1. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor Autophagy
  2. RAR/RXR Autophagy
  3. AM580

AM580  (Synonyms: CD336; NSC608001; Ro 40-6055)

目录号: HY-10475 纯度: 99.90%
COA 产品使用指南

AM580是选择性的 RARα 激动剂,IC50EC50 分别为8 nM,0.36 nM。

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AM580 Chemical Structure

AM580 Chemical Structure

CAS No. : 102121-60-8

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     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥660
In-stock
5 mg ¥600
In-stock
10 mg ¥900
In-stock
25 mg ¥2025
In-stock
50 mg ¥3443
In-stock
100 mg ¥5488
In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Customer Review

Other Forms of AM580:

    AM580 purchased from MCE. Usage Cited in: Biochem Biophys Res Commun. 2020 Jul 23;528(2):276-284.  [Abstract]

    After dealing with 10 nM AM580 for 3 days, the expression of RARβ is detected by immunobloting and quantified.
    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    AM580 is a selective RARα agonist with IC50 and EC50 of 8 nM and 0.36 nM, respectively.

    体外研究
    (In Vitro)

    G-CSF 存在下,AM580 (在 10-8 M) 对 NB4 细胞的 LAP mRNA 产生显著诱导。在浓度为 10-5 M 时,AM580 和 ATRA 与 G-CSF 联合使用,诱导几乎相同水平的 LAP 转录物。AM580 (在 10-8 M) 导致 NB4 细胞中编码 G-CSF 受体的转录本的稳态水平增加约六倍[1]
    AM580 (50 nM) 增加所有菌落中的 caspase-3 表达,并在 30% 的菌落中诱导腺泡样空化[2]。使用 shRARγ1 敲低原代 Myc 细胞中的 RARγ1,然后使用 Am580 处理导致更高水平的 CRBP1 表达,表明在这些细胞中 RARγ 对 RARα 具有抑制作用目标基因CRBP1
    Am580 (200 nM) 在 MCF-10A 和 MCF-7 细胞系中增强 RARγ 敲低表现出的抗增殖作用,但在 MDA-MB-231 细胞中没有这种作用[3]

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    体内研究
    (In Vivo)

    Am580 (0.3 mg/kg/天) 处理对 MMTV-wnt1 小鼠的无瘤生存有更深远的影响,即使在早期出现的肿瘤中效果也很明显,并且在肝、肺、肾和脾。Am580 处理显著且同等地降低了两个转基因腺体的增生水平[2]。使用 RARα 选择性激动剂 Am580 处理 MMTV-Myc 小鼠可显著抑制乳腺肿瘤生长、肺转移并延长 63% 小鼠的肿瘤潜伏期[3]

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    分子量

    351.44

    Formula

    C22H25NO3

    CAS 号
    性状

    固体

    颜色

    White to off-white

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    溶解性数据
    In Vitro: 

    DMSO 中的溶解度 : ≥ 45 mg/mL (128.04 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

    H2O 中的溶解度 : < 0.1 mg/mL (insoluble)

    * "≥" means soluble, but saturation unknown.

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.8454 mL 14.2272 mL 28.4544 mL
    5 mM 0.5691 mL 2.8454 mL 5.6909 mL
    查看完整储备液配制表

    * 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
    储备液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

    • 摩尔计算器

    • 稀释计算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    In Vivo:

    请根据您的 实验动物和给药方式 选择适当的溶解方案。

    以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
    ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用
    以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

    • 方案 一

      请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (7.11 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

      生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
    • 方案 二

      请依序添加每种溶剂: 10% DMSO    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (7.11 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液,此方案实验周期在半个月以上的动物实验酌情使用。

      1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

    动物溶解方案计算器
    请输入动物实验的基本信息:

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    由于实验过程有损耗,建议您多配一只动物的量
    请输入您的动物体内配方组成:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
    方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
    计算结果
    工作液所需浓度 : mg/mL
    储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
    您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
    动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
    连续给药周期超过半月以上,请谨慎选择该方案。
    请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
    纯度 & 产品资料

    纯度: 99.90%

    参考文献
    Kinase Assay
    [1]

    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 (1 mM MgCl2, 1 mM CaCl2, 20 mM ZnCl2, 0.1 mM NaCl, 0.1% [vol/vol] Triton X-100, 50 mM 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.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Assay
    [1]

    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.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [1]

    Four months old uniparous (1 pregnancy/lactation cycle) MMTV-neu and 6 weeks old nulliparous MMTV-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.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    参考文献

    完整储备液配制表

    * 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
    储备液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.8454 mL 14.2272 mL 28.4544 mL 71.1359 mL
    5 mM 0.5691 mL 2.8454 mL 5.6909 mL 14.2272 mL
    10 mM 0.2845 mL 1.4227 mL 2.8454 mL 7.1136 mL
    15 mM 0.1897 mL 0.9485 mL 1.8970 mL 4.7424 mL
    20 mM 0.1423 mL 0.7114 mL 1.4227 mL 3.5568 mL
    25 mM 0.1138 mL 0.5691 mL 1.1382 mL 2.8454 mL
    30 mM 0.0948 mL 0.4742 mL 0.9485 mL 2.3712 mL
    40 mM 0.0711 mL 0.3557 mL 0.7114 mL 1.7784 mL
    50 mM 0.0569 mL 0.2845 mL 0.5691 mL 1.4227 mL
    60 mM 0.0474 mL 0.2371 mL 0.4742 mL 1.1856 mL
    80 mM 0.0356 mL 0.1778 mL 0.3557 mL 0.8892 mL
    100 mM 0.0285 mL 0.1423 mL 0.2845 mL 0.7114 mL
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    产品名称:
    AM580
    目录号:
    HY-10475
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