EAI001

Modify Date: 2024-01-22 10:38:04

EAI001 Structure
EAI001 structure
Common Name EAI001
CAS Number 892772-75-7 Molecular Weight 349.41
Density N/A Boiling Point N/A
Molecular Formula C19H15N3O2S Melting Point N/A
MSDS N/A Flash Point N/A

 Use of EAI001


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].

 Names

Name 2-(1-Oxoisoindolin-2-yl)-2-phenyl-N-(thiazol-2-yl)acetamide
Synonym More Synonyms

 EAI001 Biological Activity

Description 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].
Related Catalog
In Vitro 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].
References

[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.

 Chemical & Physical Properties

Molecular Formula C19H15N3O2S
Molecular Weight 349.41

 Synonyms

MFCD30187870