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  3. EPI-001

EPI-001 

目录号: HY-100348
产品使用指南

EPI-001 是一种选择性雄激素受体 (AR) 的抑制剂,抑制 AR 氨基末端结构域 (NTD) 的反式激活,IC50 值约 6 μM。EPI-001也是 PPARγ 的选择性调节剂。EPI-001在体外和体内均表现出抗肿瘤活性。

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EPI-001 Chemical Structure

EPI-001 Chemical Structure

CAS No. : 227947-06-0

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Description

EPI-001 is a selective inhibitor of Androgen Receptor (AR), and it 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 exhibits anti-tumor activity in vitro and in vivo[1][2].

IC50 & Target

IC50: 6 μM (AR NTD)[1]

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].

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.
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].

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.
Molecular Weight

394.89

Formula

C₂₁H₂₇ClO₅

CAS No.

227947-06-0

SMILES

OCC(O)COC1=CC=C(C(C)(C2=CC=C(OCC(O)CCl)C=C2)C)C=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

EPI-001EPI001EPI 001Androgen ReceptorPPARApoptosisPeroxisome proliferator-activated receptorsAndrogenReceptorARtransactivationamino-terminaldomainNTDPPARγanti-tumorInhibitorinhibitorinhibit

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EPI-001
目录号:
HY-100348
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