Chemical Structure : AZ14289671
CAS No.:
AZ14289671
(AZ-14289671)
Catalog No.: PC-25435Not For Human Use, Lab Use Only.
AZ14289671 is a potent, highly selective and blood-brain barrier penetrant irreversible inhibitor of EGFR exon 20 insertion (EGFRExon20Ins) mutations, inhibits EGFR phosphorylation across EGFRExon20Ins with IC50 of 17-41 nM, spares wild-type EGFR.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
AZ14289671 is a potent, highly selective and blood-brain barrier penetrant irreversible inhibitor of EGFR exon 20 insertion (EGFRExon20Ins) mutations, inhibits EGFR phosphorylation across EGFRExon20Ins with IC50 of 17-41 nM, spares wild-type EGFR.
AZ14289671 is less potent with the mean IC50 ranging from 480 to 832 nM across EGFRWT cell lines.
AZ14289671 shows limited off-target inhibition activity against a panel of 400 kinases at 1 uM.
AZ14289671 is highly selective against EGFRExon20Ins with a high WT margin range between 10- and 50-fold depending on the pair of cell lines used.
AZ14289671 inhibits EGFR phosphorylation more extensively than sunvozertinib at lower doses in LXF2478ASV and clearly spares EGFRWT more effectively than sunvozertinib does in H2073WT.
AZ14289671 induced 133% TGI inhibition after 28 days of dosing at 50 mg/kg b.i.d. in LXF2478ASV xenografts.
Physicochemical Properties
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M.Wt
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499.30
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Formula
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C23H14Cl2F2N6O
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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1-(2-(5-(2,5-dichloropyridin-3-yl)-2,4-difluorophenyl)-1-(pyrimidin-4-yl)-4,6-dihydropyrrolo[3,4-d]imidazol-5(1H)-yl)prop-2-en-1-one
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References
1. Swaih AM, et al. Cell Rep Med. 2025 Aug 20:102305.
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