AZ-5104 is an active, demethylated metabolite of AZD 9291. AZ-5104 is an EGFR inhibitor with IC50s of 1, 6, 1, 25 and 7 nM for EGFR, EGFR, EGFR, EGFR and ErbB4, respectively.
体外研究
AZ-5104 inhibits EGFR phosphorylation with IC50s of 2, 1, 2, 53, and 33 nM in H1975 (EGFR), PC-9VanR (EGFR), PC-9 (EGFR), H2073 (WT), and LOVO (WT), respectively. AZ5104 exhibits a reduced selectivity margin against wild-type EGFR when compared to AZD9291. AZ5104 display minimal off-target activity against other non-HER family kinases, but has the potential to target both HER2 and HER4 kinase activity.
体内研究
The metabolite, AZ5104 (5 mg/kg/day), is effective in shrinking tumors in both C/L858R and C/L+T mice.
分子式
C27H31N7O2
分子量
485.58
CAS号
1421373-98-9
运输条件
Room temperature in continental US; may vary elsewhere.