详情描述
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).
Product information
CAS Number: 35773-42-3
Molecular Weight: 334.37
Formula: C20H18N2O3
Chemical Name: 3-(1, 3-benzoxazol-2-yl)-7-(diethylamino)-2H-chromen-2-one
Smiles: CCN(CC)C1=CC2OC(=O)C(=CC=2C=C1)C1=NC2=CC=CC=C2O1
InChiKey: UJOQSHCJYVRZKJ-UHFFFAOYSA-N
InChi: InChI=1S/C20H18N2O3/c1-3-22(4-2)14-10-9-13-11-15(20(23)25-18(13)12-14)19-21-16-7-5-6-8-17(16)24-19/h5-12H,3-4H2,1-2H3
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: Soluble in DMSO
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
EMI1 inhibits PC9 EGFR ex19del/T790M/C797S organoid growth with the EC50 of 131 nM. EMI1 (1 nM-10 μM) potently reduces the interaction of EGFR triple mutant with Shc1. 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.
References:
- 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.
Products are for research use only. Not for human use.