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AM580  ≥98%

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包装规格：5mg 25mg 100mg in glass bottle
溶解性：溶于DMSO(≥40mg/mL)
产品描述：基本信息 产品编号： A10972 产品名称： AM580 CAS: 102121-60-8   储存条件 粉末 -20℃ 四年     分子式： C22H25NO3 溶于液体 -80℃ 两年 分子量 351.45 -20℃ 一个月 化学名：  4-(5,5,8,8-tetramethyl-5,6,7,8-tetrahydronaphthalene-2-carboxamido)benzoic acid Solubility (25°C)：   体外:   DMSO 70mg/mL(199.18mM) Ethanol 24mg/mL(68.29mM) Water Insoluble 体内(现配现用): 1.请依序添加每种溶剂：10% DMSO→40% PEG300→5% Tween-80→45% saline Solubility:≥2.5mg/mL(7.11mM);Clear solution 此⽅案可获得≥2.5mg/mL(7.11mM，饱和度未知)的澄清溶液。以1mL⼯作液为例，取100μL25.0mg/mL的澄清DMSO储备液加到400μL PEG300中，混合均匀；向上述体系中加⼊50μL Tween-80，混合均匀；然后继续加⼊450μL⽣理盐⽔定容⾄1mL。 2.请依序添加每种溶剂：10% DMSO→90% corn oil Solubility:≥2.5mg/mL(7.11mM);Clear solution 此⽅案可获得≥2.5mg/mL(7.11mM，饱和度未知)的澄清溶液，此⽅案不适⽤于实验周期在半个⽉以上的实验。以1mL⼯作液为例，取100μL25.0mg/mL的澄清DMSO储备液加到900μL⽟⽶油中，混合均匀。 ＜1mg/ml表示微溶或不溶。 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。 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 2.8454mL 14.2272mL 28.4544mL 5mM 0.5691mL 2.8454mL 5.6909mL 10mM 0.2845mL 1.4227mL 2.8454mL 50mM 0.0569mL 0.2845mL 0.5691mL   生物活性 产品描述 一种选择性的RARα激动剂，IC50和EC50分别为8nM和0.36nM。 靶点   体外研究 In the presence of G-CSF, AM580 (at 10-8M) produces a remarkable induction in LAP mRNA of NB4 cells. At a concentration of 10-5M, AM580 and ATRA, in combination with G-CSF, induce almost the same level of LAP transcript. AM580 (at 10-8M) leads to an approximately sixfold increase in the steady-state levels of the transcript coding for the G-CSF receptor in NB4 cells. AM580 (50nM) increases caspase-3 expression in all of the colonies, and in 30% of the colonies induce acinar-like cavitation. Knockdown of RARγ1 in primary Myc cells using shRARγ1 followed by Am580 treatment results in an even higher level of CRBP1 expression, showing that in these cells RARγ has a repressive effect on the RARα target gene CRBP1. Am580 (200nM) enhances the anti-proliferative effect exhibited by RARγ knockdown in the MCF-10A and MCF-7 cell lines but not in the MDAMB-231 cells 体内研究 Am580 (0.3 mg/kg/day) treatment has a more profound effect on tumor-free survival ofmMTV-wnt1 mice, the effect being noticeable even in early appearing tumors, and no overt toxicity is found in liver, lungs, kidney, and spleen. Am580 treatment reduces substantially and equally the level of hyperplasia in both transgenic glands. Treatment ofmMTV-Myc mice with the RARα-selective agonist Am580 leads to significant inhibition of mammary tumor growth, lung metastasis and extends tumor latency in 63% of mice   推荐实验方法(仅供参考) Kinase Assay Approximately 1×106 NB4, HL-60, and APL fresh leukemic cells or CML neutrophils are harvested, pelletted by centrifugation at 400 g for 10 minutes, washed once with 0.9% NaCl, and centrifuged again. The washed cell pellet is resuspended in homogenization buffer (1mM MgCl2, 1mM CaCl2, 20mM ZnCl2, 0.1mM NaCl, 0.1% [vol/vol] Triton X-100, 50mM Tris/HCl, pH 7.4) and disrupted by vigorous pipetting. The homogenate is used for the LAP assay, which is performed with p-nitrophenol phosphate as substrate according to the instructions of the manufacturer. LAP activity is normalized for the content of protein in the sample. Proteins are measured according to the Bradford method using BSA fraction V as a standard. One unit of LAP activity is defined as the amount of enzyme capable of transforming 1 nmol of substrate in 1 minute at 25°C. Enzyme assays are performed in conditions of linearity relative to the substrate and to the concentration of proteins. Cell Assay MCF-10A (2×104 ) control cells or overexpressing RARγ are seeded in triplicates in 6-well culture dishes. After 24 hrs, cells are washed with PBS, incubated in 2 mL of DMEM-F12 culture medium, detached and counted every 24 hrs. Statistical significance is determined by t-test. pRB and p27 expression is tested by immunofluorescence analysis of control MCF-10A monolayers and monolayers stably transfected with pSG5-RARγ expression vector, using the same antibodies described for the IHC analysis Animal Administration Four months old uniparous (1 pregnancy/lactation cycle)mMTV-neu and 6 weeks old nulliparousmMTV-wnt1 female mice (50 mice/group) are treated with the RARα agonist AM580 (0.3 mg/kg body weight per mouse per day) in the diet (Purina 5053) by adding 1.5 mg AM580 per kg of Purina 5053 diet. Mice that develop tumors within the first month of treatment are removed from the study. Mice are palpated twice a week and tumor appearance is recorded. Once palpable, the size of the tumors is measured weekly. Tumor-free survival is calculated from Kaplan-Meier curves and statistical significance is determined by the Log-rank test for the survival studies and t-test for the tumor growth studies. Metastasis is evaluated by removing the lungs of all the anesthetized mice, selecting randomLy 20 mice per group and inspecting the lung surface for lesions using a stereoscope.
保存条件：-20℃

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