Adapalene is a third-generation topical retinoid, it is a potent RAR agonist, with AC50 values of 2.3 nM, 9.3 nM, and 22 nM for RARβ, RARγ, RARα, respectively. Adapalene inhibits the viability of ES-2, HOV-7, MCF-7 , Hela, SW1990, HT1080, and MM-468 cells, with IC50s of 10.36 μM, 10.81 μM, 12.00 μM, 19.08 μM, 19.52 μM, 21.70 μM, and 31.47 μM, respectively Adapalene also inhibits the enzymatic activity of GOT1 in a non-competitive manner. Adapalene inhibits proliferation and induces apoptosis in colorectal cancer cell in vitro.
In vivo, Adapalene (15-100 mg/kg; p.o. daily for 21 days) inhibits the growth of DLD1 cell-derived xenograft tumors in BALB/C nude mice.
Front Pharmacol. 2022 Feb 22;13:801624.
Adapalene Inhibits Prostate Cancer Cell Proliferation In Vitro and In Vivo by Inducing DNA Damage, S-phase Cell Cycle Arrest, and Apoptosis
Adapalene purchased from AbMole
Molecular Weight | 412.52 |
Formula | C28H28O3 |
CAS Number | 106685-40-9 |
Solubility (25°C) | DMSO 10 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[1] Aura Rusu, et al. Recent Advances Regarding the Therapeutic Potential of Adapalene
[2] No authors listed. Adapalene
[4] Leila Tolaymat, et al. Adapalene
[5] S Jain. Topical tretinoin or adapalene in acne vulgaris: an overview
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