892772-75-7

892772-75-7 structure

Name: EAI001
Chemical Name: 2-(1-Oxoisoindolin-2-yl)-2-phenyl-N-(thiazol-2-yl)acetamide
CAS Number: 892772-75-7
Molecular Formula: C₁₉H₁₅N₃O₂S
Molecular Weight: 349.41
Catalog: Signaling Pathways JAK/STAT Signaling EGFR
Create Date: 2022-03-09 14:50:31
Modify Date: 2024-01-22 10:38:04
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].

Name	2-(1-Oxoisoindolin-2-yl)-2-phenyl-N-(thiazol-2-yl)acetamide
Synonyms	MFCD30187870

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	Research Areas >> Cancer Signaling Pathways >> JAK/STAT Signaling >> EGFR Signaling Pathways >> Protein Tyrosine Kinase/RTK >> EGFR
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.

Molecular Formula	C₁₉H₁₅N₃O₂S
Molecular Weight	349.41