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

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

Cat. No.: HY-42424A Purity: 98.24%
Handling Instructions

(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.

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

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

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

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 330 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 330 In-stock
Estimated Time of Arrival: December 31
Solid
100 mg USD 300 In-stock
Estimated Time of Arrival: December 31
500 mg USD 650 In-stock
Estimated Time of Arrival: December 31
1 g USD 1000 In-stock
Estimated Time of Arrival: December 31
2 g USD 1800 In-stock
Estimated Time of Arrival: December 31
5 g   Get quote  
10 g   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

(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

 

Molecular Weight

517.51

Formula

C23H34Cl2N4O3S

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

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

Solvent & Solubility
In Vitro: 

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

DMSO : 50 mg/mL (96.62 mM; ultrasonic and warming and heat to 60°C)

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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are available by MCE.
References

Purity: 98.39%

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

This equation is commonly abbreviated as: C1V1 = C2V2

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× = ×
C1   V1   C2   V2

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Product Name:
(S,R,S)-AHPC-Me dihydrochloride
Cat. No.:
HY-42424A
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