中文名称: | CD437 | ||||
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英文名称: | CD437 | ||||
别名: | 6-[3-(1-金刚烷基)-4-羟基苯基]-2-萘甲酸;3-缩水甘油醚氧丙基二甲基甲氧基硅烷;O-去甲基阿达帕林;阿达帕琳杂质E;ADAP-IME;O-去甲阿达帕林 AHPN | ||||
CAS No: | 125316-60-1 | 分子式: | C27H26O3 | 分子量: | 398.49 |
CAS No: | 125316-60-1 | ||||
分子式: | C27H26O3 | ||||
分子量: | 398.49 |
基本信息
产品编号: |
C10875 |
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产品名称: |
CD437 |
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CAS: |
125316-60-1 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式: |
溶于液体 |
-80℃ |
六个月 |
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分子量 |
398.49 |
-20℃ |
一个月 |
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化学名: |
6-[3-(1-Adamantyl)-4-hydroxyphenyl]-2-naphthalene carboxylic acid |
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Solubility (25°C): |
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体外:
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DMSO |
150mg/mL(376.42mM;Need ultrasonic and warming) |
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Ethanol |
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Water |
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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(6.27mM);Clear solution |
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此⽅案可获得≥2.5mg/mL(6.27mM,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。 |
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2.请依序添加每种溶剂:10% DMSO→90% (20% SBE-β-CD in saline) Solubility:2.5mg/mL(6.27mM);Suspended solution; Need ultrasonic |
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此⽅案可获得2.5mg/mL(6.27mM)的均匀悬浊液,悬浊液可⽤于⼝服和腹腔注射。以1mL⼯作液为例,取100μL25.0mg/mL的澄清DMSO储备液加到900μL20%的SBE-β-CD⽣理盐⽔⽔溶液中,混合均匀。 |
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3.请依序添加每种溶剂:10% DMSO→90% corn oil Solubility:≥2.5mg/mL(6.27mM);Clear solution |
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此⽅案可获得≥2.5mg/mL(6.27mM,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。 |
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<1mg/ml表示微溶或不溶。 |
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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。 |
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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 |
2.5095mL |
12.5474mL |
25.0947mL |
5mM |
0.5019mL |
2.5095mL |
5.0189mL |
10mM |
0.2509mL |
1.2547mL |
2.5095mL |
生物活性
产品描述 |
一个选择性视黄酸受体 (Retinoic Acid Receptor γ (RARγ)) 激动剂。 |
靶点 |
Retinoic Acid Receptor γ (RARγ) |
体外研究 |
CD437 is a selective RARγ agonist. Growth inhibition by CD437 in these lung cancer cell lines is apparent after 2 days of treatment with 10μM CD437. Dose-response experiments demonstrate that CD437 reduces the numbers of H460, SK-MES-1, A549, and H292 cells with 50% inhibitory values of approximately 0.5, 0.4, 3, and 0.85μM, respectively[1]. Treatment for 72 h with CD437 causes a strong dose-dependent growth inhibition in all melanoma cell lines. At a concentration of 5μM CD437, only about 5 to 25% of the cells remain viable after 3 d. The concentrations of CD437 required for 50% growth inhibition (IC50) range from 10μM for MeWo to 0.1μM for SK-Mel-23 showing the highest sensitivity |
体内研究 |
Tumors in CD437-treated mice stop growing, an effect that becomes already statistically significant (P<0.01) at day 13, 3 d after first administration of CD437, and is maintained for more than 3 wk after discontinuation of treatment. Further histologic analysis demonstrates marked c-fos mRNA levels at the tumor-stroma edge in CD437-treated tumors |
推荐实验方法(仅供参考)
Cell Assay |
For morphological analysis, cells are treated with 10μM CD437, trypsinized, washed with phosphate-buffered saline (PBS), fixed with 3.7% paraformaldehyde, and stained with 50μg of 4,6-diamidino-2-phenylindole (DAPI) per mL containing 100μg 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 10μM 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). The labeled cells are analyzed with a flow cytometer |
Animal Administration |
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 2mm 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 |
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液,使用的计算公式为:
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为:C1V1 = C2V2 ( 输入 输出 )