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PD-1/PD-L1-IN-NP19

Catalog No. T36900 CAS 2377916-66-8

<a href="/target/PD_1_PD_L1" style="display: inline; color: #c13a36">PD-1/PD-L1</a>-IN-NP19 is a <a href="/target/PD_1_PD_L1" style="display: inline; color: #c13a36">PD-1/PD-L1</a> inhibitor, with an IC50 of 12.5 nM for human <a href="/target/PD_1_PD_L1" style="display: inline; color: #c13a36">PD-1/PD-L1</a> interaction. <a href="/target/PD_1_PD_L1" style="display: inline; color: #c13a36">PD-1/PD-L1</a>-IN-NP19 could activate the immune microenvironment in tumor, which may contribute to its antitumor effects[1].

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PD-1/PD-L1-IN-NP19, CAS 2377916-66-8

Pack Size	Availability	Price/USD
5 mg	8-10 weeks	$ 970.00
50 mg	8-10 weeks	$ 1,980.00
100 mg	8-10 weeks	$ 2,500.00

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Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	PD-1/PD-L1-IN-NP19 is a PD-1/PD-L1 inhibitor, with an IC50 of 12.5 nM for human PD-1/PD-L1 interaction. PD-1/PD-L1-IN-NP19 could activate the immune microenvironment in tumor, which may contribute to its antitumor effects[1].
Targets&IC50	human PD-1/PD-L1:12.5 nM (IC50)
In vitro	PD-1/PD-L1-IN-NP19 (compound NP19) (0.37-10 μM; 72 h) significantly elevates the production of IFN-γ in a dose dependent manner from T cells co-cultured with tumor cells[1].PD-1/PD-L1-IN-NP19 exhibits much lower activity for inhibiting mouse PD-1/PD-L1 interaction with an IC50 in the micromolar range (>1μM), as compared to the inhibition of human PD1/PD-L1 interaction (IC50=12.5 nM)[1].PD-1/PD-L1-IN-NP19 (10 μM; 48 h) displays no apparent cytotoxic effects on A549, MCF-7, and B16-F10 cells at a concentration of 10 μM[1].
In vivo	PD-1/PD-L1-IN-NP19 (compound NP19) (25-100 mg/kg; intragastric gavage once daily for 15 d) inhibits the growth of melanoma tumors dramatically in mice[1].PD-1/PD-L1-IN-NP19 (25 mg/kg; i.p. daily for 14 d) demonstrates significant antitumor efficacy with a tumor growth inhibition (TGI) of 76.5% and is well tolerated in an H22 hepatoma mouse model[1].PD-1/PD-L1-IN-NP19 (1 mg/kg; i.v.) shows the half time (t1/2=1.5±0.5 h), clearance rate (CL=0.9±0.2 L/h/kg) and apparent distribution volume (Vss=2.1±0.5 L/kg) in rats[1].PD-1/PD-L1-IN-NP19 (10 mg/kg; p.o.) shows the oral absorption (Tmax=0.6±0.2 h), long half-life (t1/2=10.9±7.7 h) and oral bioavailability (F=5%) in rats[1].

Molecular Weight	555.07
Formula	C33H31ClN2O4
CAS No.	2377916-66-8

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 1.8 mg/mL (3.2 mM), Need ultrasonic

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Cheng B, et, al. Discovery of Novel Resorcinol Dibenzyl Ethers Targeting the Programmed Cell Death-1/Programmed Cell Death-Ligand 1 Interaction As Potential Anticancer Agents. J Med Chem. 2020 Jul 15.

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Keywords

PD-1/PD-L1-IN-NP19 2377916-66-8 Apoptosis Cell Cycle/Checkpoint Immunology/Inflammation PD-1/PD-L1 PD-1/PD-L-1-IN-NP19 PD1/PDL1INNP19 PD 1/PD L1 IN NP19 Inhibitor inhibitor inhibit

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