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PD-1/PD-L1-IN-NP19

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Catalog No. T36900Cas No. 2377916-66-8
Alias PD-1/PD-L1-IN-NP19

PD-1/PD-L1-IN-NP19, a PD-1/PD-L1 inhibitor, exhibits an IC50 of 12.5 nM against the human PD-1/PD-L1 interaction, potentially activating the tumor immune microenvironment and contributing to its antitumor effects[1].

PD-1/PD-L1-IN-NP19

PD-1/PD-L1-IN-NP19

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Purity: 96.70%
Catalog No. T36900Alias PD-1/PD-L1-IN-NP19Cas No. 2377916-66-8
PD-1/PD-L1-IN-NP19, a PD-1/PD-L1 inhibitor, exhibits an IC50 of 12.5 nM against the human PD-1/PD-L1 interaction, potentially activating the tumor immune microenvironment and contributing to its antitumor effects[1].
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$126-In Stock
5 mg$313-In Stock
10 mg$496-In Stock
25 mg$953-In Stock
50 mg$1,490-In Stock
100 mg$2,360-In Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:96.70%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
Description
PD-1/PD-L1-IN-NP19, a PD-1/PD-L1 inhibitor, exhibits an IC50 of 12.5 nM against the human PD-1/PD-L1 interaction, potentially activating the tumor immune microenvironment and contributing to its antitumor effects[1].
Targets&IC50
PD-1/PD-L1 (human):12.5 nM (IC50)
In vitro
PD-1/PD-L1-IN-NP19 (compound NP19) (0.37-10 μM; 72 h) significantly elevates IFN-γ production 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 (IC50 >1 μM) compared to human PD-1/PD-L1 interaction (IC50=12.5 nM)[1]. PD-1/PD-L1-IN-NP19 (10 μM; 48 h) shows 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 days) significantly inhibits melanoma tumor growth in mice. Additionally, PD-1/PD-L1-IN-NP19 (25 mg/kg; i.p. daily for 14 days) exhibits substantial antitumor efficacy with a tumor growth inhibition (TGI) of 76.5% and is well-tolerated in an H22 hepatoma mouse model. In rats, PD-1/PD-L1-IN-NP19 (1 mg/kg; i.v.) has a half-life (t1/2) of 1.5±0.5 hours, clearance rate (CL) of 0.9±0.2 L/h/kg, and an apparent distribution volume (Vss) of 2.1±0.5 L/kg. Furthermore, when administered orally at 10 mg/kg, PD-1/PD-L1-IN-NP19 shows an absorption time (Tmax) of 0.6±0.2 hours, a long half-life (t1/2) of 10.9±7.7 hours, and an oral bioavailability (F) of 5% in rats.
SynonymsPD-1/PD-L1-IN-NP19
Chemical Properties
Molecular Weight555.06
FormulaC33H31ClN2O4
Cas No.2377916-66-8
SmilesCc1c(COc2cc(OCc3cccc(c3)C#N)c(CNC(C)(C)C(O)=O)cc2Cl)cccc1-c1ccccc1
Storage & Solubility Information
Storagestore at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 1.8 mg/mL (3.24 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.8016 mL9.0080 mL18.0161 mL90.0804 mL

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Preparation of the In Vivo Formulation:

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Keywords

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