|2-(5-氟-2-羟基苯基)-2-(1-氧代异吲哚啉-2-基)-N-(噻唑-2-基)乙酰胺|CsnPharm

CAS No.: 1942114-09-1

2-(5-Fluoro-2-hydroxyphenyl)-2-(1-oxoisoindolin-2-yl)-N-(thiazol-2-yl)acetamide Catalog No. CSN18738

EAI045, an allosteric inhibitor, selectively targets drug-resistant EGFR mutants like EGFR-L858R, EGFR-T790M and EGFR-L858R/T790M with IC50 of 0.019 μM, 0.19 μM and 0.002 μM respectively.

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技术信息

生物活性

描述EAI045 is an allosteric inhibitor that targets selected drug-resistant EGFR mutants but spares the wild type receptor. It inhibited cellular p-EGFR-Y1173 with IC50 values of 2nM, 163nM and >10μM for H1975 (L858R T790M), H3255 (L858R) and HaCaT (WT), respectively. It almost completely depleted p-EGFR-Y1068 at concentration of 20μM in NIH-3T3 cells expressing L858R/T790M EGFR. But it is not effective in blocking EGFR-driven proliferation in cells as a single agent due to differential potency on the two subunits of the dimeric receptor, which interact in an asymmetric manner in the active state. Combination with cetuximab which blocks EGFR dimerization could potentiate the effect of EAI045 on mouse models of lung cancer driven by L858R/T790M EGFR and by L858R/T790M/C797S EGFR, a mutant that is resistant to all currently available EGFR TKIs^[2].
作用机制EAI045 binds an allosteric site created by the displacement of the regulatory C-helix in an inactive conformation of EGFR. EAI045 is an allosteric inhibitor, which distinguished it from current EGFR TKIs target the ATP-site of the kinase.^[2]
动物研究
剂量
Mice: 60 mg/kg^[1] (p.o.)

给药途径
p.o.
参考文献

动物研究
剂量	Mice: 60 mg/kg^[1] (p.o.)
给药途径	p.o.

[1] Jia Y, Yun CH, et al. Overcoming EGFR(T790M) and EGFR(C797S) resistance with mutant-selective allosteric inhibitors. Nature. 2016 Jun 2;534(7605):129-32.
[2] Jia Y, Yun CH, Park E, Ercan D, Manuia M, Juarez J, Xu C, Rhee K, Chen T, Zhang H, Palakurthi S, Jang J, Lelais G, DiDonato M, Bursulaya B, Michellys PY, Epple R, Marsilje TH, McNeill M, Lu W, Harris J, Bender S, Wong KK, Jänne PA, Eck MJ. Overcoming EGFR(T790M) and EGFR(C797S) resistance with mutant-selective allosteric inhibitors. Nature. 2016 Jun 2;534(7605):129-32. doi: 10.1038/nature17960. Epub 2016 May 25. PMID: 27251290; PMCID: PMC4929832.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.6083 mL
- 13.0413 mL
- 26.0827 mL
- 5 mM
- 0.5217 mL
- 2.6083 mL
- 5.2165 mL
- 10 mM
- 0.2608 mL
- 1.3041 mL
- 2.6083 mL

技术信息

CAS号

1942114-09-1

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C19H14FN3O3S

运输

蓝冰

分子量

383.40

别名

溶解度

DMSO	76.0 mg/mL (198.2 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

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2-(5-Fluoro-2-hydroxyphenyl)-2-(1-oxoisoindolin-2-yl)-N-(thiazol-2-yl)acetamide Catalog No. CSN18738

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