PROTAC PI3Kalpha degrader-1 is a PI3Kalpha PROTAC degrader (DC50 = 0.08 µM), demonstrating good selectivity for PI3Kalpha degradation over PI3Kbeta, PI3Kgamma, and PI3Kdelta. PROTAC PI3Kalpha degrader-1 effectively degrades PI3Kalpha in a time- and concentration-dependent, over PI3Kbeta, PI3Ky and PI3Kdelta, and potently inhibited the phosphorylation of AKT at the Ser473site. PROTAC PI3Kalpha degrader-1 shows significant in vivo anticancer efficacy in HGC-27 and DOHH2 xenograft models. (Pink: PI3Kalpha ligand : (HY-174798), Blue: E3 ligase CRBN Ligand (HY-10984), Black: Linker, E3 ligase ligand-linker conjugate (HY-W940885))[1].
Molecular Weight:
897.99
Formula:
C46H49F2N7O8S
Target:
PI3K,PROTACs
Application Notes:
MCE Product type: Reference compound
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