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

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

Cat. No.: HY-42424 Purity: 99.59%
COA Handling Instructions

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(S,R,S)-AHPC-Me hydrochloride (VHL ligand 2 hydrochloride) 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 hydrochloride 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 hydrochloride Chemical Structure

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

CAS No. : 1948273-03-7

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Based on 1 publication(s) in Google Scholar

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

(S,R,S)-AHPC-Me hydrochloride Related Antibodies

Top Publications Citing Use of Products

View All Ligands for E3 Ligase Isoform Specific Products:

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von Hippel-Lindau (VHL) MDM2 Cereblon IAP

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Description

(S,R,S)-AHPC-Me hydrochloride (VHL ligand 2 hydrochloride) 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 hydrochloride 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

481.05

Formula

C23H33ClN4O3S
CAS No.
Appearance

Solid

Color

Off-white 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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°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 (207.88 mM; Need ultrasonic)

DMSO : ≥ 63 mg/mL (130.96 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0788 mL 10.3939 mL 20.7879 mL
5 mM 0.4158 mL 2.0788 mL 4.1576 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)

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: ≥ 2.08 mg/mL (4.32 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: 2.08 mg/mL (4.32 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.08 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 (20.8 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 (207.88 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).
Purity & Documentation

Purity: 99.59%

COA (252 KB) HNMR (282 KB) LCMS (265 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 (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 2.0788 mL 10.3939 mL 20.7879 mL 51.9697 mL
5 mM 0.4158 mL 2.0788 mL 4.1576 mL 10.3939 mL
10 mM 0.2079 mL 1.0394 mL 2.0788 mL 5.1970 mL
15 mM 0.1386 mL 0.6929 mL 1.3859 mL 3.4646 mL
20 mM 0.1039 mL 0.5197 mL 1.0394 mL 2.5985 mL
25 mM 0.0832 mL 0.4158 mL 0.8315 mL 2.0788 mL
30 mM 0.0693 mL 0.3465 mL 0.6929 mL 1.7323 mL
40 mM 0.0520 mL 0.2598 mL 0.5197 mL 1.2992 mL
50 mM 0.0416 mL 0.2079 mL 0.4158 mL 1.0394 mL
60 mM 0.0346 mL 0.1732 mL 0.3465 mL 0.8662 mL
80 mM 0.0260 mL 0.1299 mL 0.2598 mL 0.6496 mL
100 mM 0.0208 mL 0.1039 mL 0.2079 mL 0.5197 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 hydrochloride 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:

(S,R,S)-AHPC-Me1948273-03-7VHL ligand 2 E3 ligase Ligand 1VHL ligand2VHL ligand-2Ligands for E3 LigaseE3 ligase-recruiting MoietyInhibitorinhibitorinhibit

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