EMI1

Names

[ CAS No. ]:
35773-42-3

[ Name ]:
EMI1

[Synonym ]:
3-benzooxazol-2-yl-7-diethylamino-chromen-2-one
3-(1,3-BENZOXAZOL-2-YL)-7-(DIETHYLAMINO)-2H-CHROMEN-2-ONE

Biological Activity

[Description]:

EMI1 is an EGFR ex19del/T790M/C797S and EGFR L858R/T790M/C797S inhibitor[1].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> JAK/STAT Signaling >> EGFR

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> EGFR

[Target]

EGFRdel19 T790M C797S

EGFRL858R/T790M/C797S

[In Vitro]

EMI1 inhibits PC9 EGFR ex19del/T790M/C797S organoid growth with the EC50 of 131 nM[1]. EMI1 (1 nM-10 μM) potently reduces the interaction of EGFR triple mutant with Shc1[1]. EMI1 (1 nM-100μM) strongly inhibits the viability and increase the caspase 3/7 activity of PC9 EGFR ex19del/T790M/C797S triple-mutant cells than noncancerous human bronchial epithelial (HBE) cells[1]. Cell Viability Assay[1] Cell Line: PC9 EGFR ex19del/T790M/C797S and HBE bronchial epithelial lung EGFR-WT control cells. Concentration: 0.001, 0.01, 0.1, 1, 10, 100 μM Incubation Time: 72 hours Result: Strongly inhibited the viability.

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₀H₁₈N₂O₃

[ Molecular Weight ]:
334.36900

[ Exact Mass ]:
334.13200

[ PSA ]:
59.48000

[ LogP ]:
4.44740

Safety Information

[ HS Code ]:
2934999090

Customs

[ HS Code ]: 2934999090

[ Summary ]:
2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%