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 Kd 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].

Product Specifications

CAS Number

[2995357-09-8]

UNSPSC

12352211

Target

PD-1/PD-L1; PROTACs

Type

Reference compound

Related Pathways

Immunology/Inflammation; PROTAC

Applications

Cancer-programmed cell death

Field of Research

Cancer

Smiles

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

Molecular Formula

C46H42ClFN6O8

Molecular Weight

861.31

References & Citations

[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.