2. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor Autophagy Apoptosis
  3. RAR/RXR Autophagy Apoptosis
  4. Adapalene

Adapalene (CD271), a third-generation synthetic retinoid, is widely used for the research of acne. Adapalene is a potent RAR agonist, with AC50s of 2.3 nM, 9.3 nM, and 22 nM for RARβ, RARγ, RARα, respectively. Adapalene also inhibits the enzymatic activity of GOT1 in a non-competitive manner. Adapalene exhibits anti-tumor activity.

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Adapalene Chemical Structure

Adapalene Chemical Structure

CAS No. : 106685-40-9

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Based on 4 publication(s) in Google Scholar

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Adapalene Related Antibodies

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Description

Adapalene (CD271), a third-generation synthetic retinoid, is widely used for the research of acne. Adapalene is a potent RAR agonist, with AC50s of 2.3 nM, 9.3 nM, and 22 nM for RARβ, RARγ, RARα, respectively. Adapalene also inhibits the enzymatic activity of GOT1 in a non-competitive manner. Adapalene exhibits anti-tumor activity[1][2][3].

IC50 & Target

AC50: 2.3 nM (RARβ), 9.3 nM (RARγ), and 22 nM (RARα)[1]
In Vitro

Adapalene (1-200 μM; 24 h) 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[2].
Adapalene (10-40 μM; 24 h) induces ES-2 cells apoptosis and inhibits proliferation in vitro[2].
Adapalene (3-30 μM; 6-24 h) significantly increases the G1-phase population in LoVo or DLD1 cells[3].
Adapalene (1-200 μM) inhibits GOT1 activity, with an IC50 of 21.79 μM[2].
Adapalene (10-6-10-3 nM) inhibits the expression of plasma membrane-associated enzyme transglutaminase Type I, with an IC50 of 2.5 nM[1].

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

Adapalene Related Antibodies

Cell Viability Assay[2]

Cell Line: Pancreatic cancer (SW1990, Aspc-1), breast cancer (mm-231, mm-468, MCF-7), liver cancer (Hep3B), cervical cancer (Hela), ovarian cancer (HOV-7, ES-2), normal cells (CHO, L929)
Concentration: 1-200 μM
Incubation Time: 24 hours
Result: Inhibited the viability of cancer cells with higher GOT1 protein expression.

Apoptosis Analysis[2]

Cell Line: ES-2 cells[2]
Concentration: 10, 20, 40 μM
Incubation Time: 24 hours
Result: Showed a significant increase in apoptosis compared with the control group.
Down regulated the expression of anti-apoptotic protein Bcl-2 and PARP.

Cell Cycle Analysis[3]

Cell Line: LoVo or DLD1 cells
Concentration: 3, 10, 30 μM
Incubation Time: 6, 12, 24 hours
Result: Caused cell cycle arrest in G1 phase in a dose- and time-dependent manner.
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[3].

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

Animal Model: Female BALB/C nude mice (15 g, 4-5 weeks) were injected with DLD1 cells[3]
Dosage: 15, 20, 65, 100 mg/kg
Administration: P.o. daily for 21 days
Result: Significantly reduced tumor weight and volume.
Clinical Trial
Molecular Weight

412.52

Formula

C28H28O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

COC1=C(C23CC4CC(C3)CC(C2)C4)C=C(C5=CC6=C(C=C(C(O)=O)C=C6)C=C5)C=C1
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
Solvent & Solubility
In Vitro: 

DMSO : 10 mg/mL (24.24 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4241 mL 12.1206 mL 24.2412 mL
5 mM 0.4848 mL 2.4241 mL 4.8482 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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Concentration (final)

C2

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Volume (final)

V2

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.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: 1 mg/mL (2.42 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 1 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 (10.0 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 1 mg/mL (2.42 mM); Clear solution

    This protocol yields a clear solution of ≥ 1 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 (10.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation

Purity: 99.98%

COA (249 KB) RP-HPLC (277 KB)

Handling Instructions (2659 KB)
References

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 2.4241 mL 12.1206 mL 24.2412 mL 60.6031 mL
5 mM 0.4848 mL 2.4241 mL 4.8482 mL 12.1206 mL
10 mM 0.2424 mL 1.2121 mL 2.4241 mL 6.0603 mL
15 mM 0.1616 mL 0.8080 mL 1.6161 mL 4.0402 mL
20 mM 0.1212 mL 0.6060 mL 1.2121 mL 3.0302 mL
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Adapalene Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Adapalene106685-40-9CD271CD 271CD-271RAR/RXRAutophagyApoptosisRetinoic acid receptorsRetinoid X receptorsretinoidacneRARRARβRARγRARαGOT1tumorInhibitorinhibitorinhibit

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