PD-1/PD-L1-IN-9 |
| Catalog No.GC62387 |
PD-1/PD-L1-IN-9 est un inhibiteur puissant et actif par voie orale de l'interaction PD-1/PD-L1, avec une IC50 de 3,8 nM. PD-1/PD-L1-IN-9 peut renforcer l'activité de destruction des cellules tumorales par les cellules immunitaires. PD-1/PD-L1-IN-9 présente également une activité antitumorale in vivo significative dans un modèle de souris CT26.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2628506-54-5
Sample solution is provided at 25 µL, 10mM.
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PD-1/PD-L1-IN-9 is a potent and orally active inhibitor of PD-1/PD-L1 interaction, with an IC50 of 3.8 nM. PD-1/PD-L1-IN-9 can enhance the killing activity of tumor cells by immune cells. PD-1/PD-L1-IN-9 also exhibits significant in vivo antitumor activity in a CT26 mouse model[1].
PD-1/PD-L1-IN-9 (compound 24) (46.9-1500 nM; pretreated for 2 h) dose-dependently significantly activates the antitumor immunity of PBMCs to MDB-MB 231 cells, with an EC50 of ∼100 nM[1].
PD-1/PD-L1-IN-9 (compound 24) (40-80 mg/kg; p.o. once a day for 2 weeks) inhibits tumor growth in a dose-dependent manner and does not cause any body weight loss or mortality of mice[1].PD-1/PD-L1-IN-9 (3 mg/kg; a single i.v.) exhibits half-life (t1/2=4.2 h), plasma clearance (Cl=11.5 L/h/kg) and Cmax (1233 ng/mL) in rats[1].PD-1/PD-L1-IN-9 (25 mg/kg; a single p.o.) exhibits moderate oral bioavailability (F=22 %), half-life (t1/2=6.4 h) and Cmax (192 ng/mL) in rats[1].
[1]. Wang T, et, al. Novel Biphenyl Pyridines as Potent Small-Molecule Inhibitors Targeting the Programmed Cell Death-1/Programmed Cell Death-Ligand 1 Interaction. J Med Chem. 2021 May 30.
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