1. Vitamin D Related/Nuclear Receptor
  2. Androgen Receptor
  3. EPI-7170

EPI-7170,ralaniten 类似物,是一种有效的雄激素受体 N 端结构域 (androgen receptor N-terminal structural domain) 拮抗剂,可以阻断全长 AR (FL-AR) 和 AR 剪接变体 (AR-Vs) 的转录活性。 EPI-7170 对 enzalutamide 耐药的去势抵抗性前列腺癌 (CRPC) 具有抗肿瘤作用。

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EPI-7170 Chemical Structure

EPI-7170 Chemical Structure

CAS No. : 2139288-26-7

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

EPI-7170, a ralaniten analogue, is a potent androgen receptor N-terminal structural domain antagonist that blocks the transcriptional activity of full-length AR (FL-AR) and AR splice variants (AR-Vs). EPI-7170 has antitumor effects against enzalutamide resistant castration-resistant prostate cancer (CRPC)[1].

体外研究
(In Vitro)

EPI-7170 (0-12 μM, 24 or 48 h) inhibits cell proliferation in VCaP-ENZR and C4-2B-ENZR cells, also enhances the effect of enzalutamide which has a lower IC 50 when bound to EPI-7170[1].
EPI-7170 (0-20 μM, 24 or 48 h) synergistically inhibits androgen receptor (AR) transcriptional activity in ENZR cells expressing androgen receptor splice variant-7 (AR-V7) with enzalutamide[1].
EPI-7170 (3.5 μM, 48 h) results in an increase in G1 phase and a decrease in S phase, and reduces the expression levels of CDK4, cyclin D1 and cyclin A2 proteins[1].

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

Cell Cycle Analysis[1]

Cell Line: C4-2B-ENZR cells
Concentration: 3.5 μM
Incubation Time: 48 h
Result: Resulted in an increase in G1 phase and a decrease in S phase, and reduced the expression levels of CDK4, cyclin D1 and cyclin A2 proteins.
体内研究
(In Vivo)

EPI-7170 (oral administration, 30 mg/kg, daily, 31 days) has some anti-tumor activity and can be combined with enzalutamide in male NOD/SCID mice[1].

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

Animal Model: 6-8 week old male NOD/SCID mice infected with VCaP-ENZR cells[1]
Dosage: 30 mg/kg
Administration: Oral administration; daily; 31 days
Result: Significantly reduced tumor volume and decreased levels of FL-AR and AR-V7 in harvested xenografts.
分子量

540.88

Formula

C22H28Cl3NO6S

CAS 号
性状

油状物

颜色

Colorless to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
细胞实验: 

DMSO 中的溶解度 : 100 mg/mL (184.88 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.8488 mL 9.2442 mL 18.4884 mL
5 mM 0.3698 mL 1.8488 mL 3.6977 mL
查看完整储备液配制表

* 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)。-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。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: 99.86%

参考文献

完整储备液配制表

* 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)。-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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.8488 mL 9.2442 mL 18.4884 mL 46.2210 mL
5 mM 0.3698 mL 1.8488 mL 3.6977 mL 9.2442 mL
10 mM 0.1849 mL 0.9244 mL 1.8488 mL 4.6221 mL
15 mM 0.1233 mL 0.6163 mL 1.2326 mL 3.0814 mL
20 mM 0.0924 mL 0.4622 mL 0.9244 mL 2.3110 mL
25 mM 0.0740 mL 0.3698 mL 0.7395 mL 1.8488 mL
30 mM 0.0616 mL 0.3081 mL 0.6163 mL 1.5407 mL
40 mM 0.0462 mL 0.2311 mL 0.4622 mL 1.1555 mL
50 mM 0.0370 mL 0.1849 mL 0.3698 mL 0.9244 mL
60 mM 0.0308 mL 0.1541 mL 0.3081 mL 0.7703 mL
80 mM 0.0231 mL 0.1156 mL 0.2311 mL 0.5778 mL
100 mM 0.0185 mL 0.0924 mL 0.1849 mL 0.4622 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
EPI-7170
目录号:
HY-150102
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