| Identification | Back 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 Properties | Back 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 |
| 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.
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| Hazard Information | Back 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. |
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