Tamibarotene
Based on 10 publication(s) in Google Scholar
Tamibarotene is an orally active retinoic acid receptor α (RARα) agonist, showing high selectivity over RARγ.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.54%
- No. CAS: 94497-51-5
- Fòrmula: C22H25NO3
- Peso molecular:351.44
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Publications Citing Use of MedChemExpress (MCE) Tamibarotene
More- Nat Commun. 2024 Aug 27;15(1):7263. [Abstract]
- J Exp Clin Cancer Res. 2021 Apr 26;40(1):141. [Abstract]
- Pharmacol Res. 2020 Oct:160:105149. [Abstract]
- Phytomedicine. 2021 Feb:82:153444. [Abstract]
- Leukemia. 2023 Jun;37(6):1336-1348. [Abstract]
- Int J Mol Sci. 2023 Jan 30;24(3):2586. [Abstract]
- J Pathol. 2023 Jun;260(2):203-221. [Abstract]
- IBRO Neurosci Rep. 2021 Feb 14:10:153-160. [Abstract]
- Research Square Preprint. 2024 Jan 30.
- Research Square Preprint. 2023 Nov 17.
Customer Validation & Images
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Cell Proliferation/Viability Assay
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Histological Imaging/Staining
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Cell Imaging/Staining
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WB
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Cell Proliferation/Viability Assay
Actividad biológica
Descripciòn
IC50 & Target
RARα/β[1]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HL-60 | ED50 |
7.9 x 10-10M
Compound: Am80 (3)
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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
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[PMID: 8182710] |
| HL-60 | ED50 |
7.9 x 10-10M
Compound: 3
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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] |
| HL-60 | ED50 |
7.9 x 10-10M
Compound: Am80
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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.
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[PMID: 15261256] |
| HL-60 | ED50 |
7.9 x 10-10M
Compound: Am80
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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.
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[PMID: 2329565] |
| HL-60 | IC50 |
6 μM
Compound: Tamibarotene
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Antiproliferative activity against human HL60 cells
Antiproliferative activity against human HL60 cells
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[PMID: 19443225] |
| HL-60 | IC50 |
8.94 μM
Compound: AM80
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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
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10.1007/s00044-012-0019-9 |
| HL-60 | IC50 |
8.94 μM
Compound: AM80, Tamibarotene
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Antiproliferative activity against human HL60 cells after 48 hrs by MTT assay
Antiproliferative activity against human HL60 cells after 48 hrs by MTT assay
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[PMID: 22014829] |
| Jurkat | IC50 |
17.3 μM
Compound: Tamibarotene
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Antiproliferative activity against human Jurkat cells
Antiproliferative activity against human Jurkat cells
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[PMID: 19443225] |
| K562 | IC50 |
42.37 μM
Compound: AM80
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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
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10.1007/s00044-012-0019-9 |
| K562 | IC50 |
42.37 μM
Compound: AM80, Tamibarotene
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Antiproliferative activity against human K562 cells after 48 hrs by MTT assay
Antiproliferative activity against human K562 cells after 48 hrs by MTT assay
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[PMID: 22014829] |
| MOLT-4 | IC50 |
19.5 μM
Compound: Tamibarotene
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Antiproliferative activity against human MOLT4 cells
Antiproliferative activity against human MOLT4 cells
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[PMID: 19443225] |
| NB-4 | IC50 |
4.81 μM
Compound: AM80
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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
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10.1007/s00044-012-0019-9 |
| NB-4 | IC50 |
4.81 μM
Compound: AM80, Tamibarotene
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Antiproliferative activity against human NB4 cells after 48 hrs by MTT assay
Antiproliferative activity against human NB4 cells after 48 hrs by MTT assay
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[PMID: 22014829] |
| Panel leukemia (Carcinoma cell lines) | ED50 |
7.9 x 10-10M
Compound: Am80
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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] |
| U-937 | IC50 |
20.2 μM
Compound: Tamibarotene
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Antiproliferative activity against human U937 cells
Antiproliferative activity against human U937 cells
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[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 (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.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 94497-51-5
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Appearance Solid
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Peso molecular 351.44
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Fòrmula C22H25NO3
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Color White to off-white
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SMILES
O=C(C1=CC=C(C=C1)C(NC2=CC=C3C(C)(CCC(C)(C3=C2)C)C)=O)O
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Synonyms
Am 80
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (10)
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Journal Impact Factor
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Most Recent
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Nat Commun
2024 Aug 27;15(1):7263. PMID: 39191801 -
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.
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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 -
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.
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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.
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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 -
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 -
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Solvente y solubilidad
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.
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)
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.
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.
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:
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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.
Pureza y Documentación
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Ficha de datos (281 KB)
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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)
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Instrucciones de manejo (2659 KB)
Referencias
[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]
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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