2. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor Autophagy Apoptosis
  3. RAR/RXR Autophagy Apoptosis
  4. Tamibarotene

Tamibarotene is an orally active retinoic acid receptor α (RARα) agonist, showing high selectivity over RARγ.

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

CAS No. : 94497-51-5

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Customer Review

Based on 10 publication(s) in Google Scholar

Other Forms of Tamibarotene:

Tamibarotene Related Antibodies

Top Publications Citing Use of Products

    Tamibarotene purchased from MedChemExpress. Usage Cited in: Leukemia. 2023 Jun;37(6):1336-1348.  [Abstract]

    Percent CD11b-positive differentiated OCI-AML3 cells following three days of KO of mtNPM1 and then treatment with the indicated concentrations of SY-1425 (Tamibarotene) for 96 h.

    Tamibarotene purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2023 Jan 30;24(3):2586.

    Tamibarotene (5 mg/kg). A representative photomicrograph of a coronal section of the rat brain at week 7 (0.6 mm from the anterior fontanelle), showing the ventricular volume.

    Tamibarotene purchased from MedChemExpress. Usage Cited in: Pharmacol Res. 2020 Oct;160:105149.  [Abstract]

    Tamibarotene (AM80 2.5 nM). SSD-treated cells were collected and stained with Giemsa solution.

    Tamibarotene purchased from MedChemExpress. Usage Cited in: Pharmacol Res. 2020 Oct;160:105149.  [Abstract]

    Tamibarotene (AM80 2.5 nM). GAPDH was used as an internal control gene. PU.1 protein levels were detected by Western blotting.

    Tamibarotene purchased from MedChemExpress. Usage Cited in: Pharmacol Res. 2020 Oct;160:105149.  [Abstract]

    Tamibarotene (AM80 2.5 nM). SSD-induced bactericidal activity. Cells were treated with SSD for 5 days, followed by bactericidal experiments.

    View All RAR/RXR Isoform Specific Products:

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    RXRα RXRβ RXRγ

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Tamibarotene is an orally active retinoic acid receptor α (RARα) agonist, showing high selectivity over RARγ.

    IC50 & Target

    RARα/β[1]
    Cellular Effect
    Cell Line Type Value Description References
    HL-60 ED50
    7.9 x 10-10 M
    Compound: 3
    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]
    HL-60 ED50
    7.9 x 10-10 M
    Compound: Am80
    Effective concentration required for induction of differentiation of HL-60 cells into mature granulocytes.
    Effective concentration required for induction of differentiation of HL-60 cells into mature granulocytes.
    		[PMID: 15261256]
    HL-60 ED50
    7.9 x 10-10 M
    Compound: Am80
    Ability to induce differentiation of human promyelocytic leukemia cell line HL-60 to mature granulocytes.
    Ability to induce differentiation of human promyelocytic leukemia cell line HL-60 to mature granulocytes.
    		[PMID: 2329565]
    HL-60 ED50
    7.9 x 10-10 M
    Compound: Am80 (3)
    The ability to induce differentiation of human promyelocytic leukemia cell line HL-60 to mature granulocytes was determined by nitro blue tetrazolium (NBT) reduction assay
    The ability to induce differentiation of human promyelocytic leukemia cell line HL-60 to mature granulocytes was determined by nitro blue tetrazolium (NBT) reduction assay
    		[PMID: 8182710]
    HL-60 IC50
    6 μM
    Compound: Tamibarotene
    Antiproliferative activity against human HL60 cells
    Antiproliferative activity against human HL60 cells
    		[PMID: 19443225]
    HL-60 IC50
    8.94 μM
    Compound: AM80
    Cytotoxicity against Homo sapiens (human) HL60 cells assessed as growth inhibition after 48 hr by MTT assay
    Cytotoxicity against Homo sapiens (human) HL60 cells assessed as growth inhibition after 48 hr by MTT assay
    		10.1007/s00044-012-0019-9
    HL-60 IC50
    8.94 μM
    Compound: AM80, Tamibarotene
    Antiproliferative activity against human HL60 cells after 48 hrs by MTT assay
    Antiproliferative activity against human HL60 cells after 48 hrs by MTT assay
    		[PMID: 22014829]
    Jurkat IC50
    17.3 μM
    Compound: Tamibarotene
    Antiproliferative activity against human Jurkat cells
    Antiproliferative activity against human Jurkat cells
    		[PMID: 19443225]
    K562 IC50
    42.37 μM
    Compound: AM80
    Cytotoxicity against Homo sapiens (human) K562 cells assessed as growth inhibition after 48 hr by MTT assay
    Cytotoxicity against Homo sapiens (human) K562 cells assessed as growth inhibition after 48 hr by MTT assay
    		10.1007/s00044-012-0019-9
    K562 IC50
    42.37 μM
    Compound: AM80, Tamibarotene
    Antiproliferative activity against human K562 cells after 48 hrs by MTT assay
    Antiproliferative activity against human K562 cells after 48 hrs by MTT assay
    		[PMID: 22014829]
    MOLT-4 IC50
    19.5 μM
    Compound: Tamibarotene
    Antiproliferative activity against human MOLT4 cells
    Antiproliferative activity against human MOLT4 cells
    		[PMID: 19443225]
    NB-4 IC50
    4.81 μM
    Compound: AM80
    Cytotoxicity against Homo sapiens (human) NB4 cells assessed as growth inhibition after 48 hr by MTT assay
    Cytotoxicity against Homo sapiens (human) NB4 cells assessed as growth inhibition after 48 hr by MTT assay
    		10.1007/s00044-012-0019-9
    NB-4 IC50
    4.81 μM
    Compound: AM80, Tamibarotene
    Antiproliferative activity against human NB4 cells after 48 hrs by MTT assay
    Antiproliferative activity against human NB4 cells after 48 hrs by MTT assay
    		[PMID: 22014829]
    Panel leukemia (Carcinoma cell lines) ED50
    7.9 x 10-10 M
    Compound: Am80
    Effective dose for differentiation -inducing activity against human promyelocytic leukemia cells
    Effective dose for differentiation -inducing activity against human promyelocytic leukemia cells
    		[PMID: 3184125]
    U-937 IC50
    20.2 μM
    Compound: Tamibarotene
    Antiproliferative activity against human U937 cells
    Antiproliferative activity against human U937 cells
    		[PMID: 19443225]
    In Vitro

    Tamibarotene (20, 40 μM) down-regulates expression of cell cycle gene in T-cell lymphoma cells. Tamibarotene (5 μM) increases RARE activity in RARA-overexpressing cells to a much greater degree than in RARAlow cells. Moreover, RARAwt overexpression augments the degree of CDK2, CDK4, and CDK6 inhibition caused by Tamibarotene treatment[1].
    Tamibarotene directly reverses the profibrotic phenotype of transforming growth factor-β1-treated dermal fibroblasts, suppresses ICAM-1 expression in endothelial cells, and promots M1 macrophage differentiation in vitro[2].
    Tamibarotene (4 μM) up-regulates apelin mRNA and protein levels dose-dependently in VSMCs. Upon Tamibarotene stimulation, the RARα (retinoic acid receptor α) is recruited to the apelin promoter by interacting with KLF5 and Sp1 prebound to the TCE site of the apelin promoter to form a transcriptional activation complex, subsequently leading to the up-regulation of apelin expression in VSMCs. KLF5 and Sp1 co-operatively mediate Tamibarotene-induced apelin expression through their direct binding to the TCE on the apelin promoter[4].

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

    Tamibarotene Related Antibodies
    In Vivo

    Tamibarotene (1 mg/kg/day) significantly attenuates dermal and hypodermal fibrosis in bleomycin (BLM)-treated mice and tight skin 1 mice, respectively. Consistently, Tamibarotene significantly suppresses the expression of various molecules related to tissue fibrosis, including transforming growth factor-β1, connective tissue growth factor, IL-4, IL-10, IL-13, IL-17A, tumor necrosis factor-α, IFN-γ, and monocyte chemotactic protein 1 in the lesional skin of BLM-treated mice. Furthermore, Tamibarotene decreases the proportion of effector T cells, while increasing that of naive T cells among CD4+ T cells in the draining lymph nodes of BLM-treated mice[2].
    Tamibarotene (2.5 mg/kg, p.o.) does not result in any significant alteration of the AST, ALT, or ALP serum levels in periodontitis-challenged mice compared with that in untreated mice. Tamibarotene ameliorates alveolar bone resorption, significantly reduces the number of P. gingivalis-induced osteoclasts in mice. Tamibarotene measurably increases the percentage of CD4+ Foxp3+ Treg cells as compared to those in EPD mice. Tamibarotene is also effective in reducing the expression of CD4+ROR-γt+ (Th17) cells in P. gingivalis-infected gingival tissues and CLNs[3].
    Tamibarotene (1 mg/kg, p.o.) increases apelin expression in balloon-injured arteries of rats, consistent with the results from the cultured VSMCs[4]. In aged SAMP8 mice, hippocampal ADAM10 levels improve after Tamibarotene (1 mg/kg/day) administration. Hes5 and Ki67 are restored and spatial working memory also improves after Tamibarotene administration[5].

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

    351.44

    Formula

    C22H25NO3
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(C1=CC=C(C=C1)C(NC2=CC=C3C(C)(CCC(C)(C3=C2)C)C)=O)O
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 100 mg/mL (284.54 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" 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
    View the 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.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
    =
    Concentration
    ×
    Volume
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    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

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    Volume (final)

    V2

    In Vivo:

    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.

    • 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.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in 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 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.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    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).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    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.
    Purity & Documentation

    Purity: 99.57%

    SDS (396 KB)

    COA (248 KB) LCMS (267 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay
    [1]

    The CellTiter Aqueous Non-Radioactive Cell Proliferation Assay Kit is used to assess cell growth. Briefly, 10,000 cells per well are seeded in a 96-well plate and cultured in RPMI containing 2% charcoal-stripped FBS and indicated retinoid concentrations for 72 hours. At the end of the treatment period, the MTS reagent is added, cells are incubated an additional 2-4 hours, and absorbance is measured at 490 nanometers.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [3]

    For the infection, mice are given sulfamethoxazole and trimethoprim in an oral suspension at 10 mL of deionized water ad libitum for 10 days to reduce the native flora and to support colonization of P. gingivalis W83. Four days after the antibiotic therapy finishes, periodontal infection is established through oral inoculation using 1010 colony-forming units of P. gingivalis suspended in 100 μL 4% carboxymethyl cellulose (CMC) for 7 days. The mice are euthanized 4 weeks after the first oral inoculation. Tamibarotene (2.5 mg/kg) is suspended in a 0.5% carboxymethyl cellulose solution. The drug is orally gavaged into the esophagus daily in a volume of 0.1 mL/10 g body weight. Tamibarotene is administered 1 h before the induction of periodontitis and then given daily per the protocol until day 28. Control mice with periodontal disease receive the same volume of 0.5% carboxymethyl cellulose solution. The body weight of each mouse is measured every 3 days.

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

    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
    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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    Tamibarotene Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Tamibarotene94497-51-5Am 80Am80Am-80RAR/RXRAutophagyApoptosisRetinoic acid receptorsRetinoid X receptorsInhibitorinhibitorinhibit

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