CMC2.24

CMC2.24 (TRB-N0224), an orally active tricarbonylmethane agent, is effective against pancreatic tumor in mice by inhibiting Ras activation and its downstream effector ERK1/2 pathway. CMC2.24 is also a potent inhibitor of zinc-dependent MMPs with IC 50 s ranging from 2.0-69 μM. CMC2.24 alleviates osteoarthritis progression by restoring cartilage homeostasis and inhibiting chondrocyte apoptosis via the NF-κB/HIF-2α axis . In Vitro CMC2.24 (0-60 μM; 24 hours) inhibits pancreatic cancer growth in vitro. CMC2.24 reduces STAT3 Ser727 phosphorylation levels, induces mitochondrial reactive oxygen species and mitochondrial cell death in pancreatic cancer cells. CMC2.24 induces mitochondrial reactive oxygen species and intrinsic apoptosis. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: AsPC-1, Panc-1, MIA PaCa-2 and BxPC-3 PC cells Concentration: 0-60 μM Incubation Time: 24 hours Result: Inhibits PC cell growth in a concentration-dependent manner. In Vivo CMC2.24 (50 mg/kg; p.o.; five times per week during 17 days) inhibits the growth of pancreatic cancer xenografts . CMC2.24 inhibits the growth of human PC through a strong cytokinetic effect. CMC2.24 inhibits ERK signaling pathway in PC cells and xenografts . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Female immune deficient BALB/c nude mice Dosage: 50 mg/kg Administration: P.o.; five times per week during 17 days Result: Reduced the rate of growth over baseline by 66.9%. Form:Solid

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