Lin, Wen-Hsing published the artcileIdentification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia, Application In Synthesis of 622-40-2, the publication is Journal of Medicinal Chemistry (2019), 62(24), 11135-11150, database is CAplus and MEDLINE.
Gastrointestinal stromal tumors (GISTs) are prototypes of stem cell factor receptor (c-KIT)-driven cancer. Two receptor tyrosine kinases, c-KIT and fms-tyrosine kinase (FLT3), are frequently mutated in AML patients, and these mutations are associated with poor prognosis. In this study, the authors discovered a multitargeted tyrosine kinase inhibitor, (6-(4-ethylpiperazin-1-yl)-2-methylpyrimidin-4-yl)(5-pyridin-4-ylthiazol-2-yl)amine Hydrochloride [2581827-29-2] (15a), with potent inhibition against single or double mutations of c-KIT developed in GISTs. Moreover, crystal structure anal. revealed the unique binding mode of (15a) with c-KIT and may elucidate its high potency in inhibiting c-KIT kinase activity. (15A) inhibited cell proliferation and induced apoptosis by targeting c-KIT in c-KIT-mutant GIST cell lines. The antitumor effects of (15a) were also demonstrated in GIST430 and GIST patient-derived xenograft (PDX) models. Further studies demonstrated that (15a) inhibited the proliferation of c-KIT- and FLT3-driven AML cells in vitro and in vivo. The results of this study suggest that (15a) may be a potential anticancer drug for the treatment of GISTs and AML.
Journal of Medicinal Chemistry published new progress about 622-40-2. 622-40-2 belongs to alcohols-buliding-blocks, auxiliary class Morpholine,Alcohol, name is 2-Morpholinoethanol, and the molecular formula is C6H13NO2, Application In Synthesis of 622-40-2.
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