EPI-001 | whatman (沃特曼)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

EPI-001 纯度: 98.52%

EPI-001 是一种选择性雄激素受体 (AR) 的抑制剂，靶向 AR 的反式激活单元 5 (Tau-5)。EPI-001 可抑制 AR 氨基末端结构域 (NTD) 的反式激活，IC₅₀ 值约为 6 μM。EPI-001 也是一种选择性的 PPARγ 调节剂。EPI-001 对去势抵抗性前列腺癌具有活性。

EPI-001 Chemical Structure

CAS No. : 227947-06-0

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥880	In-stock
10 mg	￥800	In-stock
25 mg	￥1600	In-stock
50 mg	￥2800	询价
100 mg		询价
200 mg		询价

* Please select Quantity before adding items.

EPI-001 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Apoptosis Compound Library
Cell Cycle/DNA Damage Compound Library
Anti-Cancer Compound Library
Anti-Aging Compound Library
Neurodegenerative Disease-related Compound Library
Transcription Factor Targeted Library

生物活性

EPI-001, a selective inhibitor of Androgen Receptor (AR), targets transactivation unit 5 (Tau-5) of the AR. EPI-001 can inhibit transactivation of the AR amino-terminal domain (NTD), with an IC₅₀ of ~6 μM. EPI-001 is also a selective modulator of PPARγ. EPI-001 is active against castration-resistant prostate cancer^[1]^[2]^[3].

IC₅₀ & Target

IC50: 6 μM (AR NTD)^[1]

体外研究
(In Vitro)

EPI-001 (5-100 μM; 7 d) inhibits PCa/CRPC cell growth in a dose-dependent manner^[2].
EPI-001 (50 μM) inhibits endogenous AR mRNA and protein expression in PCa and CRPC cell lines^[2].
EPI-001 (50 μM) inhibits transcriptional activity of both AR TAU1 and TAU5^[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay^[2]

Cell Line:	PCa, CRPC, PC-3, DU 145, and T47D cell lines
Concentration:	0, 5, 10, 25, 50, 100 μM
Incubation Time:	7 days
Result:	Inhibited growth of LNCaP cells at low concentrations. Inhibited growth of AR-negative PC-3 and DU 145 cell lines as well as the T47D breast carcinoma cell line.

Western Blot Analysis^[2]

Cell Line:	LNCaP, VCaP LAPC4, C4-2,22Rv1, and CWR-R1 cells
Concentration:	50 μM
Incubation Time:	8-16 hours
Result:	Decreased expression of full-length AR protein to varying degrees.

体内研究
(In Vivo)

EPI-00 (20 mg/kg; i.v. every 5 d for 25 d) inhibits the growth of tumors and has no general toxicity in vivo^[1].
EPI-00 (50 mg/kg; i.v.) blocks the androgen-axis and inhibits androgen-dependent tumor growth^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male NOD-SCID mice (6-8 weeks) bearing LNCaP^[1]
Dosage:	20 mg/kg
Administration:	I.v. every 5 days for 25 days
Result:	Reduced tumors from 100.3±1.72 mm³ to 73.03±29.6 mm³ within 2 weeks. Did not cause general toxicity indicated by no change in animal behavior or body weight.

分子量

394.89

Formula

C₂₁H₂₇ClO₅

CAS 号

227947-06-0

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 : 33.33 mg/mL (84.40 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.5324 mL	12.6618 mL	25.3235 mL
5 mM	0.5065 mL	2.5324 mL	5.0647 mL
10 mM	0.2532 mL	1.2662 mL	2.5324 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： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.5 mg/mL (6.33 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.33 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% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (6.33 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.33 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 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
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.5 mg/mL (6.33 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.33 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。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Andersen RJ, et, al. Regression of castrate-recurrent prostate cancer by a small-molecule inhibitor of the amino-terminus domain of the androgen receptor. Cancer Cell. 2010 Jun 15; 17(6): 535-46.

[2]. Brand LJ, et, al. EPI-001 is a selective peroxisome proliferator-activated receptor-gamma modulator with inhibitory effects on androgen receptor expression and activity in prostate cancer. Oncotarget. 2015 Feb 28; 6(6): 3811-24.

[3]. Mol ED, et, al. EPI-001, A Compound Active against Castration-Resistant Prostate Cancer, Targets Transactivation Unit 5 of the Androgen Receptor. ACS Chem Biol. 2016 Sep 16;11(9):2499-505.

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