Formulation: A solid
Formal Name: 1-[6-[(4R)-4-(5-chloro-6-methyl-1H-indazol-4-yl)-5-methyl-3-(1-methyl-1H-indazol-5-yl)-1H-pyrazol-1-yl]-2-azaspiro[3.3]hept-2-yl]-2-propen-1-one
Purity: ≥98%
Formula Markup: C29H28ClN7O
Formula Weight: 526
Shelf life (days): 1460
CAS Number: 2653994-08-0
Notes: JDQ443 is a covalent inhibitor of K-RasG12C, a mutant form of K-Ras that accumulates in cancer cells.{65664} It decreases K-RasG12C-induced phosphorylation of ERK in NCI H358 non-small cell lung cancer (NSCLC) cells (IC50 = 0.020 µM). JDQ443 selectively inhibits the growth of NCI H358 cells, which express K-RasG12C, over NCI H1437 NSCLC cells expressing wild-type K-Ras and the constitutively active mutant MEKQ56P (GI50s = 0.018 and 4.4 µM, respectively). It reduces blood levels of free K-RasG12C at three, six, and 24 hours in a MiaPaCa-2 pancreatic cancer mouse xenograft model when administered at a dose of 30 mg/kg and inhibits tumor growth and decreases tumor volume in the same model at 10 and 30 mg/kg per day.
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