Product Details of 103-50-4. Recently I am researching about SMALL-MOLECULE INHIBITORS; PD-L1, Saw an article supported by the International Science and Technology Cooperation Projects of Guangdong Province of China [G819310411]; scientific research project of high-level talents in Southern Medical University [C1051008]. Published in AMER CHEMICAL SOC in WASHINGTON ,Authors: Cheng, BB; Wang, W; Niu, XG; Ren, YC; Liu, T; Cao, H; Wang, SH; Tu, YF; Chen, JX; Liu, SW; Yang, XC; Chen, JJ. The CAS is 103-50-4. Through research, I have a further understanding and discovery of Benzyl ether
A series of programmed cell death-1 (PD-1)/programmed cell death ligand 1 (PD-L1) inhibitors based on the resorcinol diphenyl ether scaffold were discovered by incorporating hydrophilic moieties into the side chain and converting into the corresponding hydrochloride salt. Among these compounds, P18 showed the highest inhibitory activity against PD-1/PD-L1 with an IC50 value of 9.1 nM in a homogeneous time-resolved fluorescence binding assay. Besides, P18 promoted HepG2 cell death dose dependently in a HepG2/PD-L1 and Jurkat/PD-1 coculture cell model. Further, P18 demonstrated significantly higher water solubility (17.61 mg/mL) and improved pharmacokinetics (e.g., t(1/2) of similar to 20 h and oral bioavailability of 12%) than the previous analogues. Moreover, P18 was highly effective in suppressing tumor growth in an immune checkpoint humanized mouse model without apparent toxicity. Collectively, these results suggest that compound P18 represents a promising PD-1/PD-L1 inhibitor worthy of further investigation as a potential anticancer agent.
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Reference:
Ether – Wikipedia,
,Ether | (C2H5)2O – PubChem