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.
性状
Solid
IC50 & Target[1][2]
IC50: 60 nM (RARα), 2.4 μM (RARβ), 3.3 μM (RARγ).
体外研究(In Vitro)
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. has not independently confirmed the accuracy of these methods. They are for reference only.Cell Proliferation Assay
体内研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moisture and light In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
参考文献
[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. doi: 10.1016/j.canlet.2004.06.018.
溶解度数据
In Vitro: DMSO : 100 mg/mL (206.33 mM; Need ultrasonic)配制储备液