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钻研人员设计并合成了一种光笼PI3K抑造剂1,它能够通过紫表线照射激活,开释出高效PI3K抑造剂2;衔1和2的ADME钻研通过新利luck18进行

Aberrant activation

2023-07-05
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Aberrant activation of the PI3K pathway has been intensively targeted for cancer therapeutics for decades. In this work, researchers designed and synthesized a novel photocaged PI3K inhibitor 1, which could be readily activated by UV irradiation to release a highly potent PI3K inhibitor 2. 

ADME studies of compounds 1 and 2 were conducted by Medicilon

Medicilon's pharmacokinetics department offers the clients a broad spectrum of high quality of services in the areas of in vitro ADME, in vivo pharmacokinetics and bioanalysis services, ranging from small molecules to large molecules, such as protein and antibody.

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Reference:

Kehui Zhang, et al. Design, Synthesis, and Biological Evaluation of a Novel Photocaged PI3K Inhibitor toward Precise Cancer Treatment. J Med Chem. 2021 Jun 10;64(11):7331-7340. doi: 10.1021/acs.jmedchem.0c02186. 

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