Art. -Nr.: HY-10475

Copy Link Print Information

AM580

(Synonyms: CD336; NSC608001; Ro 40-6055)

14 Cited Publications

Kundenbewertung

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.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit: 98.38%
CAS. Nr.: 102121-60-8
Formel: C₂₂H₂₅NO₃
Molecular Weight:351.44

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

AM580 Chemical Structure

CAS. Nr.: 102121-60-8

Größe

Preis

Verfügbarkeit

Menge

Amount: USD 0.00

* Bitte wählen Sie Menge, bevor Sie Artikel hinzufügen.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (14)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Bioz

Biologische Aktivität

Beschreibung

AM580 is a selective RARα agonist with IC₅₀ and EC₅₀ of 8 nM and 0.36 nM, respectively.

Alle RAR/RXR Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
COS-7	EC₅₀	0.3 nM Compound: AM-580	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	[PMID: 19058965]
COS-7	EC₅₀	13 nM Compound: AM-580	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	[PMID: 19058965]
COS-7	EC₅₀	8.6 nM Compound: AM-580	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	[PMID: 19058965]
HL-60	ED₅₀	3.4 x 10^-10M Compound: 5	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	[PMID: 2795600]
Panel leukemia (Carcinoma cell lines)	ED₅₀	3.4 x 10^-10M Compound: AM-580	Effective dose for differentiation -inducing activity against human promyelocytic leukemia cells Effective dose for differentiation -inducing activity against human promyelocytic leukemia cells	[PMID: 3184125]

In Vitro

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.

In Vivo

Am580 (0.3 mg/kg/day) treatment has a more profound effect on tumor-free survival of MMTV-wnt1 mice, the effect being noticeable even in early appearing tumors, and no overt toxicity is found in liver, lungs, kidney, and spleen. Am580 treatment reduces substantially and equally the level of hyperplasia in both transgenic glands^[2]. Treatment of MMTV-Myc mice with the RARα-selective agonist Am580 leads to significant inhibition of mammary tumor growth, lung metastasis and extends tumor latency in 63% of mice^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS. Nr. 102121-60-8
Appearance Solid
Molecular Weight 351.44
Formel C₂₂H₂₅NO₃
Color White to off-white
SMILES

CC(CC1)(C)C2=C(C=CC(C(NC3=CC=C(C(O)=O)C=C3)=O)=C2)C1(C)C
Synonyms

CD336; NSC608001; Ro 40-6055
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (14)

All WBCell Proliferation/Viability AssayFlow CytometryCell Imaging/Staining

Sort by:

Journal Impact Factor

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.
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.
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

Tailoring combinational therapy with Monte Carlo method-based regression modeling. [Abstract]

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

NLS-RARα blocks cell differentiation by inhibiting the retinoic acid signalling pathway. [Abstract]

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.
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

Lösungsmittel & Löslichkeit

In Vitro:

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.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.8454 mL

14.2272 mL

28.4544 mL

5 mM

0.5691 mL

2.8454 mL

5.6909 mL

10 mM

0.2845 mL

1.4227 mL

2.8454 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (7.11 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Protokoll

Kinase Assay^[1]

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.

Cell Assay^[1]

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.

Animal Administration^[1]

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.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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
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

Keywords

AM580

14 Cited Publications

100 mg Angebot einholen

Subscribe to the

MedChemExpress

Newsletter

Produktname:
Art. -Nr.:
Menge:
MCE Japan Authorized Agent:

Produktname:
CAS. Nr.:
Species:
Reinheit:
Menge:

AM580

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Autophagy Compound Library

Differentiation Inducing Compound Library

Reprogramming Compound Library

Transcription Factor-Targeted Library

Human Metabolite Library

Nuclear Receptor Compound Library

Metabolic Enzyme Compound Library

Highly Selective Activators Library

Cell Death Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Vitamin Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Publications Citing Use of MedChemExpress (MCE) AM580

Alle RAR/RXR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (14)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

AM580

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Autophagy Compound Library

Differentiation Inducing Compound Library

Reprogramming Compound Library

Transcription Factor-Targeted Library

Human Metabolite Library

Nuclear Receptor Compound Library

Metabolic Enzyme Compound Library

Highly Selective Activators Library

Cell Death Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Vitamin Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Publications Citing Use of MedChemExpress (MCE) AM580

Alle RAR/RXR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (14)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

AM580 Related Classifications

Art. -Nr.: HY-10475