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Apexbio Technology LLC AZ5104 1421373-98-9 200mg

Supplier: Apexbio Technology LLC B5836200
AZ5104 (CAS 1421373-98-9) is a demethylated metabolite of AZD9291 functioning as a potent inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase It exhibits high affinity for mutant EGFR forms with IC50 values below 1 nM for EGFR L858R/T790M 6 nM for EGFR L858R 1 nM for EGFR L861Q and 25 nM for wild-type EGFR Compared to AZD9291 AZ5104 demonstrates increased potency in cellular models harboring EGFR ex19del (PC-9) T790M (H1975) and wild-type EGFR (LOVO) In vivo oral administration in mice led to a plasma metabolite level of 33% at 3 hours post-dose and 5 mg/kg/day reduced tumor growth in relevant models AZ5104 serves as a valuable tool for studying EGFR-driven cancer mechanisms and resistance
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