| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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Purity: ≥98%
Isotretinoin (Accutane; Myorisan; Zenatane; 13-cis retinoic acid) is a topically used medication approved for the treatment of severe cystic acne. It was originally developed to be used as a chemotherapeutic drug for the treatment of various cancers such as brain cancer, pancreatic cancer etc. Isotretinoin directly interferes with the development of cranial neural crest cells. Isotretinoin selectively affects neural crest cells by decreasing their cell-substratum adhesion. Isotretinoin (500 ng/mL) and its main metabolite in the human, 4-oxo-isotretinoin, induce malformations similar to those seen in vivo.
| ln Vitro |
As a prodrug, isotretinoin (13-cis-retinoic acid) is transformed intracellularly into metabolites that agonistically bind to the nuclear receptors RAR and RXR [1]. The sensitivity of isotretinoin to light, heat, and air is quite great [3]. HepG2 cell viability is considerably inhibited by isotretinoin (0–40 μM; 24-96 hours) [4]. P1 or P2 promoter activity contributes to the downregulation of c-MYC mRNA expression caused by isotretinoin (10 μM; 48 hours) [4].
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| ln Vivo |
When administered inhalation for 45 minutes daily for two weeks, isotretinoin (1.3–481 μg/L; also known as 13-cis-retinoiic acid) can effectively prevent lung cancer in A/J mice [2]. In rats, isotretinoin speeds up alveolar healing following tooth extraction [3].
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| Cell Assay |
Cell Viability Assay[4]
Cell Types: HepG2 Tested Concentrations: 0.1, 0.5, 1, 5, 10, 20, and 40 μM Incubation Duration: 24, 48, 72, and 96 h Experimental Results: demonstrated a significant reduction in cell viability (less than 30%) at 96 h for all doses. RT-PCR[4] Cell Types: HepG2 Tested Concentrations: 10 µM Incubation Duration: 48 h Experimental Results: Dramatically decreased the expression of c-MYC mRNA by ~80%. |
| Animal Protocol |
Animal/Disease Models: Male A/J mice, lung carcinogenesis model[2]
Doses: 1.3, 20.7, or 481 μg/L Route of Administration: Inhalation exposure, 45 min daily for 2 weeks Experimental Results: decreased 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. Animal/Disease Models: Wistar rats, tooth extraction model[3] Doses: 7.5 mg/kg Route of Administration: po (oral gavage), daily for 30 days Experimental Results: Accelerated the process of alveolar repair, Dramatically diminished serum calcium levels. |
| References |
[1]. Layton A. The use of isotretinoin in acne. Dermatoendocrinol. 2009 May;1(3):162-9.
[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 [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. [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. |
| Molecular Formula |
C20H28O2
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| Molecular Weight |
300.44
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| CAS # |
4759-48-2
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| Related CAS # |
Isotretinoin-d5
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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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| InChi Key |
SHGAZHPCJJPHSC-XFYACQKRSA-N
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| InChi Code |
InChI=1S/C20H28O2/c1-15(8-6-9-16(2)14-19(21)22)11-12-18-17(3)10-7-13-20(18,4)5/h6,8-9,11-12,14H,7,10,13H2,1-5H3,(H,21,22)/b9-6+,12-11+,15-8+,16-14-
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| Chemical Name |
(2Z,4E,6E,8E)-3,7-dimethyl-9-(2,6,6-trimethylcyclohex-1-en-1-yl)nona-2,4,6,8-tetraenoic acid
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.32 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (6.92 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.3285 mL | 16.6423 mL | 33.2845 mL | |
| 5 mM | 0.6657 mL | 3.3285 mL | 6.6569 mL | |
| 10 mM | 0.3328 mL | 1.6642 mL | 3.3285 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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