EAI045 is an allosteric inhibitor targeting specific resistance EGFR mutants. There was no effect on the wild-type receptor.

 

Brand: BCM

 

Target: EGFR

 

Signaling Pathways: Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors

 

In Vitro: EAI045 potently inhibits EGFR Y1173 phosphorylation in H1975 cells (half maximal effective concentration (EC50)=2 nM), but not in HaCaT cells, a keratinocyte cell line with wild-type EGFR. Despite potent inhibition of mutant EGFR, EAI045 shows no anti-proliferative effect in the H1975 and H3255 cell lines with concentrations as high as 10 μM. EAI045 inhibits L858R/T790M mutant with an IC50 of 3 nM. However, EAI045 is not able to completely abolish EGFR autophosphorylation in H1975 NSCLC cell line harboring the L858R/T790M mutant. Dimerization-defective/independent mutants are markedly more sensitive to EAI045. Since EGFR dimerization is required for kinase enzyme activation, EAI045 may be active against one subunit of an EGFR heterodimer/asymmetric dimer.

 

pKa: 7.20±0.50(Predicted)

 

Solubility: Soluble in DMSO. Insoluble in Water; Insoluble in Ethanol.

 

GHS: GHS07

 

Isomeric SMILES: C1C2=CC=CC=C2C(=O)N1C(C3=C(C=CC(=C3)F)O)C(=O)NC4=NC=CS4  

 

InChIKey: YTUFHOKUFOQRDF-UHFFFAOYSA-N  

 

InChI: InChI=1S/C19H14FN3O3S/c20-12-5-6-15(24)14(9-12)16(17(25)22-19-21-7-8-27-19)23-10-11-3-1-2-4-13(11)18(23)26/h1-9,16,24H,10H2,(H,21,22,25)

 

Attribute
[Chem Name]	2-(5-fluoro-2-hydroxyphenyl)-2-(3-oxo-1H-isoindol-2-yl)-N-(1,3-thiazol-2-yl)acetamide
[Synonym]	EAI045
[CAS No.]	1942114-09-1
[MDL No.]	MFCD30187871
[Formula]	C19H14FN3O3S
[Molecular]	383.4
[Form]	Solid
[Storage]	Sealed in dry, 2-8°C

Goods Tag