Drug (ID: DG01492) and It's Reported Resistant Information
Name
NSC59984
Synonyms
NSC59984; 803647-40-7; NSC 59984; (E)-1-(4-methylpiperazin-1-yl)-3-(5-nitrofuran-2-yl)prop-2-en-1-one; NSC-59984; MLS000737358; SMR000528276; 1-(4-methylpiperazin-1-yl)-3-(5-nitrofuran-2-yl)prop-2-en-1-one; CHEMBL1979662; SCHEMBL17071991; SCHEMBL17654893; BDBM96260; cid_5356520; EX-A776; HMS2885J20; BCP16647; MFCD29905462; s8106; ZINC59727553; NSC59984,NCI59984; CCG-267098; CS-5382; AC-32965; BS-18159; HY-19726; NSC59984, >=98% (HPLC); A13413; J-690353; (E)-1-(4-methylpiperazino)-3-(5-nitro-2-furyl)prop-2-en-1-one; (E)-1-(4-methyl-1-piperazinyl)-3-(5-nitro-2-furanyl)-2-propen-1-one; N-[1,3-Dimethyl-2-oxo-6-(1-pyrrolidinyl)-2,3-dihydro-1H-benzimidazol-5-yl]-2-methoxybenzamide
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Structure
Target . NOUNIPROTAC [1]
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Formula
2
IsoSMILES
CN1CCN(CC1)C(=O)/C=C/C2=CC=C(O2)[N+](=O)[O-]
InChI
InChI=1S/C12H15N3O4/c1-13-6-8-14(9-7-13)11(16)4-2-10-3-5-12(19-10)15(17)18/h2-5H,6-9H2,1H3/b4-2+
InChIKey
QKTRIGNWBRHBFV-DUXPYHPUSA-N
PubChem CID
5356520
Type(s) of Resistant Mechanism of This Drug
  UAPP: Unusual Activation of Pro-survival Pathway
Drug Resistance Data Categorized by Their Corresponding Diseases
ICD-02: Benign/in-situ/malignant neoplasm
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Colorectal cancer [ICD-11: 2B91]
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Drug Sensitivity Data Categorized by Their Corresponding Mechanisms
       Unusual Activation of Pro-survival Pathway (UAPP) Click to Show/Hide
Key Molecule: Cellular tumor antigen p53 (TP53) [1]
Molecule Alteration Missense mutation
p.R175H (c.524G>A)
Sensitive Disease Colorectal cancer [ICD-11: 2B91.1]
Experimental Note Revealed Based on the Cell Line Data
In Vitro Model SW480 cells Colon Homo sapiens (Human) CVCL_0546
HCT116 cells Colon Homo sapiens (Human) CVCL_0291
DLD-1 cells Colon Homo sapiens (Human) CVCL_0248
RXF393 cells Kidney Homo sapiens (Human) CVCL_1673
MRC5 cells Fetal lung Homo sapiens (Human) CVCL_0440
Wi38 cells Fetal lung Homo sapiens (Human) CVCL_0579
Hop92 cells Lung Homo sapiens (Human) CVCL_1286
In Vivo Model Female CRL nude mouse xenograft model Mus musculus
Experiment for
Molecule Alteration
Semi-quantitative RT-PCR; Western blotting analysis
Experiment for
Drug Resistance
CellTiter-Glo assay; Colony formation assay
Key Molecule: Cellular tumor antigen p53 (TP53) [1]
Molecule Alteration Missense mutation
p.R175L (c.524G>T)
Sensitive Disease Colorectal cancer [ICD-11: 2B91.1]
Experimental Note Revealed Based on the Cell Line Data
In Vitro Model SW480 cells Colon Homo sapiens (Human) CVCL_0546
HCT116 cells Colon Homo sapiens (Human) CVCL_0291
DLD-1 cells Colon Homo sapiens (Human) CVCL_0248
RXF393 cells Kidney Homo sapiens (Human) CVCL_1673
MRC5 cells Fetal lung Homo sapiens (Human) CVCL_0440
Wi38 cells Fetal lung Homo sapiens (Human) CVCL_0579
Hop92 cells Lung Homo sapiens (Human) CVCL_1286
In Vivo Model Female CRL nude mouse xenograft model Mus musculus
Experiment for
Molecule Alteration
Semi-quantitative RT-PCR; Western blotting analysis
Experiment for
Drug Resistance
CellTiter-Glo assay; Colony formation assay
References
Ref 1 Small-Molecule NSC59984 Restores p53 Pathway Signaling and Antitumor Effects against Colorectal Cancer via p73 Activation and Degradation of Mutant p53Cancer Res. 2015 Sep 15;75(18):3842-52. doi: 10.1158/0008-5472.CAN-13-1079. Epub 2015 Aug 20.

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