3-(benzoxazol-2-yl)-7-(diethylamino)-2-benzopyrone Chemical Properties

Melting point:

185-186 °C(Solv: N,N-dimethylformamide (68-12-2))

Boiling point:

551.0±60.0 °C(Predicted)

Density 

1.284±0.06 g/cm3(Predicted)

storage temp. 

2-8°C

solubility 

DMSO: 2mg/mL, clear

form 

Solid

pka

2.94±0.20(Predicted)

color 

Light yellow to yellow

EPA Substance Registry System

2H-1-Benzopyran-2-one, 3-(2-benzoxazolyl)-7-(diethylamino)- (35773-42-3)

3-(benzoxazol-2-yl)-7-(diethylamino)-2-benzopyrone Usage And Synthesis

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. Additionally, EMI1 potently depolymerized interphase microtubules, disrupts 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

EGFR^{del19 T790M C797S}; EGFR^{L858R/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

3-(benzoxazol-2-yl)-7-(diethylamino)-2-benzopyrone (35773-42-3)Related Product Information

• Disperse Yellow 232
• (E)-2-Styrylbenzoxazole
• 7-(diethylamino)-3-(5-methylbenzoxazol-2-yl)-2-benzopyrone
• 2-ETHYL-BENZOOXAZOLE
• BENZOOXAZOL-2-YL-ACETIC ACID
• 3-(benzoxazol-2-yl)-7-(diethylamino)-2-benzopyrone