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2370013-49-1

2370013-49-1 structure
2370013-49-1 structure
  • Name: (S)-Sunvozertinib
  • Chemical Name: DZD9008
  • CAS Number: 2370013-49-1
  • Molecular Formula: C29H35ClFN7O3
  • Molecular Weight: 584.08
  • Catalog: Signaling Pathways JAK/STAT Signaling EGFR
  • Create Date: 2021-09-12 08:24:30
  • Modify Date: 2024-01-06 11:26:08
  • (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].

Name DZD9008
Synonyms 2-Propenamide, N-[5-[[4-[[5-chloro-4-fluoro-2-(1-hydroxy-1-methylethyl)phenyl]amino]-2-pyrimidinyl]amino]-2-[(3S)-3-(dimethylamino)-1-pyrrolidinyl]-4-methoxyphenyl]-
Description (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].
Related Catalog
Target

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)

In Vitro (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].
References

[1]. Zhengtao LI, et al. Erbb/btk inhibitors. WO2019149164A1.

Molecular Formula C29H35ClFN7O3
Molecular Weight 584.08