1. Metabolic Enzyme/Protease
    Apoptosis
  2. RAR/RXR
    Apoptosis
  3. Ro 41-5253

Ro 41-5253 

Cat. No.: HY-116248
Handling Instructions

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.

For research use only. We do not sell to patients.

Ro 41-5253 Chemical Structure

Ro 41-5253 Chemical Structure

CAS No. : 144092-31-9

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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].

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

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].

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.
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

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Ro 41-5253
Cat. No.:
HY-116248
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