1. Others
    Antibody-drug Conjugate/ADC Related
  2. Estrogen Receptor/ERR
    PROTAC-linker Conjugate for PAC


Cat. No.: HY-112100
Handling Instructions

PAC comprises an antibody conjugated via a linker to a PROTAC. PAC extracts from patent WO2017201449A1, compound PAC1. PAC is a more marked estrogen receptor-alpha (ERα) degrader compared to PROTAC (without Ab).

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

PAC Chemical Structure

PAC Chemical Structure

CAS No. : 2158322-33-7

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References


PAC comprises an antibody conjugated via a linker to a PROTAC. PAC extracts from patent WO2017201449A1, compound PAC1. PAC is a more marked estrogen receptor-alpha (ERα) degrader compared to PROTAC (without Ab).

IC50 & Target

Estrogen receptor-alpha (ERα)[1]

In Vitro

Treatment of HER2 expressing cells with HER2 antibody containing PAC Anti-HER2(Endox-XIAP) results in a marked decreased Estrogen Receptor-alpha (ERα) levels with an IC50 of 132 ng/mL. The PROTAC-Antibody Conjugate (PAC) molecules comprise an antibody conjugated via a linker (L1) to a PROTAC, wherein the PROTAC comprises an ubiquitin E3 ligase binding group (“E3LB”), a linker (“L2”) and a protein binding group (“PB”). The following sections describe the components that comprise the PAC. To obtain a PAC having potent efficacy and a desirable therapeutic index, the following components are provided. 1. Antibody (Ab): The antibody portion of a PAC can target a cell that expresses an antigen whereby the antigen specific PAC is delivered intracellularly to the target cell, typically through endocytosis While PACs that comprise an antibody directed to an antigen that is not found on the cell surface may result in less specific intracellular delivery of the PROTAC portion into the cell, the PAC may still undergo pinocytosis. 2. Linkers (L1): A“linker” (L1) is a bifunctional or multifunctional moiety that can be used to link one or more PROTAC moieties (D) to an antibody (Ab) to form a PAC. In some embodiments, PACs can be prepared using a L1 having reactive functionalities for covalently attaching to the PROTAC and to the antibody. 3. PROTAC(D) [1].

Kinase Assay

Syntheses of a PAC:
A. Chemical Synthesis of a PROTAC:
i. Attachment of a Linker (L2) to an E3 Ligase Binding Group (E3LB).
ii. Attachment of a protein binding moiety (PB) to an E3LB via a Linker (L2).
B. Preparation of L1-PROTAC:
iii. Attachment of Linker L1 to PROTAC.
C. Preparation of PAC:
iv. Attachment of Antibody (Ab) to PROTAC via Linker L1[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight







CN(C(COCCOCCNC(C1=CC=C(C(N2[[email protected]@H](C)[[email protected]](NC([[email protected]](C)NC)=O)C(N(CC3=C(OC)C=CC4=C3C=CC=C4)C5=C2C=C(C#N)C=C5)=O)=O)C=C1)=O)=O)CCOC(C=C6)=CC=C6/C(C7=CC=C(OCC(C=C8)=CC=C8NC([[email protected]](CCCNC(N)=O)NC([[email protected]](C(C)C)NC(CCCCCN9C(C=CC9=O)=O)=O)=O)=O)C=C7)=C(C%10=CC=CC=C%10)/CC


Please store the product under the recommended conditions in the Certificate of Analysis.


Room temperature in continental US; may vary elsewhere

  • Molarity Calculator

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The molarity calculator equation

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

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The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

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Cat. No.: HY-112100