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

Ralaniten  (Synonyms: EPI-002)

製品番号: HY-109070 純度: 99.57%
COA 取扱説明書 Technical Support

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).

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Ralaniten

Ralaniten 構造式

CAS 番号 : 1203490-23-6

容量 価格（税別） 在庫状況 数量
>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 110 在庫あり
Solution
10 mM * 1 mL in DMSO USD 110 在庫あり
Solid
5 mg $100 在庫あり
10 mg $160 在庫あり
25 mg $320 在庫あり
50 mg $500 在庫あり
100 mg $800 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

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Ralaniten 関連抗体

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製品説明

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]
Cellular Effect
Cell Line Type Value Description References
CWR22R IC50
40.4 μM
Compound: EPI002
Antiproliferative activity against AR/AR-V7 positive human 22Rv1 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK-8 assay
Antiproliferative activity against AR/AR-V7 positive human 22Rv1 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK-8 assay
[PMID: 38512060]
CWR22R IC50
> 30 μM
Compound: EPI-002
Antiproliferative activity against enzalutamide-resistant human 22Rv1 cells assessed as reduction in cell viability incubated for 6 days by CCK-8 assay
Antiproliferative activity against enzalutamide-resistant human 22Rv1 cells assessed as reduction in cell viability incubated for 6 days by CCK-8 assay
[PMID: 37556600]
LNCaP IC50
> 30 μM
Compound: EPI-002
Antiproliferative activity against human LNCaP cells assessed as reduction in cell viability incubated for 6 days by CCK-8 assay
Antiproliferative activity against human LNCaP cells assessed as reduction in cell viability incubated for 6 days by CCK-8 assay
[PMID: 37556600]
VCaP IC50
> 30 μM
Compound: EPI-002
Antiproliferative activity against human VCaP cells assessed as reduction in cell viability incubated for 6 days by CCK-8 assay
Antiproliferative activity against human VCaP cells assessed as reduction in cell viability incubated for 6 days by CCK-8 assay
[PMID: 37556600]
体外実験

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 関連抗体
体内実験

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].
分子量

394.89

分子式

C21H27ClO5
CAS 番号
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
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

4°C, protect from light

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

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
10 mM 0.2532 mL 1.2662 mL 2.5324 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)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

×
体積 （終了）

V2

体内:

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.
純度とドキュメンテーション

純度: 99.57%

COA (244 KB) HNMR (262 KB) LCMS (94 KB)

取扱説明書 (2659 KB)
参考文献

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

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
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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