Shelf life (days): 1460.0
Formulation: A solid
Formal Name: (2'S)-3-chloro-4-[(3,5-difluoro-2-pyridinyl)methoxy]-2'-[2-(1-hydroxy-1-methylethyl)-4-pyrimidinyl]-5',6-dimethyl-[1(2H),4'-bipyridin]-2-one
Purity: ≥98%
Formula Markup: C25H22ClF2N5O3
Formula Weight: 513.9
CAS Number: 1640282-42-3
Notes: Zunsemetinib is a p38α MAPK inhibitor biased toward MAPK-activated protein kinase 2 (MK2).{67907} It selectively inhibits p38α MAPK-dependent activation of MK2 over p38α MAPK-dependent activation of MK5, also known as p38-regulated/activated protein kinase (PRAK), and p38α MAPK-dependent activation of activating transcription factor 2 (ATF2) by 750- and 700-fold, respectively. It is also greater than 350-fold selective for p38α MAPK over a panel of 193 other kinases at 5 µM. Zunsemetinib (10 µM) reduces LPS-induced increases in the levels of mRNA encoding Il-1β in isolated mouse bone marrow macrophages (BMMs). It reduces body weight loss, neutrophilia, and the number of osteoclasts at trabecular and cortical bone surfaces in a model of conditional neonatal-onset multisystem inflammatory disease (NOMIDc) using Nlrp3fl(D301N)/+;CreER mice. Zunsemetinib enhances decreases in tumor volume and increases in survival in an autochthonous KPC murine pancreatic ductal adenocarcinoma (PDAC) model when used with FIRINOX, which is a combination of the FdUMP prodrug 5-fluorouracil (Item No. 14416), DNA topoisomerase I inhibitor irinotecan (Item No. 14180), and DNA-crosslinking agent oxaliplatin (Item No. 13106).{67908}
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