Network Version
AZ-5104 Data Sheet
| Product Name: | AZ-5104 |
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|---|---|---|
| CAS No.: | 1421373-98-9 | |
| Cat. No.: | HY-B0793 | |
| MWt: | 485.58 | |
| Formula: | C27H31N7O2 | |
| Purity : | >98% | |
| Solubility: | DMSO : ≥ 28 mg/mL | |
| Mechanisms: | Target: Cancer | |
| Biological Activity: | ||
| 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 EGFRL858R/T790M, EGFRL858R, EGFRL861Q, EGFR and ErbB4, respectively. IC50 & Target:IC50: 1 nM (EGFRL858R/T790M), 6 nM (EGFRL858R),1 nM EGFRL861Q,1 nM (EGFR),1 nM (ErbB4)[1] In Vitro:AZ-5104 inhibits EGFR phosphorylation with IC50s of 2, 1, 2, 53, and 33 nM in H1975 (EGFRL858R/T790M), PC-9VanR (EGFRExon 19 deletion/T790M), PC-9 (EGFRExon 19 deletion), 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[1]. In Vivo:The metabolite, AZ5104 (5 mg/kg/day), is effective in shrinking tumors in both C/L858R and C/L+T mice[1]. | ||
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