PROTAC PD-L1 degrader-2 

PROTAC PD-L1 degrader-2 (Compound 9i) is a PROTAC degrader for PD-L1, that inhibits PD-L1 with an IC₅₀ of 197.4 nM and exhibits an affinity with PD-L1 with a K_d of 301 nM. PROTAC PD-L1 degrader-2 promotes the internalization of PD-L1 on the cell membrane, and induces PD-L1 degradation via the synergistic effect of the proteasome and lysosomal pathways. PROTAC PD-L1 degrader-2 can activate the immune system, and exhibits antitumor efficacy in MC38 C57BL/6 mouse model^[1].

861.31

C₄₆H₄₂ClFN₆O₈

2995357-09-8

ClC1=C(C=CC=C1C2=CC=CC=C2F)COC3=CC(OCC4=CC(C#N)=CN=C4)=C(C=C3)CNCCOCCOCCNC5=C(C6=CC=C5)C(N(C6=O)C7C(NC(CC7)=O)=O)=O

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Zhang F, et al., Design, synthesis, anti-tumor activity and mechanism of novel PROTACs as degraders of PD-L1 and inhibitors of PD-1/PD-L1 interaction. Bioorg Med Chem. 2024 Sep 1;111:117867.  [Content Brief]