1. Metabolic Enzyme/Protease
    Autophagy
  2. RAR/RXR
    Autophagy
  3. AM580

AM580 (Synonyms: CD336; NSC608001; Ro 40-6055)

Cat. No.: HY-10475 Purity: 99.46%
Handling Instructions

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

For research use only. We do not sell to patients.

AM580 Chemical Structure

AM580 Chemical Structure

CAS No. : 102121-60-8

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
5 mg USD 60 In-stock
Estimated Time of Arrival: December 31
10 mg USD 90 In-stock
Estimated Time of Arrival: December 31
50 mg USD 370 In-stock
Estimated Time of Arrival: December 31
100 mg USD 650 In-stock
Estimated Time of Arrival: December 31
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500 mg   Get quote  

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Customer Review

Based on 2 publication(s) in Google Scholar

Top Publications Citing Use of Products

    AM580 purchased from MCE. Usage Cited in: Biochem Biophys Res Commun. 2020 May 28;S0006-291X(20)30984-0.

    After dealing with 10 nM AM580 for 3 days, the expression of RARβ is detected by immunobloting and quantified.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

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

    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].

    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].

    Molecular Weight

    351.44

    Formula

    C₂₂H₂₅NO₃

    CAS No.

    102121-60-8

    SMILES

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

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 45 mg/mL (128.04 mM)

    H2O : < 0.1 mg/mL (insoluble)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    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.
    In Vivo:
    • 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

    • 2.

      Add each solvent one by one:  10% DMSO    90% corn oil

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

    *All of the co-solvents are provided by MCE.
    References
    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.

    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.

    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.

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

    References

    Purity: 99.46%

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    Keywords:

    AM580CD336NSC608001Ro 40-6055AM 580AM-580CD 336CD-336NSC 608001NSC-608001RAR/RXRAutophagyRetinoic acid receptorsRetinoid X receptorsInhibitorinhibitorinhibit

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    Product name:
    AM580
    Cat. No.:
    HY-10475
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