CMC2.24

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

CMC2.24 (TRB-N0224) 是一种新型三羰基甲烷试剂，可抑制 Ras-RAF-MEK-ERK 通路。

CMC2.24 (TRB-N0224) is a novel tricarbonylmethane agent that inhibits the Ras-RAF-MEK-ERK pathway, inhibits Ras activation in pancreatic cancer both in vitro and in vivo; inhibits Ras-GTP in MIA PaCa-2 cells and in pancreatic acinar explants isolated from KRas mutant mice; inhibits ERK1/2 activation in pancreatic cancer cells and xenografts, inhibits pancreatic cancer growth, inhibits the growth of pancreatic cancer xenografts.

CMC2.24 (0-60 μM; 24 hours) inhibits pancreatic cancer growth in vitro.CMC2.24 reduces STAT3Ser727 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. Cell Viability Assay Cell 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.

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. 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%.

TRB-N0224

MAPK/ERK Signaling

Ras

Ras

——

——

1255639-43-0

427.456

C26H21NO5

>98% (HPLC)

In Vitro:?DMSO : < 1 mg/mL (insoluble o)

——

(2E,4E)-3-hydroxy-5-(4-hydroxyphenyl)-2-((E)-3-(4-hydroxyphenyl)acryloyl)-N-phenylpenta-2,4-dienamide

(-20℃)

With Ice Pack

≥ 2 years