EAI001

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Chemical Structure| 892772-75-7 同义名 : -
CAS号 : 892772-75-7
货号 : A1439482
分子式 : C19H15N3O2S
纯度 : 97%
分子量 : 349.406
MDL号 : MFCD30187870
存储条件：

Pure form Sealed in dry,Room Temperature

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(300.51 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 EAI001 is a potent and selective allosteric inhibitor of the mutant epidermal growth factor receptor (EGFR), exhibiting an IC50 of 24 nM for the EGFRL858R/T790M mutation. It is utilized in the research of cancer[1][2]. EAI001, at a concentration of 50 μM, interacts with the EGFR T790M/C797S/V948R mutation, which is situated deep within the EGFR near the ATP binding site and the C-helix. The inhibitory effect of EAI001 is attributed to hydrophobic interactions with the amino acids Ile759, Leu747, Leu788, Leu777, and Met766[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.86mL

0.57mL

0.29mL

14.31mL

2.86mL

1.43mL

28.62mL

5.72mL

2.86mL
参考文献

[1]Maity S, et, al. Advances in targeting EGFR allosteric site as anti-NSCLC therapy to overcome the drug resistance. Pharmacol Rep. 2020 Aug;72(4):799-813.

[2]Tinivella A, et, al. Investigating the selectivity of allosteric inhibitors for mutant t790m egfr over wild type using molecular dynamics and binding free energy calculations. 2018 Dec 4;3(12):16556-62.