1. Immunology/Inflammation
  2. PD-1/PD-L1
  3. PD-1/PD-L1-IN-9

PD-1/PD-L1-IN-9 

Cat. No.: HY-132192
Handling Instructions

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.

For research use only. We do not sell to patients.

PD-1/PD-L1-IN-9 Chemical Structure

PD-1/PD-L1-IN-9 Chemical Structure

CAS No. : 2628506-54-5

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Description

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].

IC50 & Target

IC50: 3.8 nM (PD-1/PD-L1)[1]

In Vitro

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male BALB/c mice (5-6 weeks) were inoculated CT26 cells[1]
Dosage: 40, 80 mg/kg
Administration: P.o. once a day for 2 weeks
Result: Significantly decreased the final tumor weight, with TGI values of 60 and 67% at the dose of 40 and 80 mg/kg, respectively.
Animal Model: Sprague-Dawley (SD) rats[1]
Dosage: 3 mg/kg for i.v. and 25 mg/kg for p.o. (Pharmacokinetic Analysis)
Administration: A single i.v. or p.o.
Result: I.v.: t1/2=4.2 h; Cl=11.5 L/h/kg; Cmax=1233 ng/mL.
P.o.: F=22 %; t1/2=6.4 h; Cmax=192 ng/mL.
Molecular Weight

348.44

Formula

C₂₂H₂₄N₂O₂

CAS No.
SMILES

CC1=C(C=CC=C1C2=CC=CC=C2)C3=NC(OC)=C(C=C3)CNCCO

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Keywords:

PD-1/PD-L1-IN-9PD-1/PD-L1PD-1/Programmed death-ligand 1PD-1PD-L1interactiontumorInhibitorinhibitorinhibit

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