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EAI045 is a fourth generation allosteric inhibitor of mutant EGFR, which inhibits EGFR at 10 μM ATP, EGFRL858R, EGFRT790M and EGFRL858R/T790M with IC50 values of 1.9, 0.019, 0.19 and 0.002 μM respectively.
| Cell Experiment | |
|---|---|
| Cell lines | H1975, H3255 and HaCaT cell lines |
| Preparation method | H1975, H3255 and HaCaT cell lines are plated in solid white 384-well plates at 500 cells per well in 10% FBS RPMI penicillin/streptomycin media. Using a Pin Tool, 50 nl of serial diluted compounds are transferred to the cells. After 3 days, cell viability is measured. |
| Concentrations | Serial dilution (0-100 μM) |
| Incubation time | 3 days |
| Animal Experiment | |
|---|---|
| Animal models | EGFR(TL) (bearing L858R/T790M point mutations) and EGFR(TD) (bearing exon19del/T790M point mutations) mice |
| Formulation | 10% NMP (10% 1-methyl-2-pyrrolidinone:90% PEG-300) |
| Dosages | 60 mg/kg |
| Administration | oral gavage |
| Molecular Weight | 383.40 |
| Formula | C19H14FN3O3S |
| CAS Number | 1942114-09-1 |
| Solubility (25°C) | 76 mg/mL in DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related EGFR/HER2 Products |
|---|
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| HKI-357
HKI-357 is an irreversible dual inhibitor of EGFR and ERBB2 with IC50s of 34 nM and 33 nM, respectively. |
| SJF-1528
SJF-1528 is a potent EGFR PROTAC degrader with DC50 values of 39.2 nM and 736.2 nM for wild-type EGFR in OVCAR8 cells and Exon 20 Ins mutated EGFR in HeLa cells. |
| CH7233163
CH7233163 is a noncovalent ATP-competitive inhibitor for EGFR-Del19/T790M/C797S. |
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