EAI001

Names

[ Name ]:
EAI001

[Synonym ]:
MFCD30187870

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]:

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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₁₉H₁₅N₃O₂S

[ Molecular Weight ]:
349.41

Related Compounds

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