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Sunvozertinib

Chemical Structure : Sunvozertinib

CAS No.: 2370013-49-1

Sunvozertinib (DZD9008)

Catalog No.: PC-38101Not For Human Use, Lab Use Only.

DZD9008 (Sunvozertinib) is an oral, potent, irreversible, wild type-selective EGFR inhibitor against EGFR or HER2 Exon20ins and other mutations (IC50=0.4-2.1 nM).

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

DZD9008 (Sunvozertinib) is an oral, potent, irreversible, wild type-selective EGFR inhibitor against EGFR or HER2 Exon20ins and other mutations (IC50=0.4-2.1 nM).
DZD9008 downregulates pEGFR with IC50 ranging from 1 to 22 nM in a panel of tumor cell lines expressing EGFR L858R, Exon19del, L858R/T790M, various Exon20ins or uncommon mutations.
DZD9008 shows similary potency against pHER2 in tumor cells with HER2 Exon20ins mutation, with IC50 of 7 nM.
DZD9008 is less potent in modulating pEGFR in tumor cells expressing wild type EGFR (IC50>80 nM).
DZD9008 suppressed cell proliferation with GI50 of 1 to 60 nM in tumor cells carrying EGFR L858R, Exon19del, L858R/T790M, various Exon20ins or uncommon mutations in cell proliferation assays.
DZD9008 exhibits tumor growth inhibition and regression in CDX and PDX models carrying EGFR Exon19del single mutation, L858R/T790M double mutations, and PDX models harboring G719S/L861Q or Exon20ins.

Physicochemical Properties

M.Wt 584.093
Formula C29H35ClFN7O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(S)-N-(5-((4-((5-chloro-4-fluoro-2-(2-hydroxypropan-2-yl)phenyl)amino)pyrimidin-2-yl)amino)-2-(3-(dimethylamino)pyrrolidin-1-yl)-4-methoxyphenyl)acrylamide

References

1. Yan Xu, et al. AACR Abstract 3081, Cancer Res (2019) 79 (13_Supplement): 3081.

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