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

Ralaniten triacetate  (Synonyms: EPI-506)

Cat. No.: HY-123875A Purity: 98.79%
COA Handling Instructions

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Ralaniten triacetate (EPI-506), the pro-agent of Ralaniten, is a first-in-class, orally active androgen receptor (AR) N-terminal domain (NTD) inhibitor. Ralaniten triacetate shows activity against both full length and resistance-related AR species, including AR-v7.

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

Ralaniten triacetate Chemical Structure

Ralaniten triacetate Chemical Structure

CAS No. : 1637573-04-6

Size Price Stock Quantity
Liquid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 573 In-stock
Solution
10 mM * 1 mL in DMSO USD 573 In-stock
Liquid
5 mg USD 500 In-stock
10 mg USD 850 In-stock
25 mg USD 1800 In-stock
50 mg USD 3000 In-stock
100 mg USD 4600 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Ralaniten triacetate:

Ralaniten triacetate Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Ralaniten triacetate (EPI-506), the pro-agent of Ralaniten, is a first-in-class, orally active androgen receptor (AR) N-terminal domain (NTD) inhibitor. Ralaniten triacetate shows activity against both full length and resistance-related AR species, including AR-v7[1][2].

In Vitro

Ralaniten triacetate (EPI-506) targets the N-terminal domain of the androgen receptor (AR), and is used for metastatic castration-resistant prostate cancer (mCRPC) research. EPI-506 is a first-in-class, highly-specific small molecule that binds to a novel target on the AR, the N-terminal domain (NTD) and directly inhibits AR transcriptional activity by blocking the interaction of the AR with transcriptional proteins[2].

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

Ralaniten triacetate Related Antibodies
Clinical Trial
Molecular Weight

521.00

Formula

C27H33ClO8
CAS No.
Appearance

Liquid

Color

Colorless to light yellow

SMILES

CC(C(C=C1)=CC=C1OC[C@@H](CCl)OC(C)=O)(C(C=C2)=CC=C2OC[C@H](OC(C)=O)COC(C)=O)C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Pure form -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (191.94 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 1.9194 mL 9.5969 mL 19.1939 mL
5 mM 0.3839 mL 1.9194 mL 3.8388 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. 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)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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    40% PEG300    5% Tween-80    45% Saline

    Solubility: 2.5 mg/mL (4.80 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

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

    Solubility: 2.5 mg/mL (4.80 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    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).
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: 98.79%

COA (245 KB) HNMR (283 KB) LCMS (94 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. 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 1.9194 mL 9.5969 mL 19.1939 mL 47.9846 mL
5 mM 0.3839 mL 1.9194 mL 3.8388 mL 9.5969 mL
10 mM 0.1919 mL 0.9597 mL 1.9194 mL 4.7985 mL
15 mM 0.1280 mL 0.6398 mL 1.2796 mL 3.1990 mL
20 mM 0.0960 mL 0.4798 mL 0.9597 mL 2.3992 mL
25 mM 0.0768 mL 0.3839 mL 0.7678 mL 1.9194 mL
30 mM 0.0640 mL 0.3199 mL 0.6398 mL 1.5995 mL
40 mM 0.0480 mL 0.2399 mL 0.4798 mL 1.1996 mL
50 mM 0.0384 mL 0.1919 mL 0.3839 mL 0.9597 mL
60 mM 0.0320 mL 0.1599 mL 0.3199 mL 0.7997 mL
80 mM 0.0240 mL 0.1200 mL 0.2399 mL 0.5998 mL
100 mM 0.0192 mL 0.0960 mL 0.1919 mL 0.4798 mL
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Ralaniten triacetate 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:

Ralaniten triacetate1637573-04-6EPI-506EPI506EPI 506Androgen ReceptorprodrugAR-v7speciesN-terminaldomainprostatecancerInhibitorinhibitorinhibit

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