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Propargyl-PEG4-acid

Names

[ CAS No. ]:
1415800-32-6

[ Name ]:
Propargyl-PEG4-acid

[Synonym ]:
MFCD22683284
4,7,10,13-Tetraoxahexadec-15-yn-1-oic acid
Propargyl-PEG4-acid

Biological Activity

[Description]:

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[1].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> PROTAC >> PROTAC Linker

[Target]

PEGs


[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[1].

[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.

Chemical & Physical Properties

[ Density]:
1.1±0.1 g/cm3

[ Boiling Point ]:
388.0±37.0 °C at 760 mmHg

[ Molecular Formula ]:
C12H20O6

[ Molecular Weight ]:
260.284

[ Flash Point ]:
141.0±20.0 °C

[ Exact Mass ]:
260.125977

[ LogP ]:
-0.80

[ Vapour Pressure ]:
0.0±1.9 mmHg at 25°C

[ Index of Refraction ]:
1.468

Safety Information

[ Hazard Codes ]:
Xi

Related Compounds