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PD-1/PD-L1-IN-9

Catalog No.GC62387

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.

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

Cas No.: 2628506-54-5

Size Price Stock Qty
5 mg
$315.00
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10 mg
$522.00
In stock
25 mg
$990.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

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.

Chemical Properties

Cas No. 2628506-54-5 SDF
Formula C22H24N2O2 M.Wt 348.44
Solubility DMSO : 100 mg/mL (286.99 mM; Need ultrasonic) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.8699 mL 14.3497 mL 28.6993 mL
5 mM 0.574 mL 2.8699 mL 5.7399 mL
10 mM 0.287 mL 1.435 mL 2.8699 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 30 reference(s) in Google Scholar.)

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