Identification | Back Directory | [Name]
3-(benzoxazol-2-yl)-7-(diethylamino)-2-benzopyrone | [CAS]
35773-42-3 | [Synonyms]
EMI1 (EGFR MaMTH Inhibitor 1) 3-(benzoxazol-2-yl)-7-(diethylamino)-2-benzopyrone 3-(Benzoxazol-2-yl)-7-diethylamino-2H-1-benzopyran-2-one 3-(1,3-benzoxazol-2-yl)-7-(diethylamino)-2H-chromen-2-one 2H-1-Benzopyran-2-one, 3-(2-benzoxazolyl)-7-(diethylamino)- 3-(Benzoxazole-2-yl)-7-(diethylamino)-2H-1-benzopyran-2-one 7-(Diethylamino)-3-(benzoxazole-2-yl)-2H-1-benzopyran-2-one | [EINECS(EC#)]
252-721-7 | [Molecular Formula]
C20H18N2O3 | [MOL File]
35773-42-3.mol | [Molecular Weight]
334.37 |
Hazard Information | Back Directory | [Uses]
EMI1 is an EGFR ex19del/T790M/C797S and EGFR L858R/T790M/C797S inhibitor. EMI1 can be used for the research of mutant EGFR-associated, drug-resistant non-small-cell lung cancer (NSCLC)[1]. | [Biological Activity]
EMI1 (ChemBridge 5213777) is a call penetrant and potent inhibitor of EGFR signaling in EGFR L858R/T790M/C797S and ex19del/T790M/C797S triple mutants associated with drug-resistant NSCLC. AdditionallyEMI1 potently depolymerized interphase microtubulesdisrupts spindle formation and induced mitotic block in PC9 EGFR ex19del/T790M/C797S cells. EMI1 exhibits potent anti-proliferative activity against various cancer cell lines. | [IC 50]
EGFRdel19 T790M C797S; EGFRL858R/T790M/C797S | [References]
[1] Punit Saraon, et al. A drug discovery platform to identify compounds that inhibit EGFR triple mutants. Nat Chem Biol. 2020 May;16(5):577-586. DOI:10.1038/s41589-020-0484-2 |
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