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CMC2,24
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
CMC2,24图片
CAS NO:1255639-43-0
包装与价格：
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品名称
TRB-N0224
产品介绍
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 inhibitingRasactivation and its downstream effector ERK1/2 pathway. CMC2.24 is also a potent inhibitor of zinc-dependentMMPswith IC50s ranging from 2.0-69 μM. CMC2.24 alleviates osteoarthritis progression by restoring cartilage homeostasis and inhibiting chondrocyteapoptosisvia the NF-κB/HIF-2α axis[1][2][3].

IC50& Target[1][3]

RAS

 

MMP-1

69.8 μM (IC50)

MMP-2

4.8 μM (IC50)

MMP-3

2.9 μM (IC50)

MMP-7

5 μM (IC50)

MMP-8

4.5 μM (IC50)

MMP-9

8 μM (IC50)

MMP-12

2 μM (IC50)

MMP-13

2.7 μM (IC50)

MMP-14

15.3 μM (IC50)

体外研究
(In Vitro)

CMC2.24 (0-60 μM; 24 hours) inhibits pancreatic cancer growth in vitro[1].
CMC2.24 reduces STAT3Ser727phosphorylation levels, induces mitochondrial reactive oxygen species and mitochondrial cell death in pancreatic cancer cells. CMC2.24 induces mitochondrial reactive oxygen species and intrinsic apoptosis[1].

Cell Viability Assay[1]

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.
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[1].
CMC2.24 inhibits the growth of human PC through a strong cytokinetic effect. CMC2.24 inhibits ERK signaling pathway in PC cells and xenografts[1].

Animal Model:Female immune deficient BALB/c nude mice[1]
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%.
分子量

427.45

性状

Solid

Formula

C26H21NO5

CAS 号

1255639-43-0

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)

溶解性数据
In Vitro: 

DMSO :< 1 mg/mL(insoluble or slightly soluble)