosses the blood-brain barrier and that therapeutically useful concentrations of FRAX486 are in the brain as early as 1 h and remain as long as 24 h after administration, with the maximum concentration in the target tissue at 8 h. Daily dosing results in steady-state levels of FRAX486 in the brain. FRAX486 specifically rescues the Fmr1 KO abnormality in which the spine phenotype is present in apical neurons and not simply decreasing spine density irrespective of genotype or existence of a phenotype. Also, FRAX486 reduces hyperactivity and stereotypical movements, both of which are phenotypes that characterize the mouse model of Fragile X syndrome[3]. |
细胞实验 | Cells are grown in 96-well plates (20,000 cells/well) for 24 h, before FRAX486, IPA3, or DMSO are added in indicated concentrations (1, 5, 10 μM). Subsequently, cells are grown for different periods (24, 48, 72 h). Separate controls are performed for each period. At the end of this period, 10 μl of [2-(2-methoxy-4-nitrophenyl)-3-(4-nitrophenyl)-5-(2,4-disulfophenyl)-2H-tetrazolium monosodium salt (WST-8) from CCK-8 is added, and absorbance in each well is measured at 450 nm after incubation for 2 h at 37°C. |
分子量 | 549.86 |
分子式 | C25H24Cl3FN6O |
CAS No. | T6840L |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 10.3 mg/mL (20 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.8186 mL | 9.0932 mL | 18.1864 mL | 45.4661 mL |
5 mM | 0.3637 mL | 1.8186 mL | 3.6373 mL | 9.0932 mL | |
10 mM | 0.1819 mL | 0.9093 mL | 1.8186 mL | 4.5466 mL | |
20 mM | 0.0909 mL | 0.4547 mL | 0.9093 mL | 2.2733 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
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