| Identification | Back Directory | [Name]
Alanine, N-[[5-chloro-2-[(3-cyanophenyl)methoxy]-4-[(2-methyl[1,1'-biphenyl]-3-yl)methoxy]phenyl]methyl]-2-methyl- | [CAS]
2377916-66-8 | [Synonyms]
NP19
PD-L1-IN-NP19
PD-1/PD-L1-IN-NP19
Alanine, N-[[5-chloro-2-[(3-cyanophenyl)methoxy]-4-[(2-methyl[1,1'-biphenyl]-3-yl)methoxy]phenyl]methyl]-2-methyl- | [Molecular Formula]
C33H31ClN2O4 | [MDL Number]
MFCD34167506 | [MOL File]
2377916-66-8.mol | [Molecular Weight]
555.06 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [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. |
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