aladdin 阿拉丁 A413734 AZ5104 1421373-98-9 97%

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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