| Company Name: |
InvivoChem Gold
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| Tel: |
13549236410 |
| Email: |
sales@invivochem.cn |
| Products Intro: |
Product Name:NP19
CAS:2377916-66-8
Purity:98% HPLC Package:1mg Remarks:V37662
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| Company Name: |
ChemCell Biomedicine Co.,Ltd.
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| Tel: |
020-13556033878 2965585218 13556033878 |
| Email: |
chemcell@hotmail.com |
| Products Intro: |
Product Name:PD-1/PD-L1-IN-NP19
CAS:2377916-66-8
Purity:98% Package:5mg；10mg；20mg；50mg；100mg；250mg；500mg；1g；5g；10g；25g；100g
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| | Alanine, N-[[5-chloro-2-[(3-cyanophenyl)methoxy]-4-[(2-methyl[1,1'-biphenyl]-3-yl)methoxy]phenyl]methyl]-2-methyl- Basic information |
| | Alanine, N-[[5-chloro-2-[(3-cyanophenyl)methoxy]-4-[(2-methyl[1,1'-biphenyl]-3-yl)methoxy]phenyl]methyl]-2-methyl- Chemical Properties |
| Boiling point | 715.5±60.0 °C(Predicted) | | density | 1.28±0.1 g/cm3(Predicted) | | storage temp. | Store at -20°C | | solubility | DMSO : 6.25 mg/mL (11.26 mM; Need ultrasonic) | | form | A crystalline solid | | pka | 2.03±0.10(Predicted) | | color | White to off-white |
| | Alanine, N-[[5-chloro-2-[(3-cyanophenyl)methoxy]-4-[(2-methyl[1,1'-biphenyl]-3-yl)methoxy]phenyl]methyl]-2-methyl- Usage And Synthesis |
| Biological Activity | 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].
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].
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]. | | References | [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. |
| | Alanine, N-[[5-chloro-2-[(3-cyanophenyl)methoxy]-4-[(2-methyl[1,1'-biphenyl]-3-yl)methoxy]phenyl]methyl]-2-methyl- Preparation Products And Raw materials |
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