2. Vitamin D Related/Nuclear Receptor
  3. Androgen Receptor
  4. Ralaniten

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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10 mM * 1 mL in DMSO
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Customer Review

Based on 1 publication(s) in Google Scholar

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Ralaniten Related Antibodies

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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].

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

Ralaniten Related Antibodies
In Vivo

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

MedChemExpress (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.
Appearance

Solid

Color

White to off-white

SMILES

CC(C1=CC=C(OC[C@H](O)CCl)C=C1)(C2=CC=C(OC[C@H](O)CO)C=C2)C
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; 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 2.5324 mL 12.6618 mL 25.3235 mL
5 mM 0.5065 mL 2.5324 mL 5.0647 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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 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

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

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

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.78%

SDS (251 KB)

COA (244 KB) HNMR (250 KB) LCMS (88 KB)

Handling Instructions (2659 KB)
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 (protect from light). 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 2.5324 mL 12.6618 mL 25.3235 mL 63.3088 mL
5 mM 0.5065 mL 2.5324 mL 5.0647 mL 12.6618 mL
10 mM 0.2532 mL 1.2662 mL 2.5324 mL 6.3309 mL
15 mM 0.1688 mL 0.8441 mL 1.6882 mL 4.2206 mL
20 mM 0.1266 mL 0.6331 mL 1.2662 mL 3.1654 mL
25 mM 0.1013 mL 0.5065 mL 1.0129 mL 2.5324 mL
30 mM 0.0844 mL 0.4221 mL 0.8441 mL 2.1103 mL
40 mM 0.0633 mL 0.3165 mL 0.6331 mL 1.5827 mL
50 mM 0.0506 mL 0.2532 mL 0.5065 mL 1.2662 mL
60 mM 0.0422 mL 0.2110 mL 0.4221 mL 1.0551 mL
80 mM 0.0317 mL 0.1583 mL 0.3165 mL 0.7914 mL
100 mM 0.0253 mL 0.1266 mL 0.2532 mL 0.6331 mL
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Ralaniten 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:

Ralaniten1203490-23-6EPI-002EPI002EPI 002Androgen ReceptorandrogenN-terminaldomainARNTDtranscriptionalcastrationresistantprostatecancerCRPCInhibitorinhibitorinhibit

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