EAI001 是一个有效的选择性突变体表皮生长因子受体 (EGFR) 变构抑制剂,抑制 EGFRL858R/T790M 的 IC50 值为 24 nM。EAI001 可用于癌症研究。
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EAI001 is a potent, selective mutant epidermal growth factor receptor (EGFR) allosteric inhibitor with an IC50 value of 24 nM for EGFRL858R/T790M. EAI001 can be used for research of cancer[1][2].
EAI001 (50 μM) binds to EGFR T790M/C797S/V948R that lies deep inside the EGFR towards the ATP binding site and C-helix. EAI001 showed inhibitory activity due to hydrophobic interaction with amino acid Ile759, Leu747, Leu788, Leu777 and Met766[1].
DMNPE-caged ATP diammonium salt
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