CAS No. 1942114-09-1
| IUPAC Name | 2-(5-fluoro-2-hydroxyphenyl)-2-(3-oxo-1H-isoindol-2-yl)-N-(1,3-thiazol-2-yl)acetamide | |
|---|---|---|
| CAS Number | 1942114-09-1 | |
| Molecular Formula |
C19H14FN3O3S |
|
| Molecular Weight (MW) | 383.40 | |
| SMILES | C1C2=CC=CC=C2C(=O)N1C(C3=C(C=CC(=C3)F)O)C(=O)NC4=NC=CS4 | |
| InChIKey | YTUFHOKUFOQRDF-UHFFFAOYSA-N |
EAI045 is a potent, mutant-selective allosteric inhibitor of the epidermal growth factor receptor (EGFR). It selectively targets drug-resistant EGFR mutants, particularly L858R/T790M, while sparing the wild-type receptor. By binding to an allosteric site created by subunit asymmetry, EAI045 disrupts EGFR kinase activation and downstream signaling pathways. When combined with cetuximab, it suppresses receptor autophosphorylation and induces significant tumor growth inhibition in non-small cell lung cancer models. [1]
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Concentration
Volume
Mass
|
|---|
| Solvent | Solubility & Note |
|---|---|
| DMSO |
76 mg/mL
(198.22 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO. The recommended stock concentration is 10 mM in DMSO.) |
| Water | Insoluble |
| Ethanol | Insoluble |
| DMSO |
76 mg/mL
(198.22 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO. The recommended stock concentration is 10 mM in DMSO.) |
| Water | Insoluble |
| Ethanol | Insoluble |
| DMSO |
76 mg/mL
(198.22 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO. The recommended stock concentration is 10 mM in DMSO.) |
| Water | Insoluble |
| Ethanol | Insoluble |
- Preheat media/saline to 37°C.
- Mix rapidly (pipette/vortex) upon addition.
- For complex mixes, always add the aqueous phase last.
- Re-dissolve minor precipitates with a 37°C water bath and sonication (≤30 min).
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