Lv, Handeng’s team published research in Pharmazie in 73 | CAS: 1942114-09-1

Pharmazie published new progress about 1942114-09-1. 1942114-09-1 belongs to indole-building-block, auxiliary class Indoline,Thiazole,Fluoride,Amine,Benzene,Amide,Alcohol,Protein Tyrosine Kinase/RTK, name is 2-(5-Fluoro-2-hydroxyphenyl)-2-(1-oxoisoindolin-2-yl)-N-(thiazol-2-yl)acetamide, and the molecular formula is C19H14FN3O3S, Quality Control of 1942114-09-1.

Lv, Handeng published the artcileAn UPLC-MS/MS method for the determination of EAI045 in plasma and tissues and its application to pharmacokinetic and distribution studies in rats, Quality Control of 1942114-09-1, the publication is Pharmazie (2018), 73(11), 630-634, database is CAplus and MEDLINE.

EAI045 represents a fourth generation allosteric EGFR TKI compound which targets T790M and C797S EGFR mutants. The study reported herein describes a method to explore the distribution of EAI045 in rat tissues as well as to quantify it in plasma. The method used here is an ultra-performance liquid chromatog.-tandem mass spectrometry with high sensitivity and selectivity. An ACQUITY UPLC BEN HILIC column with dimensions of 2.1 × 100 mm, 1.7 mum was used to sep. the analytes and IS. As mobile phase acetonitrile as well as 0.1% of formic acid/water was used combined with an elution gradient and 0.40 mL/min flow rate. This eluent was also used for electrospray ionization in pos. ion mode. A mode on multiple reactions monitoring (MRM) was also employed in the quantification. This quantification included the use of targeted segment ions with m/z 384.1 100.8 for EAI045, and m/z 285.1 193.3 for IS, resp. It was found that the linearity of this method was appropriate and the concentration range could be kept within a range of 2-2000 ng/mL for EAI045 in rat plasma and tissues. The level of EAI045 was found to be highest in the liver, followed by kidneys, lungs and heart. Furthermore, the results provided evidence that EAI045 could be absorbed quickly and distributed widely in different tissue types.

Pharmazie published new progress about 1942114-09-1. 1942114-09-1 belongs to indole-building-block, auxiliary class Indoline,Thiazole,Fluoride,Amine,Benzene,Amide,Alcohol,Protein Tyrosine Kinase/RTK, name is 2-(5-Fluoro-2-hydroxyphenyl)-2-(1-oxoisoindolin-2-yl)-N-(thiazol-2-yl)acetamide, and the molecular formula is C19H14FN3O3S, Quality Control of 1942114-09-1.

Referemce:
https://www.nature.com/articles/s41429-020-0333-2,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles