1. PROTAC
  2. E3 Ligase Ligand-Linker Conjugates
  3. (S,R,S)-AHPC-PEG1-N3

(S,R,S)-AHPC-PEG1-N3  (Synonyms: VH032-PEG1-N3; VHL Ligand-Linker Conjugates 9; E3 ligase Ligand-Linker Conjugates 3)

Cat. No.: HY-103600 Purity: 98.18%
COA Handling Instructions

(S,R,S)-AHPC-PEG1-N3 is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 1-unit PEG linker used in PROTAC technology. (S,R,S)-AHPC-PEG1-N3 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.

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

(S,R,S)-AHPC-PEG1-N3 Chemical Structure

(S,R,S)-AHPC-PEG1-N3 Chemical Structure

CAS No. : 2101200-09-1

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Based on 1 publication(s) in Google Scholar

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Description

(S,R,S)-AHPC-PEG1-N3 is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 1-unit PEG linker used in PROTAC technology. (S,R,S)-AHPC-PEG1-N3 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.

IC50 & Target[1]

VHL

 

Molecular Weight

557.67

Formula

C26H35N7O5S

CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

O=C(N[C@@H](C(C)(C)C)C(N(C[C@H](O)C1)[C@@H]1C(NCC2=CC=C(C(SC=N3)=C3C)C=C2)=O)=O)COCCN=[N+]=[N-]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (179.32 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7932 mL 8.9659 mL 17.9318 mL
5 mM 0.3586 mL 1.7932 mL 3.5864 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. 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)

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: ≥ 2.5 mg/mL (4.48 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 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: ≥ 2.5 mg/mL (4.48 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).
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.
Purity & Documentation

Purity: 98.18%

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. 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 1.7932 mL 8.9659 mL 17.9318 mL 44.8294 mL
5 mM 0.3586 mL 1.7932 mL 3.5864 mL 8.9659 mL
10 mM 0.1793 mL 0.8966 mL 1.7932 mL 4.4829 mL
15 mM 0.1195 mL 0.5977 mL 1.1955 mL 2.9886 mL
20 mM 0.0897 mL 0.4483 mL 0.8966 mL 2.2415 mL
25 mM 0.0717 mL 0.3586 mL 0.7173 mL 1.7932 mL
30 mM 0.0598 mL 0.2989 mL 0.5977 mL 1.4943 mL
40 mM 0.0448 mL 0.2241 mL 0.4483 mL 1.1207 mL
50 mM 0.0359 mL 0.1793 mL 0.3586 mL 0.8966 mL
60 mM 0.0299 mL 0.1494 mL 0.2989 mL 0.7472 mL
80 mM 0.0224 mL 0.1121 mL 0.2241 mL 0.5604 mL
100 mM 0.0179 mL 0.0897 mL 0.1793 mL 0.4483 mL
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(S,R,S)-AHPC-PEG1-N3 Related Classifications

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  • 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.

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Product Name:
(S,R,S)-AHPC-PEG1-N3
Cat. No.:
HY-103600
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