Bexarotene|153559-49-0|(贝沙罗汀; LGD1069)-陌孚医药/Medlife

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Bexarotene (Synonyms: 贝沙罗汀; LGD1069)

目录号: PC14835 纯度: ≥98%

CAS No. :153559-49-0

商品编号	规格	价格	会员价
PC14835-10mg	10mg	¥490.00	请登录
PC14835-50mg	50mg	¥686.00	请登录
PC14835-100mg	100mg	¥931.00	请登录
PC14835-10mM (in 1mL DMSO)	10mM (in 1mL DMSO)	¥882.00	请登录

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中文名称

Bexarotene

中文别名

蓓萨罗丁;4-[1-(5,6,7,8-四氢-3,5,5,8,8-五甲基-2-萘基)乙烯基]苯甲酸;4-氨基-7H-吡咯[2,3-d]嘧啶;贝沙罗汀;蓓萨罗丁-D4;蓓萨罗丁标准品;蓓萨罗汀;尼伐地平;萨罗丁杂质;贝沙罗汀D4;蓓萨罗丁(抗癌药);蓓萨罗丁(标准品);蓓萨罗丁(贝沙罗丁);蓓萨罗丁(4-[1-(5,6,7,8-四氢-3,5,5,8,8-五甲基-2-萘基)乙烯基]苯甲酸)

英文名称

Bexarotene

英文别名

Bexarotene;4-[1-(5,6,7,8-Tetrahydro-3,5,5,8,8-pentamethyl-2-naphthalenyl)ethenyl]benzoic acid;Targretin;4-(1-(3,5,5,8,8-Pentamethyl-5,6,7,8-tetrahydro-naphthalen-2-yl)vinyl)benzoic acid;Bexaroten;Lg 1069;LG 69;LGD1069;Targret;Targretyn;LGD-1069;SR-11247;Lg100069;SR 11247;Hsdb 7453;Targrexin;LGD 1069;bexarotenum;p-(1-(5,6,7,8-Tetrahydro-3,5,5,8,8-pentamethyl-2-naphthyl)vinyl)benzoic acid;4-[1-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydronaphthalen-2-yl)ethenyl]benzoic acid;LG 100069;A61RXM4375;4-[1-(3,5,5,8,8-pentamethyl-6,7-dihydronaphthalen-2-yl)ethenyl]benzoic acid;4-(1-(5,6,7,8-Tetrahydro-3,5,5,8,

Cas No.

153559-49-0

分子式

C₂₄H₂₈O₂

分子量

348.48

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

生物活性

Bexarotene (LGD1069) is a high-affinity and selective retinoid X receptors (RXR) agonist with EC₅₀s of 33, 24, 25 nM for RXRα, RXRβ, and RXRγ, respectively. Bexarotene shows limited affinity for RAR receptors (EC₅₀ >10000 nM). Bexarotene can be used for the research of cutaneous T-cell lymphoma.

性状

Solid

体外研究(In Vitro)

Bexarotene selectively binds and activates RXR subtypes with K_d=14±2 nM, 21±4 nM, and 29±7 nM for RXRα, RXRβ, and RXRγ subtypes.
Bexarotene is effective in limiting the proliferation of leukemic (HL-60) cells. Bexarotene inhibits the proliferation of HL-60 cells by 37% at 1 μM.
Bexarotene monotherapy of cells shows an antiproliferative effect at a high dose, and the IC₅₀s aere 40.62±0.45 μM (PC3) and 50.20±4.10 μM (DU145).
Bexarotene (20 and 40 μM) and Docetaxel (5 and 10 μM) exhibit a synergistic effect on the inhibition of PC3 and DU145 cell proliferation.
Bexarotene (20 and 40 μM) represses cyclin D1 and cyclin D3 expression in PC3 and DU145 cells.

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

Cell Proliferation Assay

Cell Line:	The human PCa androgen-independent cell lines PC3 and DU145
Concentration:	5, 10, 20, 30, 40 μM for PC3 cells; 1, 5, 10, 20, 40 μM for DU145 cells.
Incubation Time:	24 and 48 hours
Result:	Showed an antiproliferative effect with the IC₅₀s were 40.62±0.45 μM (PC3) and 50.20±4.10 μM (DU145).

Cell Viability Assay

Cell Line:	PC3 and DU145 cells
Concentration:	20 and 40 μM
Incubation Time:	24 or 48 hours
Result:	Decreased cyclin D1, and cyclin E2 after 24 hours treatment. Not only decreased the expression of cyclin D1 and cyclin E2 but repressed cyclin B1 and CDK1 expression after 48 hours treatment.

体内研究(In Vivo)

Bexarotene (1 mg/kg/day) is effective in blocking the development of behavioral deficits and dopamine neuron degeneration in a rat model of Parkinson’s disease (PD) producing significantly reduced changes in both triglycerides and T4 serum.
Bexarotene is an effective preventive agent against lung tumor growth and progression. Bexarotene ((100?mg/kg by gavage) inhibits both tumor multiplicity and tumor volume in mice of all three genotypes (p53K-ras, p53K-ras, or p53K-ras). Bexarotene reduces the progression of adenoma to adenocarcinoma by ～50% in both p53K-ras and p53K-ras mice.

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

Animal Model:	UL53-3 mice (p53K-ras, p53K-ras, or p53K-ras)
Dosage:	100?mg/kg
Administration:	Gavage with 18 gage of gavage-needle, 0.1?mL per mouse per day, 5 times a week, continued for 12 weeks
Result:	Inhibited both tumor multiplicity and tumor volume in mice of all three genotypes.

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

ClinicalTrial

参考文献

[1]. Nathalia Rodrigues de Almeida, et al. A review of the molecular design and biological activities of RXR agonists. Med Res Rev. 2019 Jul;39(4):1372-1397. [Information]

[2]. Danyang Shen, et al. Synergistic effect of a retinoid X receptor-selective ligand bexarotene and docetaxel in prostate cancer. Onco Targets Ther. 2019 Sep 24;12:7877-7886. [Information]

[3]. Y Wang, et al. Prevention of lung cancer progression by bexarotene in mouse models. Oncogene. 2006 Mar 2;25(9):1320-9. [Information]

溶解度数据

体外研究:

DMSO : 60 mg/mL (172.18 mM; Need ultrasonic)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.8696 mL	14.3480 mL	28.6961 mL
5 mM	0.5739 mL	2.8696 mL	5.7392 mL
10 mM	0.2870 mL	1.4348 mL	2.8696 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 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.

建议依照次序添加每种溶剂： 5% DMSO 40% PEG300 5% Tween-80 50% saline
Solubility: 2.62 mg/mL (7.52 mM); Suspended solution; Need ultrasonic
2.

建议依照次序添加每种溶剂： 5% DMSO 95% (20% SBE-β-CD in saline)
Solubility: 2.62 mg/mL (7.52 mM); Suspended solution; Need ultrasonic
3.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (5.97 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.97 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 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 ddH?O 中，得到澄清透明的生理盐水溶液
4.

建议依照次序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (5.97 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.97 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
5.

建议依照次序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (5.97 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.97 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 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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