PROTAC EGFR degrader 9

PROTAC EGFR degrader 9 (Compound C6) is an orally active CRBN-based PROTAC EGFR degrader. PROTAC EGFR degrader 9 exhibits a DC50 of 10.2 nM and a Kd of 240.2 nM against EGFRL858R/T790M/C797S. PROTAC EGFR degrader 9 exhibits potent degradation activity against various EGFR mutants, while sparing the EGFRWT. (Blue: CRBN ligand (HY-A0003), Black: linker (HY-161613) ; Pink: EGFR inhibitor (HY-161537) ) [1].

Product Specifications

CAS Number

[2992670-33-2]

UNSPSC

12352005

Target

Apoptosis; EGFR; PROTACs

Type

Reference compound

Related Pathways

Apoptosis; JAK/STAT Signaling; PROTAC; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/protac-egfr-degrader-9.html

Purity

98.35

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C(CCCCCCN1CCN(C2=CC=C(NC3=NC=C(C(C4=CN(C5=CC=CC=C54)S(=O)(CC)=O)=N3)C(F)(F)F)C=C2)CC1)NC6=CC=CC7=C6CN(C7=O)C8C(NC(CC8)=O)=O

Molecular Formula

C45H48F3N9O6S

Molecular Weight

899.98

References & Citations

[1]Yasheng Zhu, et al. Design, Synthesis, and Biological Evaluation of Novel EGFR PROTACs Targeting C797S Mutation. J Med Chem. 2024 May 9;67 (9) :7283-7300.