TAK-733

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TAK-733

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:	1035555-63-5
包装:	2mg, 5mg, 10mg, 50mg

包装与价格：

产品介绍

TAK-733是一种有效的，选择性的MEK变构抑制剂，作用于MEK1，IC50为3.2 nM，抑制Abl1， AKT3， c-RAF， CamK1， CDK2及c-Met等活性。

细胞实验
细胞系	a panel of CRC cell lines
方法	The antiproliferative effects of TAK-733 against CRC cell lines were determined using the sulforhodamine B (SRB) method. Briefly, cells in logarithmic growth phase were transferred to 96-well flat-bottomed plates with lids. Cell suspensions (100 μL) containing 3,000 to 5,000 viable cells were plated into each well and incubated overnight before exposure with increasing concentrations of TAK-733 for 72 hours. After treatment, medium was removed and the cells were fixed with cold 10% TCA for 30 minutes at 4°C. The cells were then washed with water and stained with 0.4% SRB (Fisher Scientific) for 30 minutes at room temperature and washed again with 1% acetic acid followed by stain solubilization with 10 mmol/L of Tris at room temperature. The plate was then read on a 96-well plate reader (Biotek Synergy 2) set at an absorbance wavelength of 565 nm. Cell proliferation curves were derived from the raw absorbance data and expressed as the percentage of vehicle-treated controls.
浓度	0~1μM
处理时间	72 h

动物实验
动物模型	Patient-derived tumor explant models
配制	0.5% methylcellulose
剂量	1 mg/kg once daily
给药处理	oral gavage

动物 A (mg/kg) = 动物 B (mg/kg) ×	动物 B的K_m系数
	动物 A的K_m系数

例如，依据体表面积折算法，将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量，需要将20 mg/kg 乘以小鼠的K_m系数（3），再除以大鼠的K_m系数（6），得到化合物用于大鼠的等效剂量为10 mg/kg。

以下数据基于产品分子量，对于特殊产品，请参照COA中的储备液配制条件和说明进行操作。

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.9832 mL	9.9161 mL	19.8322 mL
5 mM	0.3966 mL	1.9832 mL	3.9664 mL
10 mM	0.1983 mL	0.9916 mL	1.9832 mL