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