
簡要描述:AZ5104 1421373-98-9AZ5104, the demethylated metabolite of AZD-9291, is a potent EGFR inhibitor with IC50 of <1 nM, 6 nM
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| 品牌 | absin | CAS | 1421373-98-9 |
|---|---|---|---|
| 分子式 | C27H31N7O2 | 純度 | 99% |
| 分子量 | 485.58 | 貨號 | abs47028060 |
| 規(guī)格 | 5mg | 供貨周期 | 現(xiàn)貨 |
| 主要用途 | is a potent EGFR inhibitor | 應(yīng)用領(lǐng)域 | 化工,生物產(chǎn)業(yè),農(nóng)林牧漁,制藥/生物制藥,綜合 |
AZ5104 1421373-98-9
| 產(chǎn)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. |
| 純度 | 99% |
| 儲存/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 | |
| 靶點 | EGFR (L858R/T790M),EGFR (L861Q),EGFR (L858R),ErbB4,EGFR (wildtype),, |
| In vitro(體外研究) | 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(體內(nèi)研究) | In both C/L858R and C/L+T mice, AZ5104 (5 mg/kg/d, p.o.) induces significant and sustained tumor regression. |
| 參考文獻(xiàn) | |
| 參考文獻(xiàn) |
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| 研究領(lǐng)域 | |
| 研究領(lǐng)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 |
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