CMC2.24 (Synonyms: TRB-N0224)
目录号: PL07427 纯度: ≥96%
CAS No. :1255639-43-0
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中文名称
CMC2.24
英文名称
CMC2.24
英文别名
(2E,4E)-3-Hydroxy-5-(4-hydroxyphenyl)-2-((E)-3-(4-hydroxyphenyl)acryloyl)-N-phenylpenta-2,4-dienamide;Chembl4572462;CMC2.24
Cas No.
1255639-43-0
分子式
C26H21NO5
分子量
427.45
包装储存
-20°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
产品详情
CMC2.24 (TRB-N0224) 是一种口服活性三羰基甲烷制剂,通过抑制 Ras 及其下游效应子 ERK1/2 途径对小鼠胰腺肿瘤有效。CMC2.24 也是一种有效的锌依赖性 MMPs 抑制剂,IC50 范围为 2.0-69 μM。CMC2.24 通过恢复软骨内稳态和通过NF-κB/HIF-2α 轴抑制软骨细胞凋亡来减轻骨关节炎的进展。
生物活性
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.
性状
Solid
IC50 & Target[1][2]
RAS MMP-1 69.8 μM (IC50)
体外研究(In Vitro)
CMC2.24 (0-60 μM; 24 hours) inhibits pancreatic cancer growth in vitro.
CMC2.24 reduces STAT3 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. has not independently confirmed the accuracy of these methods. They are for reference only.Cell Viability Assay
体内研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
-20°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
参考文献
[1]. Mallangada NA, et al. A novel tricarbonylmethane agent (CMC2.24) reduces human pancreatic tumor growth in mice by targeting Ras. Mol Carcinog. 2018;57(9):1130-1143.
[2]. Zhou Y, et al. Chemically modified curcumin (CMC2.24) alleviates osteoarthritis progression by restoring cartilage homeostasis and inhibiting chondrocyte apoptosis via the NF-κB/HIF-2α axis. J Mol Med (Berl). 2020;98(10):1479-1491.
溶解度数据
In Vitro: DMSO : < 1 mg/mL (insoluble or slightly soluble)
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2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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