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Ralaniten (Synonyms: EPI-002)

Cat. No.: HY-109070 Purity: 99.75%
Handling Instructions

Ralaniten (EPI-002) is a potent and orally active antagonist of the androgen receptor-N-terminal domain (AR-NTD). Ralaniten inhibits AR transcriptional activity, with IC50 of 7.4 μM. Ralaniten can be used for the research of castration-resistant prostate cancer (CRPC).

For research use only. We do not sell to patients.

Ralaniten Chemical Structure

Ralaniten Chemical Structure

CAS No. : 1203490-23-6

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100 mg USD 800 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

Ralaniten (EPI-002) is a potent and orally active antagonist of the androgen receptor-N-terminal domain (AR-NTD). Ralaniten inhibits AR transcriptional activity, with IC50 of 7.4 μM. Ralaniten can be used for the research of castration-resistant prostate cancer (CRPC)[1][2].

IC50 & Target

IC50: 7.4 μM (AR-NTD)[1]

In Vitro

EPI-002 (5-35 μM; 2-3 days) reduces AR-dependent proliferation of LNCaP cells, and has no effect on the viability of PC3 human prostate cancer cells that do not express functional AR[1].
Ralaniten (10-35 μM; 4 h) inhibits transactivation of the AR N-terminal domain (NTD) induced by forskolin in LNCaP cells[1].

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

In Vivo

EPI-002 (100 mg/kg; p.o. twice daily for 28 days) inhibits the VCaP tumor growth in castrated mice[1].

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

Animal Model: Male NOD-SCID mice bearing subcutaneous tumors were castrated
Dosage: 100 mg/kg
Administration: P.o. twice daily for 28 days
Result: Inhibited the growth of castration-resistant prostate cancer (CRPC) xenografts that express AR splice variants[1].
Molecular Weight

394.89

Formula

C₂₁H₂₇ClO₅

CAS No.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (253.24 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

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

*All of the co-solvents are provided by MCE.
References
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Ralaniten
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HY-109070
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