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Although remarkable curative effects have been achieved in the past few decades, the emergence of drug resistance is a problem. Therefore, new inhibitors need to be developed. XHL\u201031 is a new candidate with significant inhibitory activity against T790M and C797S mutations <jats:italic>in vitro<\/jats:italic>. In order to study the pharmacokinetics <jats:italic>in vivo<\/jats:italic>, a sensitive and efficient UHPLC\u2013MS\/MS method was developed for the determination of XHL\u201031 in rat plasma in this study. The lower limit of quantitation of this method was 1\u2009ng\/ml and the linear range was 1\u20132,000\u2009ng\/ml. Method validation showed a high accuracy and precision, a high stability, a high recovery and repeatability. The method was successfully applied to the pharmacokinetic study of XHL\u201031 in rats. The results indicated that there were significant gender differences in oral absorption and the absolute bioavailability of XHL\u201031 in female rats were extremely low (&lt;10%).<\/jats:p>","DOI":"10.1002\/bmc.5059","type":"journal-article","created":{"date-parts":[[2021,1,12]],"date-time":"2021-01-12T22:33:06Z","timestamp":1610490786000},"update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":0,"title":["Development of a sensitive UHPLC\u2013MS\/MS method for the pharmacokinetics study of a novel tyrosine kinase inhibitors, 1\u2010[4\u2010(4\u2010{5\u2010Chloro\u20104\u2010[2\u2010(propane\u20102\u2010sulfonyl)\u2010phenylamino]\u2010pyrimidin\u20102\u2010ylamino}\u2010phenyl)\u2010piperazin\u20101\u2010yl]\u2010propenone in rats"],"prefix":"10.1002","volume":"35","author":[{"ORCID":"https:\/\/orcid.org\/0000-0002-6677-7061","authenticated-orcid":false,"given":"Lin","family":"Wang","sequence":"first","affiliation":[{"name":"School of Pharmacy, Key Laboratory of Molecular Pharmacology and Drug Evaluation (Yantai University), Ministry of Education, Collaborative Innovation Center of Advanced Drug Delivery System and Biotech Drugs in Universities of Shandong Yantai University  Yantai China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Xiangping","family":"Li","sequence":"additional","affiliation":[{"name":"Yantai Key Laboratory of Nanomedicine and Advanced Preparations Yantai Institute of Materia Medica  Yantai China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Ying","family":"Kong","sequence":"additional","affiliation":[{"name":"Yantai Key Laboratory of Nanomedicine and Advanced Preparations Yantai Institute of Materia Medica  Yantai China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Qiuyan","family":"Zhang","sequence":"additional","affiliation":[{"name":"Yantai Key Laboratory of Nanomedicine and Advanced Preparations Yantai Institute of Materia Medica  Yantai China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Honglei","family":"Xie","sequence":"additional","affiliation":[{"name":"Yantai Key Laboratory of Nanomedicine and Advanced Preparations Yantai Institute of Materia Medica  Yantai China"}],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"311","published-online":{"date-parts":[[2021,1,15]]},"reference":[{"key":"e_1_2_7_2_1","doi-asserted-by":"publisher","DOI":"10.1038\/nm.3388"},{"key":"e_1_2_7_3_1","doi-asserted-by":"publisher","DOI":"10.1056\/NEJMra0707704"},{"key":"e_1_2_7_4_1","doi-asserted-by":"publisher","DOI":"10.1021\/jm500973a"},{"key":"e_1_2_7_5_1","doi-asserted-by":"publisher","DOI":"10.1093\/annonc\/mdz141"},{"key":"e_1_2_7_6_1","doi-asserted-by":"publisher","DOI":"10.1056\/NEJMoa044238"},{"issue":"2","key":"e_1_2_7_7_1","first-page":"189","article-title":"Drug\u2013drug interactions, safety, and pharmacokinetics of EGFR tyrosine kinase inhibitors for the treatment of non\u2010small cell lung cancer","volume":"9","author":"Kucharczuk C. 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