AZ5104 1421373-98-9

简要描述：AZ5104 1421373-98-9
AZ5104, the demethylated metabolite of AZD-9291, is a potent EGFR inhibitor with IC50 of <1 nM, 6 nM

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AZ5104 1421373-98-9

产品描述
描述	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.
纯度	99%
储存/保存方法	Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
基本信息
可溶性/溶解性	200 mM in DMSO
生物活性
靶点	EGFR (L858R/T790M),EGFR (L861Q),EGFR (L858R),ErbB4,EGFR (wildtype),,
In vitro(体外研究)	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(体内研究)	In both C/L858R and C/L+T mice, AZ5104 (5 mg/kg/d, p.o.) induces significant and sustained tumor regression.
参考文献
参考文献	1. Cross DA, et al. Cancer Discov. 2014, 4(9), 1046-1061.

研究领域

CancerGrowth factorsEGF

CancerOncoproteins/suppressorsOncoproteinsGrowth factor receptors

CancerSignal transductionProtein phosphorylationTyrosine kinasesReceptor tyrosine kinases

CancerTumor biomarkersReceptors

Cell CycleCell differentiation

MicrobiologyOrganismVirusDNA VirusssRNA positive strand virusSARS Coronavirus

NeuroscienceDevelopment

NeuroscienceProcesses

Signal TransductionGrowth Factors/HormonesEGF

Signal TransductionProtein PhosphorylationTyrosine KinasesReceptor Tyrosine Kinases

Drug DiscoverySmall Molecule DrugLead Compound Discovery

AZ5104 1421373-98-9温馨提示：本产品仅作科研实验使用，不支持临床等研究

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