Ro 41-5253
Based on 3 publication(s) in Google Scholar
Ro 41-5253 is an orally active selective retinoic acid receptor alpha (RARα) antagonist. Ro 41-5253 can bind RARα without inducing transcription or affecting RAR/RXR heterodimerization and DNA binding. Ro 41-5253 can inhibit cancer cell proliferation and induce apoptosis, has antitumor activity.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 98.97%
- CAS. Nr.: 144092-31-9
- Formel: C28H36O5S
- Molecular Weight:484.65
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Speicherung:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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Biologische Aktivität
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) Ro 41-5253
More
Biologische Aktivität
IC50: 60 nM (RARα), 2.4 μM (RARβ), 3.3 μM (RARγ)[3].
Ro 41-5253 (1 nM-10 μM, 10 days) significantly inhibits MCF-7 and ZR 75.1 cell proliferation and induces cell apoptosis in a time and dose-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human breast-carcinoma lines MCF-7 and ZR 75.1
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Concentration:1 nM-10 μM
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Incubation Time:10 days
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Result:Inhibited 81% MCF-7 cell growth at 10 μM, 30% cell growth at 1 μM and no significant inhibitory effect at concentrations below 0.1 μM.
Inhibited 74% ZR 75.1 cell growth at 10 μM, 63% cell growth at 1 μM and 42% cell growth at 0.1 μM.
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Cell Line:Human breast-carcinoma lines MCF-7 and ZR 75.1
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Concentration:1 nM-10 μM
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Incubation Time:10 days
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Result:Induced 28.5, 21.6, 16 and 12% of MCF-7 cells apoptosis at 10 μM, 1 μM, 0.1 μM and 0.01 μM respectively on the fourth day while induced 58, 51, 36 and 21% of cells apoptosis at 10 μM, 1 μM, 0.1 μM and 0.01 μM respectively after six days.
Induced 80, 65, 43 and 29% of ZR 75.1 cells apoptosis at 10 μM, 1 μM, 0.1 μM and 0.01 μM respectively on the sixth day.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Six-week-old female athymic Balb/mice transplanted with MCF-7 cell line[2]
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Dosage:10, 30, 100, 300 and 600 mg/kg
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Administration:Oral gavage; once a week; 4 weeks
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Result:Resulted in a reduction in tumor volume at doses of 10, 30 and 100 mg/kg with no toxic side effects.
Chemical Information
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CAS. Nr. 144092-31-9
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Appearance Solid
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Molecular Weight 484.65
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Formel C28H36O5S
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Color White to off-white
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SMILES
O=C(C1=CC=C(C=C1)/C=C(C)/C2=C(C=C3C(C(C)(CCS3(=O)=O)C)=C2)OCCCCCCC)O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Publications (3)
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Journal Impact Factor
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Most Recent
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Adv Sci (Weinh)
Retinoic Acid Reprograms Mast Cells Toward a Proinflammatory State to Enhance Antitumor Immunity. [Abstract]2025 Nov 27:e09340. PMID: 41309490 -
J Hazard Mater
Multiple nuclear receptor-regulated endocrine disrupting effects: A case study for bisphenol-induced crosstalk between RARα and ERα signaling pathways. [Abstract]2025 Sep 5:495:139005. PMID: 40561951 -
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (206.33 mM; Need ultrasonic; 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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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 (5.16 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.
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, 6 months; -20°C, 1 month (sealed storage, away from moisture and 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.
Reinheit & Dokumentation
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Data Sheet (280 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. S Toma, et al. RARalpha antagonist Ro 41-5253 inhibits proliferation and induces apoptosis in breast-cancer cell lines. Int J Cancer. 1998 Sep 25;78(1):86-94 [Content Brief]
[2]. Salvatore Toma, et al. Retinoids and human breast cancer: in vivo effects of an antagonist for RAR-alpha. Cancer Lett. 2005 Feb 28;219(1):27-31. doi: 10.1016/j.canlet.2004.06.018. [Content Brief]
[3]. C Apfel, et al. A retinoic acid receptor alpha antagonist selectively counteracts retinoic acid effects. Proc Natl Acad Sci U S A. 1992 Aug 1;89(15):7129-33. [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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0633 mL | 10.3167 mL | 20.6334 mL | 51.5836 mL |
| 5 mM | 0.4127 mL | 2.0633 mL | 4.1267 mL | 10.3167 mL | |
| 10 mM | 0.2063 mL | 1.0317 mL | 2.0633 mL | 5.1584 mL | |
| 15 mM | 0.1376 mL | 0.6878 mL | 1.3756 mL | 3.4389 mL | |
| 20 mM | 0.1032 mL | 0.5158 mL | 1.0317 mL | 2.5792 mL | |
| 25 mM | 0.0825 mL | 0.4127 mL | 0.8253 mL | 2.0633 mL | |
| 30 mM | 0.0688 mL | 0.3439 mL | 0.6878 mL | 1.7195 mL | |
| 40 mM | 0.0516 mL | 0.2579 mL | 0.5158 mL | 1.2896 mL | |
| 50 mM | 0.0413 mL | 0.2063 mL | 0.4127 mL | 1.0317 mL | |
| 60 mM | 0.0344 mL | 0.1719 mL | 0.3439 mL | 0.8597 mL | |
| 80 mM | 0.0258 mL | 0.1290 mL | 0.2579 mL | 0.6448 mL | |
| 100 mM | 0.0206 mL | 0.1032 mL | 0.2063 mL | 0.5158 mL |
Ro 41-5253 Related Classifications
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