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Ro 41-5253
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
Ro 41-5253图片
CAS NO:144092-31-9
包装与价格：
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议

产品介绍
Ro 41-5253 是一种具有口服活性的选择性维甲酸受体 RARα 拮抗剂。Ro 41-5253 可以与 RARα 结合而不诱导转录或影响 RAR/RXR 异二聚化和 DNA 结合。Ro 415253 可抑制癌细胞增殖并诱导细胞凋亡 (apoptosis)，具有抗肿瘤活性。
Cas No.144092-31-9
分子式C28H36O5S
分子量484.65
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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 induceapoptosis, 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.