Ro 41-5253

Ro 41-5253用途

Ro 41-5253是一种口服活性选择性视黄酸受体α(RARα)拮抗剂。Ro 41-5253可以结合RARα,而不诱导转录或影响RAR/RXR异源二聚化和DNA结合。Ro 41-5253可抑制癌细胞增殖并诱导凋亡,具有抗肿瘤活性[1][2]。

Ro 41-5253名称

[ CAS 号 ]:
144092-31-9

[ 英文名 ]:
Ro 41-5253

[英文别名 ]:

LG-629
Ro 41-5253

Ro 41-5253生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 细胞凋亡 >> 细胞凋亡

研究领域 >> 癌症

信号通路 >> 代谢酶/蛋白酶 >> RAR/RXR

[ 靶点 ]

IC50: 60 nM (RARα), 2.4 μM (RARβ), 3.3 μM (RARγ)[3].

[体外研究]

Ro 41-5253(1nm-10μM,10天)显著抑制MCF-7和ZR 75.1细胞增殖,并以时间和剂量依赖性方式诱导细胞凋亡[1]。细胞增殖试验[1]细胞系：人乳腺癌细胞系MCF-7和ZR 75.1浓度：1nM-10μM孵育时间：10天结果：10μM时抑制81%的MCF-1细胞生长,1μM时30%的细胞生长,0.1μM以下浓度无明显抑制作用。在10μM时,抑制74%的ZR 75.1细胞生长,在1μM时抑制63%的细胞生长,而在0.1μM处抑制42%的细胞增长。细胞凋亡分析[1]细胞系：人乳腺癌细胞系MCF-7和ZR 75.1浓度：1nM-10μM孵育时间：10天结果：在第4天分别在10μM、1μM、0.1μM和0.01μM诱导28.5%、21.6%、16%和12%的MCF-1细胞凋亡,而在第6天分别诱导58%、51%、36%和21%的细胞凋亡。在第6天,分别在10μM、1μM、0.1μM和0.01μM诱导80%、65%、43%和29%的ZR 75.1细胞凋亡。

[体内研究]

Ro 41-5253(口服灌胃,10-600mg/kg,每周一次,4周)可减少移植有MCF-7细胞系的雌性无胸腺Balb/小鼠的肿瘤体积[2]。动物模型：6周龄雌性无胸腺Balb/小鼠移植MCF-7细胞系[2]剂量：10、30、100、300和600mg/kg给药：口服灌胃；一周一次4周结果：在10、30和100 mg/kg剂量下,肿瘤体积减少,无任何毒副作用。

[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.

[3]. C Apfel, et al. A retinoic acid receptor alpha antagonist selectively counteracts retinoic acid effects. Proc Natl Acad Sci U S A. 1992 Aug 1;89(15):7129-33.

Ro 41-5253物理化学性质

[ 密度 ]:
1.154g/cm3

[ 沸点 ]:
661.4ºC at 760 mmHg

[ 分子式 ]:
C₂₈H₃₆O₅S

[ 分子量 ]:
484.64700

[ 闪点 ]:
353.8ºC

[ 精确质量 ]:
484.22800

[ PSA ]:
89.05000

[ LogP ]:
7.83030

[ 蒸汽压 ]:
2.16E-18mmHg at 25°C

[ 折射率 ]:
1.558

Ro 41-5253MSDS

详细MSDS(安全技术说明书)

Ro 41-5253安全信息

[ 危险品运输编码 ]:
NONH for all modes of transport

Ro 41-5253文献

Effect of all-trans-retinoic acid on enterovirus 71 infection in vitro.

Br. J. Nutr. 111(9) , 1586-93, (2014)

Our previous studies have shown that vitamin A (VA) status is associated with antiviral immunity and pathogenic conditions in enterovirus 71 (EV71)-infected children. In the present study, we establis...

Retinoic acid inhibits in vivo interleukin-2 gene expression and T-cell activation in mice.

Immunology 126(4) , 514-22, (2009)

Interleukin-2 (IL-2) is an essential cytokine for T-lymphocyte homeostasis. We have previously reported that all-trans retinoic acid (atRA) enhances the secretion of IL-2 from human peripheral blood T...

Overexpression of mucin genes induced by interleukin-1 beta, tumor necrosis factor-alpha, lipopolysaccharide, and neutrophil elastase is inhibited by a retinoic acid receptor alpha antagonist.

Exp. Lung Res. 28(4) , 315-32, (2002)

Proinflammatory cytokines, lipopolysaccharide (LPS), and neutrophil elastase (NE) have been implicated in the induction of hypersecretion of respiratory mucus. In this study, we demonstrated that inte...

更多文献