CD 437
(Synonyms: 6-[3-(1-金刚烷基)-4-羟基苯基]-2-萘甲酸,CD437) 目录号 : GC11464
A selective RARγ agonist
Cas No.:125316-60-1
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cell experiment: | 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). The labeled cells are analyzed with a flow cytometer[1]. |
Animal experiment: | 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[2]. |
References: [1]. Li Y, et al. Molecular determinants of AHPN (CD437)-induced growth arrest and apoptosis in human lung cancer cell lines. Mol Cell Biol. 1998 Aug;18(8):4719-31. | |
CD 437 is a selective agonist of RARγ [1].
Retinoic acid receptor gamma (RAR-γ) is a nuclear receptor that is activated by 9-cis retinoic acid and all-trans retinoic acid. RAR-γ also functions as a transcription factor.
CD 437 is a selective RARγ agonist. In tumor cells, CD437 induced RAR-γ-dependent differentiation and apoptosis. Also, CD437 induced DNA adduct formation and p53-independent DNA damage response [1]. In DU145 human prostate cancer cells, CD437 rapidly reduced IκBα and increased nuclear translocation of the NF-κB subunit p65. Also, CD437 increased the DNA-binding activity of NF-κB and induced DR4 expression and apoptosis [2]. In human melanoma A375 cells, CD437 induced apoptosis, which was mediated by the activation of NF-κB and RIG-I (retinoic acid inducible gene I) pathway [3]. In human osteosarcoma cells, CD437 activated c-Jun N-terminal kinase 1 (JNK1) through the upregulation of thioredoxin-binding protein 2 (TBP2) and induced apoptosis. Also, CD437 induced TBP2 mRNA expression by recruitment of ETS1 transcription factor [4].
References:
[1]. Zhao X, Spanjaard RA. The apoptotic action of the retinoid CD437/AHPN: diverse effects, common basis. J Biomed Sci, 2003, 10(1): 44-49.
[2]. Jin F, Liu X, Zhou Z, et al. Activation of nuclear factor-kappaB contributes to induction of death receptors and apoptosis by the synthetic retinoid CD437 in DU145 human prostate cancer cells. Cancer Res, 2005, 65(14): 6354-6363.
[3]. Pan M, Geng S, Xiao S, et al. Apoptosis induced by synthetic retinoic acid CD437 on human melanoma A375 cells involves RIG-I pathway. Arch Dermatol Res, 2009, 301(1): 15-20.
[4]. Hashiguchi K, Tsuchiya H, Tomita A, et al. Involvement of ETS1 in thioredoxin-binding protein 2 transcription induced by a synthetic retinoid CD437 in human osteosarcoma cells. Biochem Biophys Res Commun, 2010, 391(1): 621-626.
| Cas No. | 125316-60-1 | SDF | |
| 别名 | 6-[3-(1-金刚烷基)-4-羟基苯基]-2-萘甲酸,CD437 | ||
| 化学名 | 6-(3-((1s,3R,5S,7s)-adamantan-1-yl)-4-hydroxyphenyl)-2-naphthoic acid | ||
| Canonical SMILES | OC1=CC=C(C2=CC=C3C(C=CC(C(O)=O)=C3)=C2)C=C1[C@]4(C[C@@H]5C6)C[C@@H]6C[C@H](C5)C4 | ||
| 分子式 | C27H26O3 | 分子量 | 398.5 |
| 溶解度 | DMF: 10 mg/ml,DMSO: 16 mg/ml,DMSO:PBS (pH 7.2) (1:1): 0.05 mg/ml,Ethanol: 1 mg/ml | 储存条件 | 4°C, protect from light |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.5094 mL | 12.5471 mL | 25.0941 mL |
| 5 mM | 0.5019 mL | 2.5094 mL | 5.0188 mL |
| 10 mM | 0.2509 mL | 1.2547 mL | 2.5094 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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