Sunvozertinib

Names

[ Name ]:
Sunvozertinib

Biological Activity

[Description]:

Sunvozertinib is a potent ErbBs (EGFR, Her2, especially mutant forms) and BTK inhibitor. Sunvozertinib shows IC50s of 20.4, 20.4, 1.1, 7.5, and 80.4 nM for EGFR exon 20 NPH insertion, EGFR exon 20 ASV insertion, EGFR L858R and T790M mutations, and Her2 Exon20 YVMA, and EGFR WT A431, respectively (patent WO2019149164A1, example 52)[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 insertion:20.4 nM (IC50)

EGFRL858R/T790M:1.1 nM (IC50)

Her2 Exon20 YVMA:7.5 nM (IC50)

[In Vitro]

Sunvozertinib shows GI50s of 60.4, 83.2, 3.3, 101.3, and 47.1 nM for EGFR exon NPH insertion, EGFR exon 20 ASV insertion, EGFR L858R and T790M mutations, and Her2 Exon20 YVMA, and EGFR WT A431, respectively. Sunvozertinib shows GI50s of 3.2, 5.8, 51.3, and 1983.5 nM for BTK WT OCI-LY-10, BTK WT TMD-8, BTK WT Ri-1, and non-BCR activated DB, respectively[1]. Sunvozertinib inhibits p-BTK with IC50 of 1.6 nM[1].

[References]

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

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₉H₃₅ClFN₇O₃

[ Molecular Weight ]:
584.08

Related Compounds

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