EAI-045 (EAI045)

Chemical Structure : EAI-045

CAS No.: 1942114-09-1

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货号: 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.

规格	价格	库存
10 mg	￥580	In stock
25 mg	￥980	In stock
50 mg	￥1480	In stock
100 mg	￥2380	In stock
250 mg		Get quote

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生物&药学活性

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).

物理化学性质&存储条件

分子量	383.3961
分子式	C19H14FN3O3S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20 °C 12 个月; 4°C 6 个月	配置液 -80 °C 6 个月; -20°C 6 个月
Shipping
Solubility	DMSO: ≥ 28 mg/mL
Chemical Name/SMILES	2H-Isoindole-2-acetamide, α-(5-fluoro-2-hydroxyphenyl)-1,3-dihydro-1-oxo-N-2-thiazolyl-

参考文献

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.

EAI-045 (EAI045)

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物理化学性质&存储条件

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EAI-045 (EAI045)

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