1. PROTAC
  2. E3 Ligase Ligand-Linker Conjugates
  3. (S,R,S)-AHPC-C2-PEG4-N3

(S,R,S)-AHPC-C2-PEG4-N3  (Synonyms: VH032-C2-PEG4-N3)

Cat. No.: HY-130654 Purity: 97.63%
Handling Instructions Technical Support

(S,R,S)-AHPC-C2-PEG4-N3 (VH032-C2-PEG4-N3) is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 4-unit PEG linker used in PROTAC technology. (S,R,S)-AHPC-C2-PEG4-N3 can be used in the synthesis of vRucaparib-TP4 (HY-130647). vRucaparib-TP4 a highly potent PARP1 degrader with a half-maximal degrading concentration (DC50) of 82 nM. (S,R,S)-AHPC-C2-PEG4-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. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.

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(S,R,S)-AHPC-C2-PEG4-N3

(S,R,S)-AHPC-C2-PEG4-N3 Chemical Structure

CAS No. : 2597167-24-1

Size Price Stock Quantity
Oil + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Oil
25 mg In-stock
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Based on 1 publication(s) in Google Scholar

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Description

(S,R,S)-AHPC-C2-PEG4-N3 (VH032-C2-PEG4-N3) is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 4-unit PEG linker used in PROTAC technology. (S,R,S)-AHPC-C2-PEG4-N3 can be used in the synthesis of vRucaparib-TP4 (HY-130647). vRucaparib-TP4 a highly potent PARP1 degrader with a half-maximal degrading concentration (DC50) of 82 nM[1]. (S,R,S)-AHPC-C2-PEG4-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. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.

IC50 & Target[1]

VHL

 

Molecular Weight

703.85

Formula

C33H49N7O8S

CAS No.
Appearance

Oil

Color

Colorless to light yellow

SMILES

CC(C)([C@H](NC(CCOCCOCCOCCOCCN=[N+]=[N-])=O)C(N1C[C@H](O)C[C@H]1C(NCC2=CC=C(C3=C(N=CS3)C)C=C2)=O)=O)C

Shipping

Room temperature in continental US; may vary elsewhere.

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

DMSO : 50 mg/mL (71.04 mM; Need ultrasonic; 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 1.4208 mL 7.1038 mL 14.2076 mL
5 mM 0.2842 mL 1.4208 mL 2.8415 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.

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  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 97.63%

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 1.4208 mL 7.1038 mL 14.2076 mL 35.5189 mL
5 mM 0.2842 mL 1.4208 mL 2.8415 mL 7.1038 mL
10 mM 0.1421 mL 0.7104 mL 1.4208 mL 3.5519 mL
15 mM 0.0947 mL 0.4736 mL 0.9472 mL 2.3679 mL
20 mM 0.0710 mL 0.3552 mL 0.7104 mL 1.7759 mL
25 mM 0.0568 mL 0.2842 mL 0.5683 mL 1.4208 mL
30 mM 0.0474 mL 0.2368 mL 0.4736 mL 1.1840 mL
40 mM 0.0355 mL 0.1776 mL 0.3552 mL 0.8880 mL
50 mM 0.0284 mL 0.1421 mL 0.2842 mL 0.7104 mL
60 mM 0.0237 mL 0.1184 mL 0.2368 mL 0.5920 mL
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  • Do most proteins show cross-species activity?

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(S,R,S)-AHPC-C2-PEG4-N3
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