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

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).

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EPI-7170 Chemical Structure

EPI-7170 Chemical Structure

CAS No. : 2139288-26-7

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Based on 1 publication(s) in Google Scholar

EPI-7170 Related Antibodies

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Description

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].

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].

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

EPI-7170 Related Antibodies

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.
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].

MedChemExpress (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.
Molecular Weight

540.88

Formula

C22H28Cl3NO6S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC(C1=CC(Cl)=C(C(Cl)=C1)OC[C@H](O)CCl)(C2=CC=C(C=C2)OC[C@H](O)CNS(C)(=O)=O)C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

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

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (184.88 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 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
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EPI-7170 Related Classifications

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.

Keywords:

EPI-71702139288-26-7EPI7170EPI 7170Androgen Receptorralaniten analogueandrogen receptorN-terminal structural domainFL-ARAR-Vsantitumorenzalutamide resistantCRPCInhibitorinhibitorinhibit

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