store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
CD437 (AHPN) 是一种特异性视黄酸受体激动剂。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 262 | 现货 | ||
2 mg | ¥ 369 | 现货 | ||
5 mg | ¥ 578 | 现货 | ||
10 mg | ¥ 912 | 现货 | ||
25 mg | ¥ 1,890 | 现货 | ||
50 mg | ¥ 3,150 | 现货 | ||
100 mg | ¥ 4,590 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 637 | 现货 |
产品描述 | CD437 (AHPN) is a specifc Retinoic Acid Receptor γ (RARγ) agonist. |
体外活性 | CD437 (10 μM, 2 days) inhibits the growth of these lung cancer cell lines. Dose-response experiments demonstrate that CD437 reduces the numbers of H460/SK-MES-1/A549/H292 cells (IC50: 0.5/0.4/3/0.85 μM). Treatment for 72 h with CD437 causes a strong dose-dependent growth inhibition in all melanoma cell lines. At a concentration of 5 μM CD437, only about 5 to 25% of the cells remain viable after 3 d. The concentrations of CD437 required for IC50 range from 10 μM for MeWo to 0.1 μM for SK-Mel-23 showing the highest sensitivity. |
体内活性 | Tumors in CD437-treated mice stop growing, an effect that becomes already statistically significant (P<0.01) at day 3 and 13 after first administration of CD437, and is maintained for more than 3 wk after discontinuation of treatment. Histologic analysis demonstrates marked c-fos mRNA levels at the tumor-stroma edge in CD437-treated tumors. |
激酶实验 | Forty microliter enzyme buffer (15 mM Tris HCl pH 8.1, 0.25 mM EDTA, 250 mM NaCl, 10% v:v glycerol) containing HDAC1, 3, 6 or 8 activity, 29 μL enzyme buffer and 1 μL resminostat [HCl] at different concentrations are added to a 96-well microtitre plate and the reaction started by the addition of 30 μL substrate peptide Ac-NH-GGK(Ac)-AMC (HDAC1, 3 and 6 assays, final concentrations 6 μM for HDAC1, 10 μM for HDAC6 and 25 μM for HDAC3/DAD) or Ac-RHK(Ac)K(Ac)-AMC (HDAC8 assay, final concentration 50 μM). After incubation for 180 min (HDAC1, HDAC6, HDAC8) or 120 min (HDAC3) at 30°C, the reaction is terminated by the addition of 25 μL stop solution (50 mM Tris HCl pH 8, 100 mM NaCl, 0.5 mg/mL trypsin and 2 μM trichostatin A [TSA]). After incubation at room temperature for further 40 min, fluorescence is measured using a Wallac Victor2 1420 multilabel counter (extinction 355 nm, emission 460 nm) for quantification of AMC generated by tryptic cleavage of the deacetylated peptide. For the calculation of the 50% inhibitory concentration (IC50) values the fluorescence in wells without test compound (1% DMSO, negative control) is set as 100% enzymatic activity and the fluorescence in wells with 2 μM TSA (positive control) are set at 0% enzymatic activity (background fluorescence substracted). |
细胞实验 | For morphological analysis, cells are treated with 10 μM CD437, trypsinized, washed with phosphate-buffered saline (PBS), fixed with 3.7% paraformaldehyde, and stained with 50 μg of 4,6-diamidino-2-phenylindole (DAPI) per mL containing 100 μg of DNase-free RNase A per mL to visualize the nuclei. Stained cells are examined by fluorescence microscopy. For the terminal deoxynucleotidyl transferase (TdT) assay, cells are treated with or without 10 μM CD437. After treatment, cells are trypsinized, washed with PBS, fixed in 1% formaldehyde in PBS, washed with PBS, resuspended in 70% ice-cold ethanol, and immediately stored at -20°C overnight. Cells are then labeled with biotin-16-dUTP by terminal transferase and stained with avidin-FITC (fluorescein isothiocyanate). |
动物实验 | Male Swiss-nu/nu mice weighing 20 to 25 g are used in this study. Mice are kept under sterile conditions at 24 to 26°C room temperature, 50% relative humidity, and 12 h light-dark rhythm in laminar flow shelves and are supplied with autoclaved food and bedding. For treatment of melanoma xenografts, previously established MeWo melanoma tumors of 1 to 2 mm in diameter are implanted into the right flank of animals. After tumor growth for 10 d, groups of mice (n=8) are either treated with saline p.o. or are injected intratumorally for 3 wk or are fed with various concentrations of CD437 (10 mg/kg/body weight and 30 mg/kg/body weight). In addition, tumors of a fifth group are injected with CD437 (10 mg/kg/body weight) each day. Mice are visited daily and growing tumors are measured twice weekly with a caliperlike instrument. |
别名 | AHPN, O-Desmethyl Adapalene, 6-[3-(1-金刚烷基)-4-羟基苯基]-2-萘甲酸, Apoptosis Activator VI |
分子量 | 398.49 |
分子式 | C27H26O3 |
CAS No. | 125316-60-1 |
store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 150 mg/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。
CD437 125316-60-1 Autophagy Metabolism Retinoid Receptor inhibit Retinoid X receptors AHPN O-Desmethyl Adapalene RAR/RXR Inhibitor 6-[3-(1-金刚烷基)-4-羟基苯基]-2-萘甲酸 Retinoic acid receptors Apoptosis Activator VI CD-437 CD 437 inhibitor