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(S)-Sunvozertinib

Names

[ CAS No. ]:
2370013-49-1

[ Name ]:
(S)-Sunvozertinib

[Synonym ]:
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]-

Biological Activity

[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]:

Research Areas >> Cancer
Signaling Pathways >> JAK/STAT Signaling >> EGFR
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> EGFR
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> Btk

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C29H35ClFN7O3

[ Molecular Weight ]:
584.08

Related Compounds