Ro 41-5253
Ro 41-5253 Basic information
- Product Name:
- Ro 41-5253
- Synonyms:
-
- Ro 41-5253
- 4-(2-(7-(Heptyloxy)-3,4-dihydro-4,4-dimethyl-2H-1-benzothiopyran-6-yl)-1-propenyl)-Benzoic acid, S,S-dioxide
- 4-[(1E)-2-[7-(Heptyloxy)-3,4-dihydro-4,4-dimethyl-1,1-dioxido-2H-1-benzothiopyran-6-yl]-1-propen-1-yl]-benzoic acid
- 4-[2-(7-Heptoxy-4,4-dimethyl-1,1-dioxo-2,3-dihydrothiochromen-6-yl)
- Benzoic acid, 4-[(1E)-2-[7-(heptyloxy)-3,4-dihydro-4,4-dimethyl-1,1-dioxido-2H-1-benzothiopyran-6-yl]-1-propen-1-yl]-
- Ro 41-5253 >=98% (HPLC)
- CAS:
- 144092-31-9
- MF:
- C28H36O5S
- MW:
- 484.65
- Mol File:
- 144092-31-9.mol
Ro 41-5253 Chemical Properties
- storage temp.
- -20°C
- solubility
- DMSO: soluble20mg/mL, clear
- form
- powder
- color
- white to beige
- Stability:
- Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 3 months.
Ro 41-5253 Usage And Synthesis
Description
Ro 41-5253 (144092-31-9) is a selective RARα antagonist.1?Binds RARα without inducing transcription or influencing RAR/RXR heterodimerization and DNA binding.2?Ro 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
Ro 41-5253Supplier
- Tel
- 021-65675885 18964387627
- info@efebio.com
- Tel
- 025-58859352 13155353615
- qzhang@aikonchem.com
- Tel
- +1-781-999-5354; +17819995354
- marketing@targetmol.com
- Tel
- 021-58432009 400-005-6266
- marketing1@energy-chemical.com
- Tel
- 4008200310
- marketing@tsbiochem.com
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