PD-1/PD-L1-IN-14

• CAT Number: I044061
• CAS Number: 2499965-12-5
• Molecular Formula: C24H24N4O2
• Molecular Weight: 400.47
• Purity: ≥95%
• Synonyms: 2-[[3-[[5-(2-methyl-3-phenylphenyl)-1,3,4-oxadiazol-2-yl]amino]phenyl]methylamino]ethanol
• InChI: InChI=1S/C24H24N4O2/c1-17-21(19-8-3-2-4-9-19)11-6-12-22(17)23-27-28-24(30-23)26-20-10-5-7-18(15-20)16-25-13-14-29/h2-12,15,25,29H,13-14,16H2,1H3,(H,26,28)
• InChIKey: YBHXMLDVPTWSAS-UHFFFAOYSA-N
• SMILES: CC1=C(C=CC=C1C2=NN=C(O2)NC3=CC=CC(=C3)CNCCO)C4=CC=CC=C4

PD-1/PD-L1-IN-14 (compound 17) is a bifunctional inhibitor of PD-1/PD-L1 interactions, with an IC50 of 27.8 nM. PD-1/PD-L1-IN-14 (compound 17) inhibits PD-1/PD-L1 interactions and promotes dimerization, internalization, and degradation of PD-L1[1].
PD-1/PD-L1-IN-14 (compound 17) promotes cell-surface PD-L1 internalized into the cytosol and induces the degradation of PD-L1 in tumor cells through a lysosome-dependent pathway[1].

Reference

[1]. Tianyu Wang, et al. Discovery of Small-Molecule Inhibitors of the PD-1/PD-L1 Axis That Promote PD-L1 Internalization and Degradation. J Med Chem. 2022 Mar 10;65(5):3879-3893.
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