EPI-001

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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

EPI-001 Chemical Structure

CAS No. : 227947-06-0

规格 价格 是否有货 数量
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

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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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