The author of 《Discovery of MD-224 as a First-in-Class, Highly Potent, and Efficacious Proteolysis Targeting Chimera Murine Double Minute 2 Degrader Capable of Achieving Complete and Durable Tumor Regression》 were Li, Yangbing; Yang, Jiuling; Aguilar, Angelo; McEachern, Donna; Przybranowski, Sally; Liu, Liu; Yang, Chao-Yie; Wang, Mi; Han, Xin; Wang, Shaomeng. And the article was published in Journal of Medicinal Chemistry in 2019. Recommanded Product: tert-Butyl (5-aminopentyl)carbamate The author mentioned the following in the article:
Human murine double minute 2 (MDM2) protein is a primary endogenous cellular inhibitor of the tumor suppressor p53 and has been pursued as an attractive cancer therapeutic target. Several potent, nonpeptide, small-mol. inhibitors of MDM2 are currently in clin. development. In this paper, we report our design, synthesis, and evaluation of small-mol. MDM2 degraders based on the proteolysis targeting chimera (PROTAC) concept. The most promising compound (MD-224, I) effectively induces rapid degradation of MDM2 at concentrations <1 nM in human leukemia cells. It achieves an IC50 value of 1.5 nM in inhibition of growth of RS4;11 cells and also low nanomolar IC50 values in a panel of leukemia cell lines. MD-224 (I) achieves complete and durable tumor regression in vivo in the RS4;11 xenograft tumor model in mice at well-tolerated dose schedules. MD-224 (I) is thus a highly potent and efficacious MDM2 degrader and warrants extensive evaluations as a new class of anticancer agent. In the experiment, the researchers used tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3Recommanded Product: tert-Butyl (5-aminopentyl)carbamate)
Some of the reported applications of tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3) include: synthesis of of a supermacrocycle that self-assemble to form organic nanotubes., preparation of water-soluble unsymmetrical sulforhodamine fluorophores from monobrominated sulfoxanthene dye, synthesis of functionalized porphyrins as biocompatible carrier system for photodynamic therapy (PDT).Recommanded Product: tert-Butyl (5-aminopentyl)carbamate
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