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EAI045

目录号: PL01036 纯度: ≥99%

EAI045是突变体 EGFR 的第四代变构抑制剂，在10 μM ATP时抑制EGFR，EGFR^L858R，EGFR^T790M 和 EGFR^L858R/T790M 的IC50 值分别为1.9，0.019，0.19 和 0.002 μM。

CAS No. :1942114-09-1

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PL01036-1 mL x 10 mM (in DMSO)		¥372.00	请登录

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中文名称	EAI045
中文别名	alpha-(5-氟-2-羟基苯基)-1,3-二氢-1-氧代-N-2-噻唑基-2H-异吲哚-2-乙酰胺
英文名称	EAI045
英文别名	EAI045;EAI-045;2-(5-fluoro-2-hydroxyphenyl)-2-(3-oxo-1H-isoindol-2-yl)-N-(1,3-thiazol-2-yl)acetamide;2-(5-fluoro-2-hydroxyphenyl)-2-(1-oxo-2,3-dihydro-1H-isoindol-2-yl)-N-(1,3-thiazol-2-yl)acetamide;GTPL9222;BCP17698;s8242;EA1045;AK607730;2-(5-Fluoro-2-hydroxyphenyl)-2-(1-oxoisoindolin-2-yl)-N-(thiazol-2-yl)acetamide
Cas No.	1942114-09-1
分子式	C₁₉H₁₄FN₃O₃S
分子量	383.40
包装储存	Powder -20°C 3 years；4°C 2 years
详情描述	EAI045是突变体 EGFR 的第四代变构抑制剂，在10 μM ATP时抑制EGFR，EGFR^L858R，EGFR^T790M 和 EGFR^L858R/T790M 的IC50 值分别为1.9，0.019，0.19 和 0.002 μM。

产品详情	EAI045是突变体 EGFR 的第四代变构抑制剂，在10 μM ATP时抑制EGFR，EGFR^L858R，EGFR^T790M 和 EGFR^L858R/T790M 的IC₅₀ 值分别为1.9，0.019，0.19 和 0.002 μM。
生物活性	EAI045 is an allosteric and the fourth-generation inhibitor of mutant EGFR with IC 50 s of 1.9, 0.019, 0.19 and 0.002 μM for EGFR, EGFR, EGFR and EGFR at 10 μM ATP, respectively.
性状	Solid
IC50 & Target[1][2]	EGFR 1.9 μM (IC50) EGFR 0.019 μM (IC5
体外研究(In Vitro)	EAI045 potently inhibits EGFR Y1173 phosphorylation in H1975 cells (EC50=2 nM), but not in HaCaT cells. EAI045 is an inhibitor of the L858R/T790M mutant with 1000-fold selectivity versus wild type EGFR at 1 mM ATP. Profiling of EAI045 against a panel of 250 protein kinases reveals exquisite selectivity; no other kinases are inhibited by more than 20% at 1 μM EAI045. EAI045 has high potency and selectivity for L858R/T790M mutation. In L858R/T790M-mutant NSCLC cell line H1975 cells, EAI045 decreases but does not completely abolish the EGFR autophosphorylation. In stably transfected NIH-3T3 cells harboring the L858R/T790M EGFR mutant, EAI045 shows the same activity. In L858R-mutant H3255 cells, EAI045 exhibits moderate activity. In the HaCaT cells, a keratinocyte cell line with wild-type EGFR, EAI045 does not show any activity of inhibiting EGFR phosphorylation. It con
体内研究(In Vivo)	In a genetically engineered mouse model of L858R/T790Mmutant-driven lung cancer , remarkable tumor regression is observed in L858R/T790M-mutant mice treated with the combination of EAI045 and cetuximab. No response is seen in those mice treated with EAI045 alone. The same effect is seen in both L858R/T790M/C797S- engineered Ba/F3 cells and in mice carrying the L858R/T790M/C797S tumor xenografts. These assays clearly show that EAI045 can overcome resistance from acquired T790M and C797S mutations. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Powder -20°C 3 years；4°C 2 years
参考文献	[1]. Jia Y, et al. Overcoming EGFR(T790M) and EGFR(C797S) resistance with mutant-selective allosteric inhibitors. Nature. 2016 Jun 2;534(7605):129-32. [2]. Wang S, et al. EAI045: The fourth-generation EGFR inhibitor overcoming T790M and C797S resistance. Cancer Lett. 2017 Jan 28;385:51-54.

溶解度数据	In Vitro: DMSO : 100 mg/mL (260.82 mM; Need ultrasonic)配制储备液

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[1]. Jia Y, et al. Overcoming EGFR(T790M) and EGFR(C797S) resistance with mutant-selective allosteric inhibitors. Nature. 2016 Jun 2;534(7605):129-32.
[2]. Wang S, et al. EAI045: The fourth-generation EGFR inhibitor overcoming T790M and C797S resistance. Cancer Lett. 2017 Jan 28;385:51-54.

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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