Ro 41-5253

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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。

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.

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.Cell Proliferation Assay Cell Line:Human breast-carcinoma lines MCF-7 and ZR.Concentration:1 nM-10 μMIncubation 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 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.Animal Model:Six-week-old female athymic Balb/mice transplanted with MCF-7 cell line 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.

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Metabolic Enzyme/Protease

Retinoid Receptor

Retinoid Receptor | Apoptosis

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144092-31-9

484.65

C28H36O5S

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 100 mg/mL (206.33 mM; 超声助溶 )

CCCCCCCOc1cc2c(cc1\C(C)=C\c1ccc(cc1)C(O)=O)C(C)(C)CCS2(=O)=O

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(-20℃)

With Ice Pack

≥ 2 years