化合物AZ5104 T2491

Product Introduction
Bioactivity


英文名: AZ-5104

描述: 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。

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.

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]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: Ethanol : 16 mg/mL(33 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 90 mg/mL (185.3 mM)


关键字: AZ 5104 | Epidermal growth factor receptor | HER1 | AZ-5104 | EGFR | ErbB-1 | inhibit | AZ5104 | Inhibitor

相关产品: Dacomitinib | Olmutinib | Neratinib maleate | Erlotinib | EGFR-IN-8 | CP-380736 | Naluzotan hydrochloride | DZD1516 | EGFR-IN-73 | TX1-85-1

相关库: Angiogenesis related Compound Library | Cytokine Inhibitor Library | Membrane Protein-targeted Compound Library | Bioactive Compounds Library Max | Kinase Inhibitor Library | Inhibitor Library | Tyrosine Kinase Inhibitor Library | Anti-Pancreatic Cancer Compound Library | NO PAINS Compound Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途