AM580
Based on 14 publication(s) in Google Scholar
AM580 is a selective RARα agonist with IC50 and EC50 of 8 nM and 0.36 nM, respectively.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 98.38%
- CAS No.: 102121-60-8
- Formule: C22H25NO3
- Masse moléculaire:351.44
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Activité biologique
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Chemical Information
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Solvant et solubilité
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- Pureté et documentation
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Publications Citing Use of MedChemExpress (MCE) AM580
More- Cancer Res. 2023 Jul 14;83(14):2387-2404. [Abstract]
- Adv Sci (Weinh). 2025 Nov 27:e09340. [Abstract]
- J Exp Clin Cancer Res. 2021 Apr 26;40(1):141. [Abstract]
- Allergy. 2022 Feb;77(2):483-498. [Abstract]
- J Hazard Mater. 2022 Aug 5:435:129024. [Abstract]
- EMBO J. 2021 Jun 1;40(11):e106771. [Abstract]
- Fundam Res. 2023 Apr 7;5(6):2975-2982. [Abstract]
- mBio. 2024 Feb 14;15(2):e0319723. [Abstract]
- Cancers (Basel). 2023 Oct 15;15(20):4995. [Abstract]
- J Biol Chem. 2024 Sep 12:107765. [Abstract]
- Viruses. 2020 Jun 10;12(6):628. [Abstract]
- Genes (Basel). 2024 Sep 13;15(9):1206. [Abstract]
- Biochem Biophys Res Commun. 2020 Jul 23;528(2):276-284. [Abstract]
- Am J Transl Res. 2022 Sep 15;14(9):6536-6549. [Abstract]
Customer Validation & Images
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Cell Proliferation/Viability Assay
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WB
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Cell Proliferation/Viability Assay
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Flow Cytometry
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Cell Imaging/Staining
Activité biologique
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Cell Line
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Type | Value | Description | References |
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| COS-7 | EC50 |
0.3 nM
Compound: AM-580
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Activity at human RARalpha ligand binding domain expressed in COS7 cells co-transfected with Gal4-DBD assessed as transcriptional activation after 16 hrs by Gal4 response element-driven luciferase reporter gene assay
Activity at human RARalpha ligand binding domain expressed in COS7 cells co-transfected with Gal4-DBD assessed as transcriptional activation after 16 hrs by Gal4 response element-driven luciferase reporter gene assay
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[PMID: 19058965] |
| COS-7 | EC50 |
13 nM
Compound: AM-580
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Activity at human RARgamma ligand binding domain expressed in COS7 cells co-transfected with Gal4-DBD assessed as transcriptional activation after 16 hrs by Gal4 response element-driven luciferase reporter gene assay
Activity at human RARgamma ligand binding domain expressed in COS7 cells co-transfected with Gal4-DBD assessed as transcriptional activation after 16 hrs by Gal4 response element-driven luciferase reporter gene assay
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[PMID: 19058965] |
| COS-7 | EC50 |
8.6 nM
Compound: AM-580
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Activity at human RARbeta ligand binding domain expressed in COS7 cells co-transfected with Gal4-DBD assessed as transcriptional activation after 16 hrs by Gal4 response element-driven luciferase reporter gene assay
Activity at human RARbeta ligand binding domain expressed in COS7 cells co-transfected with Gal4-DBD assessed as transcriptional activation after 16 hrs by Gal4 response element-driven luciferase reporter gene assay
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[PMID: 19058965] |
| HL-60 | ED50 |
3.4 x 10-10M
Compound: 5
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Compound was tested for differentiation-inducing activity against human promyelocytic leukemia cell line HL-60
Compound was tested for differentiation-inducing activity against human promyelocytic leukemia cell line HL-60
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[PMID: 2795600] |
| Panel leukemia (Carcinoma cell lines) | ED50 |
3.4 x 10-10M
Compound: AM-580
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Effective dose for differentiation -inducing activity against human promyelocytic leukemia cells
Effective dose for differentiation -inducing activity against human promyelocytic leukemia cells
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[PMID: 3184125] |
In the presence of G-CSF, AM580 (at 10-8 M) produces a remarkable induction in LAP mRNA of NB4 cells. At a concentration of 10-5 M, AM580 and ATRA, in combination with G-CSF, induce almost the same level of LAP transcript. AM580 (at 10-8 M) leads to an approximately sixfold increase in the steady-state levels of the transcript coding for the G-CSF receptor in NB4 cells[1]. AM580 (50 nM) increases caspase-3 expression in all of the colonies, and in 30% of the colonies induce acinar-like cavitation[2]. Knockdown of RARγ1 in primary Myc cells using shRARγ1 followed by Am580 treatment results in an even higher level of CRBP1 expression, showing that in these cells RARγ has a repressive effect on the RARα target gene CRBP1. Am580 (200 nM) enhances the anti-proliferative effect exhibited by RARγ knockdown in the MCF-10A and MCF-7 cell lines but not in the MDA-MB-231 cells[3].
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.
Chemical Information
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CAS No. 102121-60-8
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Appearance Solid
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Masse moléculaire 351.44
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Formule C22H25NO3
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Color White to off-white
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SMILES
CC(CC1)(C)C2=C(C=CC(C(NC3=CC=C(C(O)=O)C=C3)=O)=C2)C1(C)C
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Synonyms
CD336; NSC608001; Ro 40-6055
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (14)
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Journal Impact Factor
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Most Recent
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Cancer Res
Retinol saturase mediates retinoid metabolism to impair a ferroptosis defense system in cancer cells. [Abstract]2023 Jul 14;83(14):2387-2404. PMID: 37184371
AM580 purchased from MedChemExpress. Usage Cited in: Cancer Res. 2023 Jul 14;83(14):2387-2404. [Abstract]
Cell viability in A549, HT1080, or H1299 cells treated with RSL3 (A549 and HT1080, 4 μmol/L for 6 hours; H1299, 40 μmol/L for 24 hours) following pretreatment with 5 μmol/L AM580, or 5 μmol/L Ch55, and/or 10 μmol/L AGN193109 for 36 hours.
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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 Exp Clin Cancer Res
Inhibition of retinoic acid receptor α phosphorylation represses the progression of triple-negative breast cancer via transactivating miR-3074-5p to target DHRS3. [Abstract]2021 Apr 26;40(1):141. PMID: 33902658
AM580 purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2021 Apr 26;40(1):141. [Abstract]
Western blotting analysis of RARαS77 phosphorylation levels in non-TNBC cell lines (MCF-7, T47D, and SKBR3) and TNBC cell lines (MDA-MB-231, MDA-MB-453 and MDA-MB-436) with or without RARα agonist AM580 (1 μM) for 48 h.
AM580 purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2021 Apr 26;40(1):141. [Abstract]
TNBC cells overexpressing RARαS77A, RARα, and empty vector were further cultured with AM580 (0, 1 μM) for 14 days. The colony formation was observed by crystal violet staining.
AM580 purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2021 Apr 26;40(1):141. [Abstract]
Annexin V-APC/7-AAD double-staining assay by flow cytometry was used to detect apoptosis of TNBC cells stably overexpressing RARαS77A, RARα, or vector with or without AM580 (1-10 μM; 48 h) treatment.
AM580 purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2021 Apr 26;40(1):141. [Abstract]
AO staining of transfected TNBC cells with or without AM580 (1 μM) for 72 h. Scale bar, 20 μm.
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Allergy
The bile acid-activated retinoic acid response in dendritic cells is involved in food allergen sensitization. [Abstract]2022 Feb;77(2):483-498. PMID: 34365653 -
J Hazard Mater
Constructing an MCF-7 breast cancer cell-based transient transfection assay for screening RARα (Ant)agonistic activities of emerging phenolic compounds. [Abstract]2022 Aug 5:435:129024. PMID: 35523094 -
EMBO J
Inhibition of Syk promotes chemical reprogramming of fibroblasts via metabolic rewiring and H2 S production. [Abstract]2021 Jun 1;40(11):e106771. PMID: 33909912 -
Fundam Res
2023 Apr 7;5(6):2975-2982. PMID: 41467005 -
mBio
PEDV inhibits HNRNPA3 expression by miR-218-5p to enhance cellular lipid accumulation and promote viral replication. [Abstract]2024 Feb 14;15(2):e0319723. PMID: 38259103 -
Cancers (Basel)
A Combinatorial Regulatory Platform Determines Expression of RNA Polymerase III Subunit RPC7α (POLR3G) in Cancer. [Abstract]2023 Oct 15;15(20):4995. PMID: 37894362 -
J Biol Chem
PPARγ and C/EBPα enable adipocyte differentiation upon inhibition of histone methyltransferase PRC2 in malignant tumors. [Abstract]2024 Sep 12:107765. PMID: 39276936 -
Viruses
Broad-Spectrum Host-Based Antivirals Targeting the Interferon and Lipogenesis Pathways as Potential Treatment Options for the Pandemic Coronavirus Disease 2019 (COVID-19). [Abstract]2020 Jun 10;12(6):628. PMID: 32532085 -
Genes (Basel)
CHIR99021 and Brdu Are Critical in Chicken iPSC Reprogramming via Small-Molecule Screening. [Abstract]2024 Sep 13;15(9):1206. PMID: 39336797 -
Biochem Biophys Res Commun
2020 Jul 23;528(2):276-284. PMID: 32475642
AM580 purchased from MedChemExpress. Usage Cited in: Biochem Biophys Res Commun. 2020 Jul 23;528(2):276-284. [Abstract]
After dealing with 10 nM AM580 for 3 days, the expression of RARβ is detected by immunobloting and quantified.
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Am J Transl Res
Involvement of hedgehog signaling in all-trans retinoic acid-mediated suppression of colon cancer. [Abstract]2022 Sep 15;14(9):6536-6549. PMID: 36247302
Solvant et solubilité
DMSO : ≥ 45 mg/mL (128.04 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
* "≥" means soluble, but saturation unknown.
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. 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. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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 (7.11 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.
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.
Protocole
Approximately 1×106 NB4, HL-60, and APL fresh leukemic cells or CML neutrophils are harvested, pelletted by centrifugation at 400 g for 10 minutes, washed once with 0.9% NaCl, and centrifuged again. The washed cell pellet is resuspended in homogenization buffer (1 mM MgCl2, 1 mM CaCl2, 20 mM ZnCl2, 0.1 mM NaCl, 0.1% [vol/vol] Triton X-100, 50 mM Tris/HCl, pH 7.4) and disrupted by vigorous pipetting. The homogenate is used for the LAP assay, which is performed with p-nitrophenol phosphate as substrate according to the instructions of the manufacturer. LAP activity is normalized for the content of protein in the sample. Proteins are measured according to the Bradford method using BSA fraction V as a standard. One unit of LAP activity is defined as the amount of enzyme capable of transforming 1 nmol of substrate in 1 minute at 25°C. Enzyme assays are performed in conditions of linearity relative to the substrate and to the concentration of proteins.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MCF-10A (2×104) control cells or overexpressing RARγ are seeded in triplicates in 6-well culture dishes. After 24 hrs, cells are washed with PBS, incubated in 2 mL of DMEM-F12 culture medium, detached and counted every 24 hrs. Statistical significance is determined by t-test. pRB and p27 expression is tested by immunofluorescence analysis of control MCF-10A monolayers and monolayers stably transfected with pSG5-RARγ expression vector, using the same antibodies described for the IHC analysis.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Four months old uniparous (1 pregnancy/lactation cycle) MMTV-neu and 6 weeks old nulliparous MMTV-wnt1 female mice (50 mice/group) are treated with the RARα agonist AM580 (0.3 mg/kg body weight per mouse per day) in the diet (Purina 5053) by adding 1.5 mg AM580 per kg of Purina 5053 diet. Mice that develop tumors within the first month of treatment are removed from the study. Mice are palpated twice a week and tumor appearance is recorded. Once palpable, the size of the tumors is measured weekly. Tumor-free survival is calculated from Kaplan-Meier curves and statistical significance is determined by the Log-rank test for the survival studies and t-test for the tumor growth studies. Metastasis is evaluated by removing the lungs of all the anesthetized mice, selecting randomLy 20 mice per group and inspecting the lung surface for lesions using a stereoscope.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (280 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Gianní M, et al. AM580, a stable benzoic derivative of retinoic acid, has powerful and selective cyto-differentiating effects on acute promyelocytic leukemia cells. Blood. 1996 Feb 15;87(4):1520-31. [Content Brief]
[2]. Lu Y, et al. Mechanism of inhibition of MMTV-neu and MMTV-wnt1 induced mammary oncogenesis by RARalpha agonist AM580. Oncogene. 2010 Jun 24;29(25):3665-76. [Content Brief]
[3]. Bosch A, et al. Reversal by RARα agonist Am580 of c-Myc-induced imbalance in RARα/RARγ expression during MMTV-Myc tumorigenesis. Breast Cancer Res. 2012 Aug 24;14(4):R121. [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. 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 |
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| DMSO | 1 mM | 2.8454 mL | 14.2272 mL | 28.4544 mL | 71.1359 mL |
| 5 mM | 0.5691 mL | 2.8454 mL | 5.6909 mL | 14.2272 mL | |
| 10 mM | 0.2845 mL | 1.4227 mL | 2.8454 mL | 7.1136 mL | |
| 15 mM | 0.1897 mL | 0.9485 mL | 1.8970 mL | 4.7424 mL | |
| 20 mM | 0.1423 mL | 0.7114 mL | 1.4227 mL | 3.5568 mL | |
| 25 mM | 0.1138 mL | 0.5691 mL | 1.1382 mL | 2.8454 mL | |
| 30 mM | 0.0948 mL | 0.4742 mL | 0.9485 mL | 2.3712 mL | |
| 40 mM | 0.0711 mL | 0.3557 mL | 0.7114 mL | 1.7784 mL | |
| 50 mM | 0.0569 mL | 0.2845 mL | 0.5691 mL | 1.4227 mL | |
| 60 mM | 0.0474 mL | 0.2371 mL | 0.4742 mL | 1.1856 mL | |
| 80 mM | 0.0356 mL | 0.1778 mL | 0.3557 mL | 0.8892 mL | |
| 100 mM | 0.0285 mL | 0.1423 mL | 0.2845 mL | 0.7114 mL |
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