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ChemicalBook--->CAS DataBase List--->1942114-09-1

1942114-09-1

1942114-09-1 Structure

1942114-09-1 Structure
IdentificationBack Directory
[Name]

EAI-045
[CAS]

1942114-09-1
[Synonyms]

EA1045
EAI-045
2-(5-fluoro-2-hydroxyphenyl)-2-(1-oxoisoindolin-2-yl)-N-(thiazol-2-yl)acetamide
α-(5-fluoro-2-hydroxyphenyl)-1,3-dihydro-1-oxo-N-2-thiazolyl-2H-Isoindole-2-acetamide
[Molecular Formula]

C19H14FN3O3S
[MDL Number]

MFCD30187871
[MOL File]

1942114-09-1.mol
[Molecular Weight]

383.4
Chemical PropertiesBack Directory
[density ]

1.546±0.06 g/cm3(Predicted)
[storage temp. ]

Sealed in dry,2-8°C
[solubility ]

≥38.3 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH
[form ]

solid
[pka]

7.20±0.50(Predicted)
[color ]

White to khaki
Safety DataBack Directory
[Symbol(GHS) ]


GHS07
[Signal word ]

Warning
[Hazard statements ]

H302-H315-H319-H335
[Precautionary statements ]

P261-P305+P351+P338
Questions and Answers (Q&A)Back Directory
[Description]

EAI045 is a potent and selective EGFR inhibitor (fourth generation). EAI045 targets selected drug-resistant EGFR mutants without affecting the wild-type receptor. EAI045 inhibits L858R/T790M-mutant EGFR with low-nanomolar potency in biochemical assays. Therefore, it is a potential candidate drug for the treatment of related non-small cell lung cancer (NSCLC). It should be noted that EAI-045 is effectively in targeting the EGFR C797S mutation, which is resistance to the third-generation EGFR inhibitors including AZD9291 (osimertinib) and CO-1686 (rociletinib).
[References]

Wang, S., Y. Song, and D. Liu. "EAI045: The fourth-generation EGFR inhibitor overcoming T790M and C797S resistance." Cancer Letters385(2017):51.
Jia, Y., et al. "Overcoming EGFR T790M and C797S resistance with mutant-selective allosteric inhibitors:." Nature 534.7605(2016):129.
Hazard InformationBack Directory
[Uses]

Epidermal growth factor receptor (EGFR) is a cell surface receptor often mutated in cancer cells. α-?(5-Fluoro-?2-?hydroxyphenyl)?-?1,?3-?dihydro-?1-?oxo-?N-?2-?thiazolyl-2H-?isoindole-?2-?acetamide is an allosteric EGFR inhibitor that is selective against drug-resistant EGFR mutants.
Spectrum DetailBack Directory
[Spectrum Detail]

EAI-045(1942114-09-1)1HNMR
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