No abstract

Small-molecule irreversible tyrosine kinase inhibitors as high potent agents have led to improvements in disease-free and overall survival in patients with HER2-amplified cancer. The approved irreversible HER2 inhibitors, neratinib and pyrotinib, both lack HER2 selectivity, leading to off-target adverse events in patients. The development of HER2 mutation during treatment also hampers the progress of the treatment. We used a molecular hybridization strategy for structural optimizations, in conjunction with in vitro and in vivo drug-like property screening, to obtain a clinical candidate SPH5030. Overall, SPH5030 showed excellent activities against four frequent kinds of HER2 mutants and high relative HER2 selectivity compared with neratinib and pyrotinib, good pharmacokinetic characteristics with desirable bioavailabilities, and significant in vivo antitumor efficacy in xenograft mouse models, especially in a HER2 mutation A775_G776insYVMA xenograft mouse model with its potency much higher than those of neratinib and pyrotinib.

Sodium dehydroacetate, a common food additive and preservative, is investigated as a co‐reactant in efficient electrochemiluminescence reactions of [Ru(bpy)3]2+ for the first time. A linear electrochemiluminescence response is observed over the range of 0.001–1.0 mm with a detection limit of 0.27 μm sodium dehydroacetate. The proposed method has been applied to detect sodium dehydroacetate in baking bread with satisfactory recoveries.

SnO 2 nanomicropheres were prepared via hydro-thermal method, then the structure and micromorphology were characterized by XRD and SEM. The photocatalytic degradation ability of microspheres was studied by ultraviolet absorption. The material was pure SnO 2 nanomicrospheres with good crystallinity, uniform size, good dispersion, and strong photocatalytic degradation.