2. PROTAC
  3. Ligands for E3 Ligase
  4. (S,R,S)-AHPC-Me dihydrochloride

(S,R,S)-AHPC-Me dihydrochloride  (Synonyms: VHL ligand 2 dihydrochloride; E3 ligase Ligand 1 dihydrochloride)

製品番号: HY-42424A 純度: 99.84%
COA 取扱説明書 Technical Support

(S,R,S)-AHPC-Me dihydrochloride (VHL ligand 2 dihydrochloride) is the (S,R,S)-AHPC-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC-Me dihydrochloride can be used to synthesize ARV-771, a von Hippel-Landau (VHL) E3 ligase-based BET PROTAC degrader. ARV-771 potently degrades BET protein in castration-resistant prostate cancer (CRPC) cells with a DC50 <1 nM.

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(S,R,S)-AHPC-Me dihydrochloride

(S,R,S)-AHPC-Me dihydrochloride 構造式

CAS 番号 : 2504950-56-3

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 55 在庫あり
Solution
10 mM * 1 mL in DMSO USD 55 在庫あり
Solid
50 mg $50 在庫あり
100 mg $80 在庫あり
500 mg $160 在庫あり
1 g $240 在庫あり
5 g $660 在庫あり
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50 g   お問い合わせ  

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Other Forms of (S,R,S)-AHPC-Me dihydrochloride:

(S,R,S)-AHPC-Me dihydrochloride 関連抗体

Top Publications Citing Use of Products

Ligands for E3 Ligase アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
von Hippel-Lindau (VHL) MDM2 Cereblon IAP KLHDC2 Fbxo3 RNF4 DCAF11 DCAF1 UHRF1 TRIM21 NEURL1B KLHL41

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製品説明

(S,R,S)-AHPC-Me dihydrochloride (VHL ligand 2 dihydrochloride) is the (S,R,S)-AHPC-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein[1]. (S,R,S)-AHPC-Me dihydrochloride can be used to synthesize ARV-771, a von Hippel-Landau (VHL) E3 ligase-based BET PROTAC degrader. ARV-771 potently degrades BET protein in castration-resistant prostate cancer (CRPC) cells with a DC50 <1 nM[2].

IC50 & Target

VHL

 

体外実験

The VHL protein is a substrate recognition subunit of two ubiquitously expressed and biologically important Cullin RING E3 ubiquitin ligase complexes. VHL is one of the most popular E3 ligases being recruited by bifunctional Proteolysis-targeting chimeras (PROTACs) to induce ubiquitination and subsequent proteasomal degradation of a target protein[1].

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

(S,R,S)-AHPC-Me dihydrochloride 関連抗体
分子量

517.51

分子式

C23H34Cl2N4O3S
CAS 番号
Appearance

Solid

Color

Light yellow to yellow

SMILES

N[C@@H](C(C)(C)C)C(N1[C@H](C(N[C@@H](C)C2=CC=C(C3=C(C)N=CS3)C=C2)=O)C[C@@H](O)C1)=O.Cl.Cl
輸送条件

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

4°C, sealed storage, away from moisture

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

H2O : 100 mg/mL (193.23 mM; Need ultrasonic)

DMSO : 50 mg/mL (96.62 mM; ultrasonic and warming and heat to 60°C; 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 1.9323 mL 9.6616 mL 19.3233 mL
5 mM 0.3865 mL 1.9323 mL 3.8647 mL
10 mM 0.1932 mL 0.9662 mL 1.9323 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.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

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

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Concentration
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Volume
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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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 5 mg/mL (9.66 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: ≥ 5 mg/mL (9.66 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  PBS

    Solubility: 100 mg/mL (193.23 mM); Clear solution; Need ultrasonic

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.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
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).
純度とドキュメンテーション

純度: 99.84%

COA (251 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 (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 / H2O 1 mM 1.9323 mL 9.6616 mL 19.3233 mL 48.3082 mL
5 mM 0.3865 mL 1.9323 mL 3.8647 mL 9.6616 mL
10 mM 0.1932 mL 0.9662 mL 1.9323 mL 4.8308 mL
15 mM 0.1288 mL 0.6441 mL 1.2882 mL 3.2205 mL
20 mM 0.0966 mL 0.4831 mL 0.9662 mL 2.4154 mL
25 mM 0.0773 mL 0.3865 mL 0.7729 mL 1.9323 mL
30 mM 0.0644 mL 0.3221 mL 0.6441 mL 1.6103 mL
40 mM 0.0483 mL 0.2415 mL 0.4831 mL 1.2077 mL
50 mM 0.0386 mL 0.1932 mL 0.3865 mL 0.9662 mL
60 mM 0.0322 mL 0.1610 mL 0.3221 mL 0.8051 mL
80 mM 0.0242 mL 0.1208 mL 0.2415 mL 0.6039 mL
H2O 100 mM 0.0193 mL 0.0966 mL 0.1932 mL 0.4831 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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(S,R,S)-AHPC-Me dihydrochloride 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:

(S,R,S)-AHPC-Me2504950-56-3VHL ligand 2E3 ligase Ligand 1VHL ligand2VHL ligand-2Ligands for E3 LigaseE3 ligase-recruiting MoietyInhibitorinhibitorinhibit

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製品名:
(S,R,S)-AHPC-Me dihydrochloride
製品番号:
HY-42424A
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