Luecking, Ulrich published the artcileChanging for the Better: Discovery of the Highly Potent and Selective CDK9 Inhibitor VIP152 Suitable for Once Weekly Intravenous Dosing for the Treatment of Cancer, Quality Control of 1214344-25-8, the main research area is CDK9 inhibitor VIP152 weekly intravenous dosing cancer; diffuse large B cell lymphoma.
Selective inhibition of exclusively transcription-regulating pos. transcription elongation factor b/CDK9 is a promising new approach in cancer therapy. Starting from atuveciclib, the first selective CDK9 inhibitor to enter clin. development, lead optimization efforts aimed at identifying i.v. (iv) applicable CDK9 inhibitors with an improved therapeutic index led to the discovery of the highly potent and selective clin. candidate VIP152 (I). The evaluation of various scaffold hops was instrumental in the identification of VIP152, which is characterized by the underexplored benzyl sulfoximine group. VIP152 exhibited the best preclin. overall profile in vitro and in vivo, including high efficacy and good tolerability in xenograft models in mice and rats upon once weekly iv administration. VIP152 has entered clin. trials for the treatment of cancer with promising longterm, durable monotherapy activity in double-hit diffuse large B-cell lymphoma patients.
Journal of Medicinal Chemistry published new progress about Antitumor agents. 1214344-25-8 belongs to class chlorides-buliding-blocks, name is 1-(Chloromethyl)-3-fluoro-5-nitrobenzene, and the molecular formula is C7H5ClFNO2, Quality Control of 1214344-25-8.
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Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics