1942114-09-1

Basic information

• Product Name: EAI-045
• Synonyms: 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;EA1045
• CAS NO: 1942114-09-1
• Molecular Formula: C19H14FN3O3S
• Molecular Weight: 383.3961632
• EINECS: -0
• Product Categories: API
• Mol File: 1942114-09-1.mol
• Article Data: 0

Chemical Properties

• Appearance: /
• Density: 1.546±0.06 g/cm3(Predicted)
• Storage Temp.: 2-8°C
• Solubility: ≥38.3 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH
• PKA: 7.20±0.50(Predicted)
• CAS DataBase Reference: EAI-045(CAS DataBase Reference)
• NIST Chemistry Reference: EAI-045(1942114-09-1)
• EPA Substance Registry System: EAI-045(1942114-09-1)

Safety Data

• Hazardous Substances Data: 1942114-09-1(Hazardous Substances Data)

Usage

Description

EAI-045 is a potent and selective fourth-generation EGFR inhibitor that targets specific drug-resistant EGFR mutants without affecting the wild-type receptor. It exhibits low-nanomolar potency in biochemical assays and effectively targets the EGFR C797S mutation, which is resistant to third-generation EGFR inhibitors such as AZD9291 (osimertinib) and CO-1686 (rociletinib). EAI-045 is a promising candidate drug for the treatment of non-small cell lung cancer (NSCLC) associated with EGFR mutations.

Uses

Used in Pharmaceutical Industry:
EAI-045 is used as an anticancer agent for the treatment of non-small cell lung cancer (NSCLC) with specific EGFR mutations. It is particularly effective against drug-resistant EGFR mutants, such as L858R/T790M, EGFRExon19del/T790M, and EGFRL858R/T790M/C797S, making it a potential therapeutic option for patients with these mutations.
Used in Cancer Research:
EAI-045 is used as a research tool to study the role of EGFR mutations in cancer progression and to develop new strategies for overcoming drug resistance in cancer treatment. Its ability to selectively target mutant EGFRs without affecting the wild-type receptor makes it a valuable compound for investigating the molecular mechanisms underlying EGFR-mediated tumor growth and resistance to EGFR inhibitors.
Used in Drug Development:
EAI-045 is used as a lead compound in the development of new drugs targeting EGFR mutations in various cancers. Its high potency and selectivity for mutant EGFRs make it an attractive candidate for further optimization and development into a more effective and safer drug for cancer treatment.

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.