Bexarotene - CAS:153559-49-0

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Bexarotene (Synonyms:贝沙罗汀; LGD1069)

目录号 : KM10920 CAS No. : 153559-49-0 纯度 : 98%

Data Sheet 产品使用指南

Bexarotene (LGD1069) 是一种高亲和力的选择性类视黄醇 X 受体 (RXR) 激动剂，对 RXRα、RXRβ 和 RXRγ 的 EC₅₀ 分别为 33、24、25 nM。Bexarotene 对 RAR 受体的亲和力有限 (EC₅₀ >10000 nM)。Bexarotene 可用于皮肤 T 细胞淋巴瘤的研究。

规格	价格	是否有货
50mg		In-stock
100mg		In-stock
500mg		In-stock
1g	询价	In-stock
5g	询价	In-stock

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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.

体外研究

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.

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

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.

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.

分子式

C₂₄H₂₈O₂

分子量

348.48

CAS号

153559-49-0

中文名称

贝沙罗汀；蓓萨罗丁

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

溶解性数据

In Vitro:

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

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.8696 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

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。-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： 5% DMSO 40% PEG300 5% Tween-80 50% saline
Solubility: 2.62 mg/mL (7.52 mM); Suspended solution; Need ultrasonic
2.

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

请依序添加每种溶剂： 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。
4.

请依序添加每种溶剂： 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。
5.

请依序添加每种溶剂： 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。

临床试验

科研文献

纯度： 98%

Data Sheet

产品使用指南

摩尔计算器
稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量

浓度

体积

分子量*

重置计算

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

浓度

体积

浓度

体积

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Other Forms of Rapamycin:

KKL 顾客使用本产品发表的 9 篇科研文献

The molarity calculator equation

The dilution calculator equation