Ro 41-5253|cas:144092-31-9|西域试剂

Ro 41-5253,98.44%

产品编号：Bellancom-116248| CAS NO：144092-31-9| 分子式：C₂₈H₃₆O₅S| 分子量：484.65

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货号	价格	库存与货期
Bellancom-116248	￥1660.00	杭州北京（现货）
Bellancom-116248	￥2980.00	杭州北京（现货）
Bellancom-116248	￥6750.00	杭州北京（现货）
Bellancom-116248	￥12150.00	杭州北京（现货）

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Ro 41-5253

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。

生物活性

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.

体外研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay

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

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.

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (206.33 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.0633 mL	10.3167 mL	20.6334 mL
5 mM	0.4127 mL	2.0633 mL	4.1267 mL
10 mM	0.2063 mL	1.0317 mL	2.0633 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (5.16 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.16 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (5.16 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.16 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。