AZ5104是AZD 9291的活性去甲基化代谢物，是一种有效的 EGFR 抑制剂，抑制EGFRL858R/T790M、EGFRL858R、EGFRL861Q、EGFR 和ErbB4的IC50值分别为1、6、1、25 和 7 nM。
产品描述
AZ5104 is a potent EGFR inhibitor.
体外活性
AZ5104 shows great potency against ex19del (2 nM in PC-9), T790M (2 nM in H1975), and wild-type EGFR (33 nM in LOVO) cell lines. AZ5104 causes inhibition of cell viability with IC50 of 3.3 nM, 2.6 nM, 80 nM, and 53 nM for H1975 (T790M/L858R), PC-9 (ex19del), Calu 3 (WT), and NCI-H2073 (WT), respectively. [1]
体内活性
In both C/L858R and C/L+T mice, AZ5104 (5 mg/kg/d, p.o.) induces significant and sustained tumor regression. [1]
激酶实验
Recombinant Kinase assays: Kinase assays are performed using peptide or protein substrates in a filter-binding radioactive ATP transferase assay for protein kinases, or lipid substrates and HTRF assay for lipid kinase.
Cas No.
1421373-98-9
分子式
C27H31N7O2
分子量
485.58
储存和溶解度
DMSO:90 mg/mL (185.3 mM)
Ethanol:16 mg/mL(33 mM)
H2O:<1 mgml
Powder: -20°C for 3 years
In solvent: -80°C for 2 years
