Isotretinoin
Based on 14 publication(s) in Google Scholar
Isotretinoin (13-cis-Retinoic acid) is an orally active vitamin A derivative and is often be used for the research of severe acne. Isotretinoin also shows anticancer activity.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.90%
- No. CAS: 4759-48-2
- Fòrmula: C20H28O2
- Peso molecular:300.44
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Almacenamiento:
-20°C, protect from light, stored under nitrogen
* The compound is unstable in solutions, freshly prepared is recommended.
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
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Publications Citing Use of MedChemExpress (MCE) Isotretinoin
More- Nat Commun. 2025 Feb 28;16(1):2036. [Abstract]
- Proc Natl Acad Sci U S A. 2021 Jan 12;118(2):e2009539118. [Abstract]
- Br J Cancer. 2024 Sep;131(4):763-777. [Abstract]
- Drug Des Devel Ther. 2026 Feb 18:20:585422. [Abstract]
- Cell Rep Methods. 2023 Oct 23;3(10):100599. [Abstract]
- Eur J Pharmacol. 2019 May 15:851:174-185. [Abstract]
- Cell Oncol (Dordr). 2023 Dec;46(6):1763-1775. [Abstract]
- Neuromolecular Med. 2025 May 2;27(1):32. [Abstract]
- Adv Biol (Weinh). 2025 Jul 18:e00730. [Abstract]
- Fundam Clin Pharmacol. 2020 Jun;34(3):380-388. [Abstract]
- J Pediatr Surg. 2025 Feb;60(2):161679. [Abstract]
- University of Michigan. 2026.
- bioRxiv. 2025 Jul 2:2025.07.01.662644. [Abstract]
- bioRxiv. 2025 Jul 12:2025.07.08.663754. [Abstract]
Customer Validation & Images
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In Vivo Efficacy Study
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Cell Proliferation/Viability Assay
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Cell Imaging/Staining
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RT-PCR
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Cell Proliferation/Viability Assay
Ver todos los productos específicos de isoformas Endogenous Metabolite
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Actividad biológica
Descripciòn
IC50 & Target
[2]|
Human Endogenous Metabolite |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
35.8 μM
Compound: 3, 13-cis-RA
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Cytotoxicity against human A549 cells after 24 hrs by MTT assay
Cytotoxicity against human A549 cells after 24 hrs by MTT assay
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[PMID: 19231037] |
| BEL-7404 tumor cell line | IC50 |
42.6 μM
Compound: 3, 13-cis-RA
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Cytotoxicity against human Bel7404 cells after 24 hrs by MTT assay
Cytotoxicity against human Bel7404 cells after 24 hrs by MTT assay
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[PMID: 19231037] |
| F9 | ED50 |
3.0 x 10-10M
Compound: 2a
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Ability to induce differentiation of mouse F9 embryonal carcinoma cells.
Ability to induce differentiation of mouse F9 embryonal carcinoma cells.
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[PMID: 2836589] |
| HL-60 | ED50 |
100 nM
Compound: 2
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Compound was evaluated for the retinoid-induced differentiation of the human myeloid leukemia cell line HL-60 using trans-retinoic acid as the standard.
Compound was evaluated for the retinoid-induced differentiation of the human myeloid leukemia cell line HL-60 using trans-retinoic acid as the standard.
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[PMID: 1992144] |
| HL-60 | ED50 |
5.9 x 10-9M
Compound: 2
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Concentration required for 50% inhibition of differentiation-inducing activity against human promyelocytic leukemia cell line HL-60
Concentration required for 50% inhibition of differentiation-inducing activity against human promyelocytic leukemia cell line HL-60
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[PMID: 1738149] |
In Vitro
Isotretinoin (13-cis-Retinoic acid) may act as a pro-drug that is converted intracellularly to metabolites that are agonists for RAR and RXR nuclear receptors[1].
Isotretinoin is highly sensitive to air, heat, and light[3].
Isotretinoin (0-40 μM; 24-96 h) significantly inhibits HepG2 cell viability[4].
Isotretinoin (10 μM; 48 h) down-regulates c-MYC mRNA expression and this is partially due to P1 or P2 promoter activity[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HepG2
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Concentration:0.1, 0.5, 1, 5, 10, 20, and 40 μM
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Incubation Time:24, 48, 72, and 96 h
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Result:Showed a significant reduction in cell viability (less than 30%) at 96 h for all doses.
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Cell Line:HepG2
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Concentration:10 µM
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Incubation Time:48 h
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Result:Significantly reduced the expression of c-MYC mRNA by ~80%.
In Vivo
Isotretinoin accelerates alveolar repair after exodontia in rats[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male A/J mice, lung carcinogenesis model[2]
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Dosage:1.3, 20.7, or 481 μg/L
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Administration:Inhalation exposure, 45 min daily for 2 weeks
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Result:Reduced the tumor multiplicity. Caused up-regulation of lung tissue nuclear retinoic acid receptors (RARs) relative to vehicle-exposed mice, RARα (3.9-fold vehicle), RARβ (3.3-fold), and RARγ (3.7-fold) at 20.7 μg/L.
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Animal Model:Wistar rats, tooth extraction model[3]
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Dosage:7.5 mg/kg
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Administration:Oral gavage, daily for 30 days
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Result:Accelerated the process of alveolar repair, significantly decreased serum calcium levels.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 4759-48-2
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Appearance Solid
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Peso molecular 300.44
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Fòrmula C20H28O2
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Color Yellow to orange
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SMILES
CC1(C)C(/C=C/C(C)=C/C=C/C(C)=C\C(O)=O)=C(C)CCC1
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Synonyms
13-cis-Retinoic acid
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Structure Classification
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Initial Source
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
-20°C, protect from light, stored under nitrogen
* The compound is unstable in solutions, freshly prepared is recommended.
Publications (14)
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Journal Impact Factor
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Most Recent
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Nat Commun
Bone morphogenetic protein (BMP) signaling determines neuroblastoma cell fate and sensitivity to retinoic acid. [Abstract]2025 Feb 28;16(1):2036. PMID: 40021625 -
Proc Natl Acad Sci U S A
2021 Jan 12;118(2):e2009539118. PMID: 33376206 -
Br J Cancer
Synergy of retinoic acid and BH3 mimetics in MYC(N)-driven embryonal nervous system tumours. [Abstract]2024 Sep;131(4):763-777. PMID: 38942989
Isotretinoin purchased from MedChemExpress. Usage Cited in: Br J Cancer. 2024 Sep;131(4):763-777. [Abstract]
Representative zebrafish embryo xenograft images before (Day1) and after 48h (Day3) of treatment and corresponding waterfall plots representing the change from baseline growth of individual NB-S-124 zebrafish embryo neuroblastoma xenografts treated with DMSO (blue), Isotretinoin (500 nM) (red), navitoclax (10 μM) (green), and combination (yellow) for 48 h.
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Drug Des Devel Ther
Untargeted Metabolomics Investigating the Intracellular Metabolic Alterations of HaCaT Cells Treated with Isotretinoin. [Abstract]2026 Feb 18:20:585422. PMID: 41737990 -
Cell Rep Methods
RECOVER identifies synergistic drug combinations in vitro through sequential model optimization. [Abstract]2023 Oct 23;3(10):100599. PMID: 37797618 -
Eur J Pharmacol
Adapalene suppressed the proliferation of melanoma cells by S-phase arrest and subsequent apoptosis via induction of DNA damage. [Abstract]2019 May 15:851:174-185. PMID: 30836068
Isotretinoin purchased from MedChemExpress. Usage Cited in: Eur J Pharmacol. 2019 May 15:851:174-185. [Abstract]
Isotretinoin (2.5-40 μM; 72 h) exhibited strong cytotoxic effects on the proliferation of M14 cells.
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Cell Oncol (Dordr)
Targeting TRIM24 promotes neuroblastoma differentiation and decreases tumorigenicity via LSD1/CoREST complex. [Abstract]2023 Dec;46(6):1763-1775. PMID: 37466744
Isotretinoin purchased from MedChemExpress. Usage Cited in: Cell Oncol (Dordr). 2023 Dec;46(6):1763-1775. [Abstract]
Isotretinoin (RA) (1-10 μM; 7 d) treatment reduced cell viability in SK-NBE(2) and SH-SY5Y cells.
Isotretinoin purchased from MedChemExpress. Usage Cited in: Cell Oncol (Dordr). 2023 Dec;46(6):1763-1775. [Abstract]
The morphology changes and quantification of neurite lengths of SK-N-BE(2) cells after TRIM24 KO in the absence or presence of Isotretinoin (RA) (10 μM; 7 d).
Isotretinoin purchased from MedChemExpress. Usage Cited in: Cell Oncol (Dordr). 2023 Dec;46(6):1763-1775. [Abstract]
qRT-PCR analysis of the mRNA levels of neural differentiation marker genes upon Isotretinoin (RA) (10 μM; 7 d) treatment in control and TRIM24-KO SK-N-BE(2) cells. Isotretinoin (RA) upregulated the expression of neural differentiation marker genes.
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Neuromolecular Med
Spatiotemporal Expression of IRS-1 During Brain Development and its Role in Neural Stem Cell Differentiation. [Abstract]2025 May 2;27(1):32. PMID: 40314831 -
Adv Biol (Weinh)
2025 Jul 18:e00730. PMID: 40679030 -
Fundam Clin Pharmacol
The third-generation retinoid adapalene triggered DNA damage to induce S-phase arrest in HaCat cells. [Abstract]2020 Jun;34(3):380-388. PMID: 31808972 -
J Pediatr Surg
2025 Feb;60(2):161679. PMID: 39266386 -
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bioRxiv
KAT6A/B inhibition synergizes with retinoic acid and enhances the efficacy of GD2-targeted immunotherapy in neuroblastoma. [Abstract]2025 Jul 2:2025.07.01.662644. PMID: 40631259 -
bioRxiv
2025 Jul 12:2025.07.08.663754. PMID: 40672312
Solvente y solubilidad
In Vitro:
DMSO : 140 mg/mL (465.98 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.
Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.
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 (8.32 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 (8.32 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
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. * The compound is unstable in solutions, freshly prepared is recommended.
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 (278 KB)
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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)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Layton A. The use of isotretinoin in acne. Dermatoendocrinol. 2009 May;1(3):162-9. [Content Brief]
[2]. Dahl AR, et al. Inhaled isotretinoin (13-cis retinoic acid) is an effective lung cancer chemopreventive agent in A/J mice at low doses: a pilot study. Clin Cancer Res. 2000 Aug;6(8):3015-24 [Content Brief]
[3]. Bergoli RD, et al. Isotretinoin effect on alveolar repair after exodontia--a study in rats. Oral Maxillofac Surg. 2011 Jun;15(2):85-92. [Content Brief]
[4]. Ramírez-Flores PN, et al. Isotretinoin and Thalidomide Down-Regulate c-MYC Gene Expression and Modify Proteins Associated with Cancer in Hepatic Cells. Molecules. 2021 Sep 22;26(19):5742. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.3285 mL | 16.6423 mL | 33.2845 mL | 83.2113 mL |
| 5 mM | 0.6657 mL | 3.3285 mL | 6.6569 mL | 16.6423 mL | |
| 10 mM | 0.3328 mL | 1.6642 mL | 3.3285 mL | 8.3211 mL | |
| 15 mM | 0.2219 mL | 1.1095 mL | 2.2190 mL | 5.5474 mL | |
| 20 mM | 0.1664 mL | 0.8321 mL | 1.6642 mL | 4.1606 mL | |
| 25 mM | 0.1331 mL | 0.6657 mL | 1.3314 mL | 3.3285 mL | |
| 30 mM | 0.1109 mL | 0.5547 mL | 1.1095 mL | 2.7737 mL | |
| 40 mM | 0.0832 mL | 0.4161 mL | 0.8321 mL | 2.0803 mL | |
| 50 mM | 0.0666 mL | 0.3328 mL | 0.6657 mL | 1.6642 mL | |
| 60 mM | 0.0555 mL | 0.2774 mL | 0.5547 mL | 1.3869 mL | |
| 80 mM | 0.0416 mL | 0.2080 mL | 0.4161 mL | 1.0401 mL | |
| 100 mM | 0.0333 mL | 0.1664 mL | 0.3328 mL | 0.8321 mL |
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