Propargyl-PEG4-acid is a PEG-based PROTAC linker can be used in the synthesis of BTK-IAP PROTACs Ibrutinib (HY-10997)-based PROTAC 2 and an analogue PROTAC 3. PROTAC 3 causes BTK degradation with a DC50 of 200 nM in THP-1 cells.

Product information

CAS Number: 1415800-32-6

Molecular Weight: 260.28

Formula: C12H20O6

Chemical Name: 4,7,10,13-tetraoxahexadec-15-ynoic acid

Smiles: C#CCOCCOCCOCCOCCC(O)=O

InChiKey: WMBXAUWIPBFEOK-UHFFFAOYSA-N

InChi: InChI=1S/C12H20O6/c1-2-4-15-6-8-17-10-11-18-9-7-16-5-3-12(13)14/h1H,3-11H2,(H,13,14)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

BTK-IAP PROTACs act as stoichiometric degraders, resulting in degradation of BTK protein. Degradation of BTK is a result of IAP E3 ligases family recruitment.

References:

1. Tinworth CP, et al. PROTAC-Mediated Degradation of Bruton's Tyrosine Kinase Is Inhibited by Covalent Binding. ACS Chem Biol. 2019 Mar 15;14(3):342-347.

Products are for research use only. Not for human use.