| Identification | Back Directory | [Name]
CMC2.24 | [CAS]
1255639-43-0 | [Synonyms]
CMC2.24
CMC2.24,CMC-2.24
4-Pentenamide, 5-(4-hydroxyphenyl)-2-[(2E)-3-(4-hydroxyphenyl)-1-oxo-2-propen-1-yl]-3-oxo-N-phenyl-, (4E)- | [Molecular Formula]
C26H21NO5 | [MDL Number]
MFCD32899876 | [MOL File]
1255639-43-0.mol | [Molecular Weight]
427.45 |
| Chemical Properties | Back Directory | [Boiling point ]
711.1±60.0 °C(Predicted) | [density ]
1.345±0.06 g/cm3(Predicted) | [storage temp. ]
-20°C, protect from light | [solubility ]
DMSO : < 1 mg/mL (insoluble or slightly soluble) | [form ]
Solid | [pka]
8.28±0.59(Predicted) | [color ]
Light yellow to orange |
| Hazard Information | Back Directory | [Uses]
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 IC50s 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[1][2][3]. | [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%.
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| [IC 50]
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) | [References]
[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. DOI:10.1002/mc.22830
[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. DOI:10.1007/s00109-020-01972-1
[3] Zhang Y, et al. Design, synthesis and biological activity of new polyenolic inhibitors of matrix metalloproteinases: a focus on chemically-modified curcumins. Curr Med Chem. 2012;19(25):4348-4358. DOI:10.2174/092986712802884295 |
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| Company Name: |
BOC Sciences
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| Tel: |
1-631-485-4226; 16314854226 |
| Website: |
https://www.bocsci.com |
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