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EGFR inhibitor 57

Chemical Structure : EGFR inhibitor 57

CAS No.: 2781912-10-3

EGFR inhibitor 57

Catalog No.: PC-49365Not For Human Use, Lab Use Only.

EGFR inhibitor 57 is a novel potent, selective, allosteric fourth-generation EGFR L858R inhibitor, overcomes EGFRC797S-mediated resistance in NSCLC harboring the activating EGFRL858R mutation.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

EGFR inhibitor 57 is a novel potent, selective, allosteric fourth-generation EGFR L858R inhibitor, overcomes EGFRC797S-mediated resistance in NSCLC harboring the activating EGFRL858R mutation.
EGFR inhibitor 57 is the first allosteric EGFR inhibitor that demonstrates robust tumor regression in a mutant EGFRL858R/C797S tumor model.
EGFR inhibitor 57 is active in an H1975 EGFRL858R/T790M NSCLC xenograft model and shows superior efficacy in combination with osimertinib compared to the single agents.

Physicochemical Properties

M.Wt 681.81
Formula C37H37F2N7O2S
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

2-(4-(difluoromethyl)-6-((4-((4-(hydroxymethyl)piperidin-1-yl)methyl)phenyl)ethynyl)-7-methyl-2H-indazol-2-yl)-2-(6',7'-dihydrospiro[cyclopropane-1,5'-pyrrolo[1,2-c]imidazol]-1'-yl)-N-(thiazol-2-yl)acetamide

References

1. Ulrike Obst-Sander, Journal of Medicinal Chemistry, 2022.

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