NPH16 is a PD-1/PD-L1 Inhibitor. NPH16 exhibited the most potent PD-L1inhibitory activity (IC50 = 24.4 nM). The X-ray crystal structure further confirmed the high binding affinity of NPH16 to PD-L1dimer. In the HepG2/Jurkat T cell coculture model, NPH16promoted HepG2 cell apoptosis dose-dependently. In addition, NPH16 showed excellent in vivo antitumor efficacy (TGI = 92.1%) in a Hepa1−6 mouse tumor model and increased CD8+ cells in tumor microenvironment. Importantly, NPH16 possessed favorable pharmacokinetic properties with an oral bioavailability of 15.9%
MedKoo Cat#: 129050
Name: NPH16
CAS#: N/A
Chemical Formula: C39H44ClN3O6
Exact Mass: 685.2900
Molecular Weight: 686.25
Elemental Analysis: C, 68.26; H, 6.46; Cl, 5.17; N, 6.12; O, 13.99
The following data is based on the product molecular weight 686.25 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
Yang Z, Yang P, Xu J, Yang X, Zhou J, He H, Li L, Ren Y, Chen M, Xiao Y, Chen J. Discovery and Crystallography Study of Novel Resorcinol Dibenzyl Ether-Based PD-1/PD-L1 Inhibitors with Improved Drug-like and Pharmacokinetic Properties for Cancer Treatment. J Med Chem. 2025 Jun 16. doi: 10.1021/acs.jmedchem.5c00344. Epub ahead of print. PMID: 40518797.
