Cat. No.: HY-14652

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Tamibarotene

(Synonyms: Am 80)

10 Cited Publications

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Based on 10 publication(s) in Google Scholar

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.

Purity: 99.54%
CAS No.: 94497-51-5
Formula: C₂₂H₂₅NO₃
Molecular Weight:351.44

Storage:

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

Tamibarotene Chemical Structure

CAS No.: 94497-51-5

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (10)
Solvent & Solubility
- In Vitro
- In Vivo
Protocol
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

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

IC₅₀ & Target

RARα/β^[1]

All RAR/RXR Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
HL-60	ED₅₀	7.9 x 10^-10M 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	ED₅₀	7.9 x 10^-10M 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^-10M 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^-10M 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	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^-10M 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.

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

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 94497-51-5
Appearance Solid
Molecular Weight 351.44
Formula C₂₂H₂₅NO₃
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
Synonyms

Am 80
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

Publications (10)

All Cell Imaging/StainingHistological Imaging/StainingWBCell Proliferation/Viability Assay

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Journal Impact Factor

Nat Commun

RNA nanotherapeutics with fibrosis overexpression and retention for MASH treatment. [Abstract]

2024 Aug 27;15(1):7263. PMID: 39191801
Leukemia

Causal linkage of presence of mutant NPM1 to efficacy of novel therapeutic agents against AML cells with mutant NPM1. [Abstract]

2023 Jun;37(6):1336-1348. PMID: 36977823

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.
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
Pharmacol Res

Saikosaponin d contributed to cancer chemotherapy induced neutropenia therapy by promoting neutrophil differentiation via activation CBL-dependent ERK pathway. [Abstract]

2020 Oct;160:105149. PMID: 32822868

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.
Phytomedicine

Saikosaponin a contributed to CCIN treatment by promoting neutrophil bactericidal activity via activation CBL-dependent ERK pathway. [Abstract]

2021 Feb:82:153444. PMID: 33421903
J Pathol

Novel prognostication biomarker adipophilin reveals a metabolic shift in uveal melanoma and new therapeutic opportunities. [Abstract]

2023 Jun;260(2):203-221. PMID: 36825655
Int J Mol Sci

Activation of the RARα Attenuated CSF Hypersecretion to Inhibit Hydrocephalus Development via Regulating the MAFB/MSR1 Pathway. [Abstract]

2023 Jan 30;24(3):2586. PMID: 36768908

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

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.
IBRO Neurosci Rep

Reduction BACE1 expression via suppressing NF-κB mediated signaling by Tamibarotene in a mouse model of Alzheimer's disease. [Abstract]

2021 Feb 14:10:153-160. PMID: 33842919
Research Square Preprint

2024 Jan 30.
Research Square Preprint

2023 Nov 17.

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.

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.

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

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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% (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.

Protocol 3

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

Protocol

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.

MedChemExpress (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.

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 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)

References

[1]. Wang X, et al. Retinoic acid receptor alpha drives cell cycle progression and is associated with increased sensitivity to retinoids in T-cell lymphoma. Oncotarget. 2017 Apr 18;8(16):26245-26255. [Content Brief]

[2]. Toyama T, et al. Tamibarotene Ameliorates Bleomycin-Induced Dermal Fibrosis by Modulating Phenotypes of Fibroblasts, Endothelial Cells, and Immune Cells. J Invest Dermatol. 2016 Feb;136(2):387-98. [Content Brief]

[3]. Jin Y, et al. Tamibarotene modulates the local immune response in experimental periodontitis. Int Immunopharmacol. 2014 Dec;23(2):537-45. [Content Brief]

[4]. Lv XR, et al. Synthetic retinoid Am80 up-regulates apelin expression by promoting interaction of RARα with KLF5 and Sp1 in vascular smooth muscle cells. Biochem J. 2013 Nov 15;456(1):35-46. [Content Brief]

[5]. Kitaoka K, et al. The retinoic acid receptor agonist Am80 increases hippocampal ADAM10 in aged SAMP8 mice. Neuropharmacology. 2013 Sep;72:58-65. [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

Tamibarotene

10 Cited Publications

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Publications Citing Use of MedChemExpress (MCE) Tamibarotene

All RAR/RXR Isoforms

Biological Activity

Chemical Information

Publications (10)

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Tamibarotene Related Classifications

Cat. No.: HY-14652