Drug Information

Drug (ID: DG01654) and It's Reported Resistant Information

• Name: EAI045
• Synonyms: EAI045; 1942114-09-1; EAI-045; 2-(5-fluoro-2-hydroxyphenyl)-2-(3-oxo-1H-isoindol-2-yl)-N-(1,3-thiazol-2-yl)acetamide; CHEMBL4214567; 2-(5-Fluoro-2-hydroxyphenyl)-2-(1-oxoisoindolin-2-yl)-N-(thiazol-2-yl)acetamide; 2-(5-fluoro-2-hydroxyphenyl)-2-(1-oxo-2,3-dihydro-1H-isoindol-2-yl)-N-(1,3-thiazol-2-yl)acetamide; GTPL9222; SCHEMBL18472992; AMY9112; BCP17698; EX-A1735; BDBM50453891; s8242; AKOS030573300; CCG-268438; CS-5835; AC-29880; AS-55933; BE162167; HY-100213; F20673; Q27077145
• Target: .; NOUNIPROTAC; [1]
• Formula: 4
• IsoSMILES: C1C2=CC=CC=C2C(=O)N1C(C3=C(C=CC(=C3)F)O)C(=O)NC4=NC=CS4
• 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)
• InChIKey: YTUFHOKUFOQRDF-UHFFFAOYSA-N
• PubChem CID: 121231412

Type(s) of Resistant Mechanism of This Drug

  ADTT: Aberration of the Drug's Therapeutic Target

Drug Resistance Data Categorized by Their Corresponding Diseases

ICD-02: Benign/in-situ/malignant neoplasm

Solid tumour/cancer [ICD-11: 2A00-2F9Z]

Drug Sensitivity Data Categorized by Their Corresponding Mechanisms

Aberration of the Drug's Therapeutic Target (ADTT)

Key Molecule: Epidermal growth factor receptor (EGFR) [1]

• Molecule Alteration: Missense mutation; p.L858R (c.2573T>G)
• Sensitive Disease: Solid tumour/cancer [ICD-11: 2A00-2F9Z]
• Experimental Note: Revealed Based on the Cell Line Data
• In Vitro Model: H1975 cells; Lung; Homo sapiens (Human); CVCL_1511
• In Vitro Model: HaCaT cells; Tongue; Homo sapiens (Human); CVCL_0038
• In Vitro Model: H3255 cells; Lung; Homo sapiens (Human); CVCL_6831
• In Vitro Model: Ba/F3 cells; Colon; Homo sapiens (Human); CVCL_0161
• In Vitro Model: NIH-3T3 cells; Embryo; Mus musculus (Mouse); CVCL_0594
• In Vivo Model: Nude mouse PDX model; Mus musculus
• Experiment for Drug Resistance: CellTitre-Glo assay; MTS assay
• Mechanism Description: EAI045 is a kind of EGFR tyrosine kinase inhibitor.

References

• Ref 1: Overcoming EGFR(T790M) and EGFR(C797S) resistance with mutant-selective allosteric inhibitorsNature. 2016 Jun 2;534(7605):129-32. doi: 10.1038/nature17960. Epub 2016 May 25.