PROTAC FAK degrader 2

• UNSPSC Description:

  PROTAC FAK degrader 2 (Compound F2) is a PROTAC degrader for focal adhesion kinase (FAK), with DC50 of 27.72 and 60.1 nM, for total FAK and phosphorylated p-FAK. PROTAC FAK degrader 2 inhibits cell viability of cancer cells 4T1, MDA-MB-231, MDA-MB-468 and MDA-MB-435, with IC50s of 0.73-5.84 μM. PROTAC FAK degrader 2 reverses the multidrug resistance (MDR) through inhibition of AKT and ERK signaling pathway. PROTAC FAK degrader 2 exhibits antitumor efficacy in HCT/8 xenograft mouse model. (Pink: ligand for target protein Ifebemtinib (HY-122844); Black: linker (HY-Y0681); Blue: ligand for E3 ligase Thalidomide (HY-14658))[1]

• Target Antigen:

  FAK; PROTACs

• Type:

  Reference compound

• Related Pathways:

  PROTAC;Protein Tyrosine Kinase/RTK

• Applications:

  Cancer-Kinase/protease

• Field of Research:

  Cancer

• Assay Protocol:

  https://www.medchemexpress.com/protac-fak-degrader-2.html

• Smiles:

  COC1=CC(C(NC2CCN(CC2)CC3CCN(CC3)C4=CC5=C(C(N(C5=O)C6CCC(NC6=O)=O)=O)C=C4)=O)=C(C=C1NC7=NC(OC8=CC=CC9=C8C(N(C9)C)=O)=C(C=N7)C(F)(F)F)F

• Molecular Weight:

  927.90

• References & Citations:

  [1]Xu MS, et al., A novel FAK-degrading PROTAC molecule exhibited both anti-tumor activities and efficient MDR reversal effects. Acta Pharmacol Sin. 2024 Jun 6.

• Shipping Conditions:

  Room temperature

• Clinical Information:

  No Development Reported