CD437
Based on 4 publication(s) in Google Scholar
CD437 is a selective Retinoic Acid Receptor γ (RARγ) agonist.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 98.76%
- CAS 番号: 125316-60-1
- 分子式: C27H26O3
- 分子量:398.49
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保管条件:
4°C, protect from light
* In solvent : -80°C, 2 years; -20°C, 1 year (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
Retinoic Acid Receptor γ (RARγ)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A-431 | IC50 |
0.51 μM
Compound: 1
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Antiproliferative effect of compound on A431 cell line expressing mutant p53
Antiproliferative effect of compound on A431 cell line expressing mutant p53
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[PMID: 12620066] |
| DU-145 | IC50 |
0.28 μM
Compound: 1
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Antiproliferative effect of compound on DU145 cell line expressing mutant p53
Antiproliferative effect of compound on DU145 cell line expressing mutant p53
|
[PMID: 12620066] |
| GBM | IC50 |
0.55 μM
Compound: 1
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Antiproliferative effect of compound on GBM cell line expressing mutant p53
Antiproliferative effect of compound on GBM cell line expressing mutant p53
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[PMID: 12620066] |
| HCT-116 | IC50 |
0.68 μM
Compound: 1
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Antiproliferative effect of compound on HCT116 cell line expressing wild-type p53
Antiproliferative effect of compound on HCT116 cell line expressing wild-type p53
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[PMID: 12620066] |
| HepG2 | IC50 |
2.93 μM
Compound: PC2; CD437
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Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
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[PMID: 32717483] |
| IGROV-1 | IC50 |
0.35 μM
Compound: 1 (CD 437)
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Concentration of compound required for inhibition of (IGROV-1) human ovarian carcinoma cell growth by 50%
Concentration of compound required for inhibition of (IGROV-1) human ovarian carcinoma cell growth by 50%
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[PMID: 16033272] |
| IGROV-1 | IC50 |
0.35 μM
Compound: 1
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Antiproliferative effect of compound on IGROV-1 cell line expressing wild-type p53
Antiproliferative effect of compound on IGROV-1 cell line expressing wild-type p53
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[PMID: 12620066] |
| L02 | IC50 |
10.08 μM
Compound: PC2; CD437
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Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
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[PMID: 32717483] |
| LNCaP | IC50 |
0.32 μM
Compound: 1
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Antiproliferative effect of compound on LNcaP cell line expressing wild-type p53
Antiproliferative effect of compound on LNcaP cell line expressing wild-type p53
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[PMID: 12620066] |
| LoVo | IC50 |
0.49 μM
Compound: 1
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Antiproliferative effect of compound on LoVo cell line expressing wild-type p53
Antiproliferative effect of compound on LoVo cell line expressing wild-type p53
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[PMID: 12620066] |
| Me665/2/21 | IC50 |
0.42 μM
Compound: 1
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Antiproliferative effect of compound on Me665/2/21 cell line expressing mutant p53
Antiproliferative effect of compound on Me665/2/21 cell line expressing mutant p53
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[PMID: 12620066] |
| NB-4 | IC50 |
0.4 μM
Compound: 1 (CD 437)
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Concentration of compound required for inhibition of (NB4) human promyelocytic leukemia cell growth by 50%
Concentration of compound required for inhibition of (NB4) human promyelocytic leukemia cell growth by 50%
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[PMID: 16033272] |
| NCI-H460 | IC50 |
0.43 μM
Compound: 1
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Antiproliferative effect of compound on H460 cell line expressing wild-type p53
Antiproliferative effect of compound on H460 cell line expressing wild-type p53
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[PMID: 12620066] |
| OVCAR-3 | IC50 |
0.13 μM
Compound: 1, AHPN, CD437
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Antiproliferative activity against human OVCAR3 cell
Antiproliferative activity against human OVCAR3 cell
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[PMID: 21548569] |
| PC-3 | IC50 |
0.43 μM
Compound: 1
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Antiproliferative effect of compound on PC3 cell line
Antiproliferative effect of compound on PC3 cell line
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[PMID: 12620066] |
| QGY-7703 | IC50 |
2.38 μM
Compound: PC2; CD437
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Antiproliferative activity against human QGY-7703 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Antiproliferative activity against human QGY-7703 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
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[PMID: 32717483] |
| SAOS-2 | IC50 |
0.67 μM
Compound: 1
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Antiproliferative effect of compound on SAOS cell line
Antiproliferative effect of compound on SAOS cell line
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[PMID: 12620066] |
| SMMC-7721 | IC50 |
5.25 μM
Compound: PC2; CD437
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Antiproliferative activity against human SMMC-7721 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Antiproliferative activity against human SMMC-7721 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
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[PMID: 32717483] |
| U2OS | IC50 |
0.44 μM
Compound: 1
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Antiproliferative effect of compound on U2OS cell line expressing wild-type p53
Antiproliferative effect of compound on U2OS cell line expressing wild-type p53
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[PMID: 12620066] |
CD437 is a selective RARγ agonist. Growth inhibition by CD437 in these lung cancer cell lines is apparent after 2 days of treatment with 10 μM 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 0.85 μM, respectively[1].
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 50% growth inhibition (IC50) range from 10 μM for MeWo to 0.1 μM for SK-Mel-23 showing the highest sensitivity[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 125316-60-1
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性状 Solid
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分子量 398.49
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分子式 C27H26O3
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Color Off-white to light yellow
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SMILES
O=C(C1=CC=C2C=C(C3=CC=C(O)C(C4(C5)CC6CC5CC(C6)C4)=C3)C=CC2=C1)O
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別名
AHPN
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, protect from light
* In solvent : -80°C, 2 years; -20°C, 1 year (protect from light)
Publications (4)
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Journal Impact Factor
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Most Recent
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Science
Different repair pathways support intact or truncated insertions by R2 retrotransposon protein. [Abstract]2026 Feb 26;391(6788):eadz3121. PMID: 41231928 -
Cell
Amplification editing enables efficient and precise duplication of DNA from short sequence to megabase and chromosomal scale. [Abstract]2024 Jul 25;187(15):3936-3952.e19. PMID: 38936359 -
Arch Toxicol
Metabolic impact of genetic and chemical ADP/ATP carrier inhibition in renal proximal tubule epithelial cells. [Abstract]2023 Jul;97(7):1927-1941. PMID: 37154957 -
Mediators Inflamm
Retinoic Acid Receptor Gamma (RAR γ) Promotes Cartilage Destruction through Positive Feedback Activation of NF- κ B Pathway in Human Osteoarthritis. [Abstract]2022 Nov 7:2022:1875736. PMID: 36387933
溶剤 & 溶解度
DMSO : 150 mg/mL (376.42 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (protect from light). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (protect from light). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.27 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (6.27 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 2 years; -20°C, 1 year (protect from light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
プロトコル
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
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データシート (277 KB)
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SDS (536 KB)
- English - EN (536 KB)
- Français - FR (536 KB)
- Deutsch - DE (536 KB)
- Norwegian - NO (536 KB)
- Español - ES (536 KB)
- Swedish - SV (536 KB)
- Italian - IT (536 KB)
- Korean - KR (536 KB)
- Portuguese - PT (536 KB)
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取扱説明書 (2659 KB)
参考文献
[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. [Content Brief]
[2]. Schadendorf D, et al. Treatment of melanoma cells with the synthetic retinoid CD437 induces apoptosis via activation of AP-1 in vitro, and causes growth inhibition in xenografts in vivo. J Cell Biol. 1996 Dec;135(6 Pt 2):1889-98. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (protect from light). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.5095 mL | 12.5474 mL | 25.0947 mL | 62.7368 mL |
| 5 mM | 0.5019 mL | 2.5095 mL | 5.0189 mL | 12.5474 mL | |
| 10 mM | 0.2509 mL | 1.2547 mL | 2.5095 mL | 6.2737 mL | |
| 15 mM | 0.1673 mL | 0.8365 mL | 1.6730 mL | 4.1825 mL | |
| 20 mM | 0.1255 mL | 0.6274 mL | 1.2547 mL | 3.1368 mL | |
| 25 mM | 0.1004 mL | 0.5019 mL | 1.0038 mL | 2.5095 mL | |
| 30 mM | 0.0836 mL | 0.4182 mL | 0.8365 mL | 2.0912 mL | |
| 40 mM | 0.0627 mL | 0.3137 mL | 0.6274 mL | 1.5684 mL | |
| 50 mM | 0.0502 mL | 0.2509 mL | 0.5019 mL | 1.2547 mL | |
| 60 mM | 0.0418 mL | 0.2091 mL | 0.4182 mL | 1.0456 mL | |
| 80 mM | 0.0314 mL | 0.1568 mL | 0.3137 mL | 0.7842 mL | |
| 100 mM | 0.0251 mL | 0.1255 mL | 0.2509 mL | 0.6274 mL |
CD437 関連分類
HY-100532 関連分類
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