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

Name: (S,R,S)-AHPC-Me dihydrochloride
Brand: MedChemExpress
SKU: HY-42424A
Rating: 4.5 (1 reviews)

Cat. No.: HY-42424A Purity: 99.84%: FAQs
Data Sheet SDS COA Handling Instructions

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(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

CAS No. : 2504950-56-3

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10 mM * 1 mL in DMSO ready for reconstitution	USD 165	In-stock	Estimated Time of Arrival: December 31
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10 mM * 1 mL in DMSO	USD 165	In-stock	Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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

(S,R,S)-AHPC-Me hydrochloride In-stock
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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

CAS No.

2504950-56-3

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

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; 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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: ≥ 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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 5 mg/mL (9.66 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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)

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: 99.84%

Select Batch:

Data Sheet (274 KB) SDS (393 KB)

COA (251 KB) LCMS (94 KB)

Handling Instructions (2659 KB)

References

[1]. Raina K, et al. PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancer. Proc Natl Acad Sci U S A. 2016 Jun 28;113(26):7124-9. [Content Brief]

Complete Stock Solution Preparation Table

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.

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

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

Customer Review

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

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

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Ligands for E3 Ligase Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

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Dilution Calculator

Complete Stock Solution Preparation Table

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

Keywords:

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