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Chemical Structure : EAI-045
CAS No.: 1942114-09-1
Catalog No.: PC-42087Not For Human Use, Lab Use Only.
EAI-045 (EAI045) is a potent, mutant-selective allosteric EGFR inhibitor with IC50 of 3 nM for double mutant L858R/T790M in biochemical assays at 1 mM ATP.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 25 mg | $158 | In stock | |
| 50 mg | $248 | In stock | |
| 100 mg | $398 | In stock | |
| 200 mg | Get quote | ||
| 1 g | Get quote |
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EAI-045 (EAI045) is a potent, mutant-selective allosteric EGFR inhibitor with IC50 of 3 nM for double mutant L858R/T790M in biochemical assays at 1 mM ATP.
EAI-045 (EAI045) displays >1000-fold selectivity versus wild type EGFR, also inhibits L858R and T790M with IC50 of 76 and 49 nM.
EAI-045 (EAI045) potently inhibits EGFR Y1173 phosphorylation in H1975 cells (EC50=2 nM).
EAI-045 (EAI045) exhibits true mechanistic synergy combined with cetuximab in mouse models of lung cancer driven by EGFR(L858R/T790M) and by EGFR(L858R/T790M/C797S).
| M.Wt | 383.3961 | |
| Formula | C19H14FN3O3S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
DMSO: ≥ 28 mg/mL |
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| Chemical Name/SMILES |
2H-Isoindole-2-acetamide, α-(5-fluoro-2-hydroxyphenyl)-1,3-dihydro-1-oxo-N-2-thiazolyl- |
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1. Jia Y, et al. Nature. 2016 Jun 2;534(7605):129-32.
2. Wang S, et al. J Hematol Oncol. 2016 Jul 22;9(1):59.
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