PROTACPI3Kalpha degrader-1 is a PI3Kalpha-targeting PROTAC degrader (DC50= 0.08 µM) that demonstrates notable selectivity in degrading PI3Kalpha over the PI3Kbeta, PI3Kgamma, and PI3Kdelta isoforms. It degrades PI3Kalpha effectively in a time- and concentration-dependent manner and significantly inhibits the phosphorylation of AKT at the Ser473 site. Additionally, PROTACPI3Kalpha degrader-1 exhibits significant in vivo anticancer efficacy in HGC-27 and DOHH2 xenograft models.
Target-Kategorie:
PI3K|||PROTACs
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