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首页-小分子抑制剂&激动剂-Tyrosine Kinase-EGFR-AZ14289671
AZ14289671

Chemical Structure : AZ14289671

CAS No.:

AZ14289671 (AZ-14289671)

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

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.

物理化学性质&存储条件

分子量 499.30
分子式 C23H14Cl2F2N6O
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

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

参考文献

1. Swaih AM, et al. Cell Rep Med. 2025 Aug 20:102305.

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