Uses
(S)-Sunvozertinib ((S)-DZD9008), the S-enantiomer of Sunvozertinib, shows inhibitory activity against EGFR exon 20 NPH and ASV insertions, EGFR L858R/T790M mutation and Her2 exon20 YVMA insertion (IC50=51.2 nM, 51.9 nM, 1 nM, and 21.2 nM, respectively). (S)-Sunvozertinib also inhibits BTK[1].
Biological Activity
(S)-Sunvozertinib ((S)-DZD9008), the S-enantiomer of Sunvozertinib, shows inhibitory activity against EGFR exon 20 NPH and ASV insertions, EGFR L858R/T790M mutation and Her2 exon20 YVMA insertion (IC50=51.2 nM, 51.9 nM, 1 nM, and 21.2 nM, respectively). (S)-Sunvozertinib also inhibits BTK[1].
(S)-Sunvozertinib shows proliferation inhibition of Ba/F3 EGFR NPH ins (GI50=139.7 nM), Ba/F3 FGFR ASV ins (155.7 nM), NCI-HI975 EGFRL858R/T790M (24.4), Her2 YVMA ins (827 nM) and WT EGFR (84.8 nM)[1].(S)-Sunvozertinib shows proliferation inhibition of BTK WT cells (OCI-LY-10, TMD-8, Ri-1and DB, with GI50 ranging from 13.7-48 nM)[1].
IC 50
EGFR exon 20 NPH: 51.2 nM (IC50); EGFR exon 20 ASV insertion: 51.9 nM (IC50); EGFRL858R/T790M: 1 nM (IC50); Her2 exon 20 YVMA insertion: 21.2 nM (IC50)
References
[1]. Zhengtao LI, et al. Erbb/btk inhibitors. WO2019149164A1.
