AZ5104

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

AZ5104 是 AZD-9291 的去甲基化代谢物，是一种有效的 EGFR 抑制剂。

AZ5104, the demethylated metabolite of AZD-9291, is a potent EGFR inhibitor with IC50 of <1 nM, 6 nM, 1 nM, and 25 nM for EGFR (L858R/T790M), EGFR (L858R), EGFR (L861Q), and EGFR (wildtype), respectively. Phase 1.

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.

The metabolite, AZ5104 (5 mg/kg/day), is effective in shrinking tumors in both C/L858R and C/L+T mice.

AZ5104 | AZ-5104 | AZ 5104. Demethylated AZ9291. metabolite of AZD9291

Angiogenesis

EGFR

EGFR (L858R)| EGFR (L858R/T790M)| EGFR (L861Q)| EGFR (wildtype)| HER2/ErbB2

Cancer

——

1421373-98-9

485.58

C27H31N7O2

>98% (HPLC)

Ethanol: 23 mg/mL warmed (47.36 mM); DMSO: 97 mg/mL (199.76 mM)

C=CC(NC1=CC(NC2=NC=CC(C3=CNC4=C3C=CC=C4)=N2)=C(OC)C=C1N(CCN(C)C)C)=O.

N-(5-((4-(1H-indol-3-yl)pyrimidin-2-yl)amino)-2-((2-(dimethylamino)ethyl)(methyl)amino)-4-methoxyphenyl)acrylamide

(-20℃)

With Ice Pack

≥ 2 years