CAS 803647-40-7|NSC59984

Introduction:Basic information about CAS 803647-40-7|NSC59984, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
Common NameNSC59984
CAS Number803647-40-7Molecular Weight265.265
Density1.3±0.1 g/cm3Boiling Point451.8±45.0 °C at 760 mmHg
Molecular FormulaC12H15N3O4Melting Point/
MSDS/Flash Point227.1±28.7 °C

Names

Name1-(4-Methyl-1-piperazinyl)-3-(5-nitro-2-furanyl)-2-propen-1-one
SynonymMore Synonyms

NSC59984 BiologicalActivity

DescriptionNSC59984 induces mutant p53 protein degradation via MDM2 and the ubiquitin-proteasome pathway. The EC50 of NSC59984 in most cancer cells is significantly lower than those of normal cells, with EC50 of 8.38 μM for p53-null HCT116 cells.IC50 value: 8.38 μM (EC50, for p53-null HCT116 cells)Target: p53in vitro: NSC59984 specifically restores p53 pathway signaling in mutant p53-expressing human colorectal cancer cells. NSC59984 induces cell death in tumor cells but not normal cells with little or no genotoxicity. NSC59984 induces mutant p53 protein degradation through MDM2-mediated ubiquitination in cancer cells. NSC59984 restores p53 pathway signaling through activation of p73. NSC59984 induces p73-dependent cell apoptosis in cancer.in vivo: NSC59984 synergizes with CPT11 to induce cell death in mutant p53-expressing colorectal cancer cells and inhibits mutant p53-associated colon tumor xenograft growth in a p73-dependent manner.
Related CatalogSignaling Pathways >>Apoptosis >>MDM-2/p53Research Areas >>Cancer
References

[1]. Zhang S, et al. Small-Molecule NSC59984 Restores p53 Pathway Signaling and Antitumor Effects against Colorectal Cancer via p73 Activation and Degradation of Mutant p53. Cancer Res. 2015 Sep 15;75(18):3842-52.

Chemical & Physical Properties

Density1.3±0.1 g/cm3
Boiling Point451.8±45.0 °C at 760 mmHg
Molecular FormulaC12H15N3O4
Molecular Weight265.265
Flash Point227.1±28.7 °C
Exact Mass265.106262
LogP0.82
Vapour Pressure0.0±1.1 mmHg at 25°C
Index of Refraction1.596
InChIKeyQKTRIGNWBRHBFV-DUXPYHPUSA-N
SMILESCN1CCN(C(=O)C=Cc2ccc([N+](=O)[O-])o2)CC1
Storage condition-20℃

Synonyms

(2E)-1-(4-Methyl-1-piperazinyl)-3-(5-nitro-2-furyl)-2-propen-1-one
2-Propen-1-one, 1-(4-methyl-1-piperazinyl)-3-(5-nitro-2-furanyl)-, (2E)-
NSC59984
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