Description
Ro 41-5253 (144092-31-9) is a selective RARα antagonist.1Binds RARα without inducing transcription or influencing RAR/RXR heterodimerization and DNA binding.2Ro 415253 inhibits proliferation and induces apoptosis in a variety of cell lines/types. Cell Permeable.
Uses
Ro 415253 is a retinoic acid receptor antagonists, a promising starting point for antimetastatic therapies.
Definition
ChEBI: A thiochromane that is 3,4-dihydro-2H-1-benzothiopyran S,S-dioxide in which the hydrogens at position 4 are both replaced by methyl groups, the hydrogens at position 7 is replaced by a heptyloxy group, w
ile the hydrogen at position 6 is replaced by a 1-phenylprop-1-en-2-yl group, the phenyl group of which is substituted at the para position by a carboxy group. It is a selective antagonist for retinoic acid receptor alpha.
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].
| 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. |
References
[1] C APFEL. A retinoic acid receptor alpha antagonist selectively counteracts retinoic acid effects.[J]. Proceedings of the National Academy of Sciences of the United States of America, 1992, 89 15: 7129-7133. DOI:
10.1073/pnas.89.15.7129[2] SALVATORE TOMA. RARα antagonist RO 41-5253 inhibits proliferation and induces apoptosis in breast-cancer cell lines[J]. International Journal of Cancer, 1999, 78 1: 86-94. DOI:
10.1002/(sici)1097-0215(19980925)78:1<86::aid-ijc14>3.0.co;2-3
