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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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| Sapitinib (AZD8931)
AZD8931 (Sapitinib) is an equipotent, reversible inhibitor of Signaling by EGFR, ERBB2 (HER2), and ERBB3 with IC50 of 4, 3, 4 nM respectively. |
| Afatinib
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| CP-724714
CP-724714 is a potent and selective orally active HER-2 tyrosine kinase inhibitor, IC50 = 3 nM. |
| Erlotinib Hydrochloride
Erlotinib is an inhibitor of human EGFR tyrosine kinase (IC50 = 2 nM) and decreases EGFR autophosphorylation in tumor cells (IC50 = 20 nM). |
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