PROTAC EGFR degrader 9

• UNSPSC Description:

  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].

• Target Antigen:

  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

• 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 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.

• Shipping Conditions:

  Blue Ice

• Clinical Information:

  No Development Reported

• CAS Number:

  2992670-33-2