2. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor Apoptosis
  3. RAR/RXR Apoptosis
  4. Ro 41-5253

Ro 41-5253 is an orally active selective retinoic acid receptor alpha (RARα) antagonist. Ro 41-5253 can bind RARα without inducing transcription or affecting RAR/RXR heterodimerization and DNA binding. Ro 41-5253 can inhibit cancer cell proliferation and induce apoptosis, has antitumor activity.

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Ro 41-5253 Chemical Structure

Ro 41-5253 Chemical Structure

CAS No. : 144092-31-9

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Based on 1 publication(s) in Google Scholar

Ro 41-5253 Related Antibodies

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Description

Ro 41-5253 is an orally active selective retinoic acid receptor alpha (RARα) antagonist. Ro 41-5253 can bind RARα without inducing transcription or affecting RAR/RXR heterodimerization and DNA binding. Ro 41-5253 can inhibit cancer cell proliferation and induce apoptosis, has antitumor activity[1][2].

IC50 & Target

IC50: 60 nM (RARα), 2.4 μM (RARβ), 3.3 μM (RARγ)[3].
In Vitro

Ro 41-5253 (1 nM-10 μM, 10 days) significantly inhibits MCF-7 and ZR 75.1 cell proliferation and induces cell apoptosis in a time and dose-dependent manner[1].

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

Ro 41-5253 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: Human breast-carcinoma lines MCF-7 and ZR 75.1
Concentration: 1 nM-10 μM
Incubation Time: 10 days
Result: Inhibited 81% MCF-7 cell growth at 10 μM, 30% cell growth at 1 μM and no significant inhibitory effect at concentrations below 0.1 μM.
Inhibited 74% ZR 75.1 cell growth at 10 μM, 63% cell growth at 1 μM and 42% cell growth at 0.1 μM.

Apoptosis Analysis[1]

Cell Line: Human breast-carcinoma lines MCF-7 and ZR 75.1
Concentration: 1 nM-10 μM
Incubation Time: 10 days
Result: Induced 28.5, 21.6, 16 and 12% of MCF-7 cells apoptosis at 10 μM, 1 μM, 0.1 μM and 0.01 μM respectively on the fourth day while induced 58, 51, 36 and 21% of cells apoptosis at 10 μM, 1 μM, 0.1 μM and 0.01 μM respectively after six days.
Induced 80, 65, 43 and 29% of ZR 75.1 cells apoptosis at 10 μM, 1 μM, 0.1 μM and 0.01 μM respectively on the sixth day.
In Vivo

Ro 41-5253 (oral gavage, 10-600 mg/kg, once a week, 4 weeks) can reduce tumor volume in female athymic Balb/mice transplanted with MCF-7 cell line[2].

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

Animal Model: Six-week-old female athymic Balb/mice transplanted with MCF-7 cell line[2]
Dosage: 10, 30, 100, 300 and 600 mg/kg
Administration: Oral gavage; once a week; 4 weeks
Result: Resulted in a reduction in tumor volume at doses of 10, 30 and 100 mg/kg with no toxic side effects.
Molecular Weight

484.65

Formula

C28H36O5S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CC=C(C=C1)/C=C(C)/C2=C(C=C3C(C(C)(CCS3(=O)=O)C)=C2)OCCCCCCC)O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (206.33 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0633 mL 10.3167 mL 20.6334 mL
5 mM 0.4127 mL 2.0633 mL 4.1267 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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • 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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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: ≥ 2.5 mg/mL (5.16 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.
  • Protocol 2

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

    Solubility: ≥ 2.5 mg/mL (5.16 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 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 (25.0 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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

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
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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0633 mL 10.3167 mL 20.6334 mL 51.5836 mL
5 mM 0.4127 mL 2.0633 mL 4.1267 mL 10.3167 mL
10 mM 0.2063 mL 1.0317 mL 2.0633 mL 5.1584 mL
15 mM 0.1376 mL 0.6878 mL 1.3756 mL 3.4389 mL
20 mM 0.1032 mL 0.5158 mL 1.0317 mL 2.5792 mL
25 mM 0.0825 mL 0.4127 mL 0.8253 mL 2.0633 mL
30 mM 0.0688 mL 0.3439 mL 0.6878 mL 1.7195 mL
40 mM 0.0516 mL 0.2579 mL 0.5158 mL 1.2896 mL
50 mM 0.0413 mL 0.2063 mL 0.4127 mL 1.0317 mL
60 mM 0.0344 mL 0.1719 mL 0.3439 mL 0.8597 mL
80 mM 0.0258 mL 0.1290 mL 0.2579 mL 0.6448 mL
100 mM 0.0206 mL 0.1032 mL 0.2063 mL 0.5158 mL
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Ro 41-5253 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:

Ro 41-5253144092-31-9RAR/RXRApoptosisRetinoic acid receptorsRetinoid X receptorsRARαretinoic acidantagonistapoptosisantitumorbreast cancerInhibitorinhibitorinhibit

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