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CHMFL-EGFR-202

CAS No. : 2089381-40-6

Biological Activity：CHMFL-EGFR-202 is a potent, irreversible inhibitor of epidermal growth factor receptor (EGFR) mutant kinase, with IC₅₀s of 5.3 nM and 8.3 nM for drug-resistant mutant EGFR T790M and WT EGFR kinases, respectively. CHMFL-EGFR-202 exhibits ∼10-fold selectivity for EGFR L858R/T790M against the EGFR wild-type in cells. CHMFL-EGFR-202 adopts a covalent “DFG-in-C-helix-out” inactive binding conformation with EGFR, with strong antiproliferative effects against EGFR mutant-driven nonsmall-cell lung cancer (NSCLC) cell lines.

Research Area：Cancer

Targets：EGFR|MEK|BMX Kinase|Btk

Related Small Molecules:Avutometinib;JAK3/BTK-IN-1;NSC81111;pp60 (v-SRC) Autophosphorylation Site, Phosphorylated;BMS-690514;Osimertinib-13C,d3;Elsubrutinib;EGFR-IN-5;FGFR2-IN-3;Cobimetinib racemate;ARQ 531;PF-06250112;PCI 29732;Genistein;Epertinib hydrochloride;EBI-1051;UNC-CA359;Osimertinib mesylate;AV-412 free base;Nelipepimut-S;Falnidamol;HER2-IN-6;PROTAC EGFR degrader 7

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