EAI-045 is the fourth-generation EGFR inhibitor overcoming T790M and C797S resistance [1]. EAI045 is an allosteric inhibitor that targets selected drug-resistant EGFR mutants but spares the wild-type receptor [2]. When combined with cetuximab that blocks EGFR dimerization, EAI-045 markedly reduces tumor growth in a mouse model of EGFR L858R/T790M and L858R/T790M/C797S-mutant-driven lung cancer [1].
Technical information:
| Chemical Formula: | C19H14FN3O3S | |
| CAS #: | 1942114-09-1 | |
| Molecular Weight: | 383.4 | |
| Purity: | > 98% | |
| Appearance: | White | |
| Chemical Name: | 2-(5-fluoro-2-hydroxyphenyl)-2-(1-oxoisoindolin-2-yl)-N-(thiazol-2-yl)acetamide | |
| Solubility: | Up to 200 mM in DMSO | |
| Synonyms: | EAI-045, EAI 045 |
Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder or DMSO solution at -20oC desiccated.
Reference:
| 1. | Jia Y, et al. Overcoming EGFR(T790M) and EGFR(C797S) resistance with mutant-selective allosteric inhibitors. Nature 2016; 534:129132. Pubmed ID: 27251290 |
| 2. | Wang S, et al. EAI045: The fourth-generation EGFR inhibitor overcoming T790M and C797S resistance. Cancer Let 2017; 385:51-54. Pubmed ID: 27840244 |
| 3. | Zhao P, et al. Crystal structure of EGFR T790M/C797S/V948R in complex with EAI045. Biochem Biophys Res Commun 2018; 502(3):332-337. Pubmed ID: 29802850 |
Other Information:
Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.