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Ro 41-5253

Catalog No. T28589   CAS 144092-31-9
Synonyms: Ro-41-5253, Ro 415253

Ro 41-5253 is an orally active RARα antagonist, ligand and partial agonist of peroxisome proliferator-activated receptor (PPAR)-γ. It exhibits antitumor activity, inhibits proliferation and induces apoptosis in MCF-7 and ZR-75.1 estrogen receptor positive breast cancer cells.

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Ro 41-5253 Chemical Structure
Ro 41-5253, CAS 144092-31-9
Pack Size Availability Price/USD Quantity
25 mg 8-10 weeks $ 954.00
50 mg 8-10 weeks $ 1,240.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Ro 41-5253 is an orally active RARα antagonist, ligand and partial agonist of peroxisome proliferator-activated receptor (PPAR)-γ. It exhibits antitumor activity, inhibits proliferation and induces apoptosis in MCF-7 and ZR-75.1 estrogen receptor positive breast cancer cells.
Targets&IC50 RARγ:3.3 μM, RARβ:2.4 μM, RARα:60 nM
In vitro In human breast cancer cell lines MCF-7 and ZR 75.1, Ro 41-5253 (1 nM-10 μM; for 10 days) inhibited cell growth. At a concentration of 10 μM, the inhibition rate of MCF-7 cell growth was 81%, 30% at 1 μM, and no significant inhibition was observed at concentrations below 0.1 μM. For ZR 75.1 cells, the growth inhibition rate was 74% at 10 μM, 63% at 1 μM, and 42% at 0.1 μM[1].
In vivo In six-week-old athymic female Balb/c mice implanted with MCF-7 cell line, Ro 41-5253 (10, 30, 100, 300, and 600 mg/kg; oral gavage; once weekly; for 4 weeks) resulted in a reduction in tumor volume at doses of 10, 30, and 100 mg/kg, with no toxic side effects[2].
Synonyms Ro-41-5253, Ro 415253
Molecular Weight 484.65
Formula C28H36O5S
CAS No. 144092-31-9

Storage

keep away from direct sunlight,keep away from moisture

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 80 mg/mL (165.07 mM), Sonication is recommended.

TargetMolReferences and Literature

1. S Toma, et al. RARalpha antagonist Ro 41-5253 inhibits proliferation and induces apoptosis in breast-cancer cell lines. Int J Cancer. 1998 Sep 25;78(1):86-94. 2. Salvatore Toma, et al. Retinoids and human breast cancer: in vivo effects of an antagonist for RAR-alpha. Cancer Lett. 2005 Feb 28;219(1):27-31. 3. C Apfel, et al. A retinoic acid receptor alpha antagonist selectively counteracts retinoic acid effects. Proc Natl Acad Sci U S A. 1992 Aug 1;89(15):7129-33.

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Keywords

Ro 41-5253 144092-31-9 Apoptosis Metabolism Retinoid Receptor Ro-41-5253 Ro 41 5253 Ro 415253 inhibitor inhibit

 

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