中文名：AZ5104
英文名：AZ5104
纯度：Moligand™，≥97%
货号：A413734
Cas号：1421373-98-9
存储温度：-20°C储存
运输条件：超低温运输
产品介绍：
Information
AZ5104, the demethylated metabolite of AZD-9291, is a potentEGFRinhibitor withIC50of <1 nM, 6 nM, 1 nM, and 25 nM for EGFR (L858R/T790M), EGFR (L858R), EGFR (L861Q), and EGFR (wildtype), respectively. Phase 1.
Targets
EGFR (L858R/T790M) ; EGFR (L861Q) ; EGFR (L858R) ; ErbB4 ; EGFR (wildtype) 15117,<1 nM; 1 nM; 6 nM; 7 nM; 25 nM
In vitro
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.
In vivo
In both C/L858R and C/L+T mice, AZ5104 (5 mg/kg/d, p.o.) induces significant and sustained tumor regression.
Cell Research(from reference)
Cell lines：H1975 (T790M/L858R), PC-9 (ex19del), Calu 3 (WT), and NCI-H2073 (WT) cells
Incubation Time：96 h
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关键字： 2-Propenamide, N-(2-((2-(dimethylamino)ethyl)methylamino)-5-((4-(1H-indol-3-yl)-2-pyrimidinyl)amino)-4-methoxyphenyl)- ; AKOS025404698 ; CCG-269587 ; 2DWZ6SE1E1
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