Page last updated: 2024-11-12

cp 31398

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth

Description

CP 31398: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID9950868
CHEMBL ID186928
SCHEMBL ID13158851
SCHEMBL ID17890250
MeSH IDM0355271

Synonyms (18)

Synonym
cp-31,398
cp-31398
cp 31398
CHEMBL186928
259199-65-0
unii-in3wh41h3a
in3wh41h3a ,
1,3-propanediamine, n3-(2-(2-(4-methoxyphenyl)ethenyl)-4-quinazolinyl)-n1,n1-dimethyl-
SCHEMBL13158851
SCHEMBL17890250
bdbm389561
n''-{2-[(e)-2-(4- methoxyphenyl)vinyl]quinazolin-4- yl}-n,n-dimethylpropane-1,3- diamine
us9951029, 12
(e)-n1-(2-(4-methoxystyryl)quinazolin-4-yl)-n3,n3-dimethylpropane-1,3-diamine
1654733-02-4
1,3-propanediamine, n3-[2-[2-(4-methoxyphenyl)ethenyl]-4-quinazolinyl]-n1,n1-dimethyl-
Q27280804
n-[2-[(e)-2-(4-methoxyphenyl)ethenyl]quinazolin-4-yl]-n',n'-dimethylpropane-1,3-diamine

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" Although only modest and apparently reversible toxicities (microscopic changes in rats; reductions in body weight gain and alterations in red cell parameters in dogs) were seen in the low dose groups, no observed adverse effect levels (NOAELs) for CP-31398 could not be established for either species."( Subchronic oral toxicity and metabolite profiling of the p53 stabilizing agent, CP-31398, in rats and dogs.
Detrisac, CJ; Johnson, WD; Kapetanovic, IM; Kopelovich, L; McCormick, DL; Muzzio, M, 2011
)
0.37

Pharmacokinetics

ExcerptReferenceRelevance
" The objective of the current study was to describe the pharmacokinetic profile and tissue distribution of this novel agent following intravenous or oral (gavage and dietary) administration."( Pharmacokinetics and tissue and tumor exposure of CP-31398, a p53-stabilizing agent, in rats.
Horn, TL; Johnson, WD; Kapetanovic, IM; Kopelovich, L; McCormick, DL; Mohammed, A; Muzzio, M; Rao, CV; Thompson, TN, 2012
)
0.38
" Concentrations of CP-31398 in plasma and tissue samples were analyzed using LC–MS/MS, and the resultant data were subjected to a non-compartmental pharmacokinetic analysis."( Pharmacokinetics and tissue and tumor exposure of CP-31398, a p53-stabilizing agent, in rats.
Horn, TL; Johnson, WD; Kapetanovic, IM; Kopelovich, L; McCormick, DL; Mohammed, A; Muzzio, M; Rao, CV; Thompson, TN, 2012
)
0.38
"Bioavailability (12–32%), elimination half-life (14–20 h), clearance (4."( Pharmacokinetics and tissue and tumor exposure of CP-31398, a p53-stabilizing agent, in rats.
Horn, TL; Johnson, WD; Kapetanovic, IM; Kopelovich, L; McCormick, DL; Mohammed, A; Muzzio, M; Rao, CV; Thompson, TN, 2012
)
0.38

Compound-Compound Interactions

ExcerptReferenceRelevance
" The present study explores the effects of p53-modulating agent CP-31398 alone and combined with celecoxib on azoxymethane-induced aberrant crypt foci (ACF) and colon adenocarcinomas in F344 rats."( Inhibition of azoxymethane-induced colorectal cancer by CP-31398, a TP53 modulator, alone or in combination with low doses of celecoxib in male F344 rats.
Guruswamy, S; Kopelovich, L; Patlolla, JM; Rao, CV; Steele, VE; Swamy, MV, 2009
)
0.35

Dosage Studied

ExcerptRelevanceReference
" Levels of CP-31398 in tissues were higher after gavage dosing than after dietary administration."( Pharmacokinetics and tissue and tumor exposure of CP-31398, a p53-stabilizing agent, in rats.
Horn, TL; Johnson, WD; Kapetanovic, IM; Kopelovich, L; McCormick, DL; Mohammed, A; Muzzio, M; Rao, CV; Thompson, TN, 2012
)
0.38
"CP-31398 is bioavailable and has a relatively long elimination half-life, which supports the achievement of plasma steady-state levels with a once daily dosing regimen."( Pharmacokinetics and tissue and tumor exposure of CP-31398, a p53-stabilizing agent, in rats.
Horn, TL; Johnson, WD; Kapetanovic, IM; Kopelovich, L; McCormick, DL; Mohammed, A; Muzzio, M; Rao, CV; Thompson, TN, 2012
)
0.38
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (1)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Receptor-type tyrosine-protein kinase FLT3Homo sapiens (human)IC50 (µMol)3.81000.00010.32759.5480AID1518692
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (25)

Processvia Protein(s)Taxonomy
hemopoiesisReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
leukocyte homeostasisReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
myeloid progenitor cell differentiationReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
pro-B cell differentiationReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
cell surface receptor protein tyrosine kinase signaling pathwayReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
positive regulation of cell population proliferationReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
response to organonitrogen compoundReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
peptidyl-tyrosine phosphorylationReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
cytokine-mediated signaling pathwayReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
B cell differentiationReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
animal organ regenerationReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
common myeloid progenitor cell proliferationReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
vascular endothelial growth factor signaling pathwayReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
positive regulation of tyrosine phosphorylation of STAT proteinReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
regulation of apoptotic processReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
positive regulation of MAP kinase activityReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
positive regulation of MAPK cascadeReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
lymphocyte proliferationReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
protein autophosphorylationReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
cellular response to cytokine stimulusReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
cellular response to glucocorticoid stimulusReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
dendritic cell differentiationReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
positive regulation of kinase activityReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
multicellular organism developmentReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (10)

Processvia Protein(s)Taxonomy
protein tyrosine kinase activityReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
transmembrane receptor protein tyrosine kinase activityReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
cytokine receptor activityReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
vascular endothelial growth factor receptor activityReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
protein bindingReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
ATP bindingReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
nuclear glucocorticoid receptor bindingReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
protein-containing complex bindingReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
phosphatidylinositol 3-kinase activator activityReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
growth factor bindingReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (5)

Processvia Protein(s)Taxonomy
endoplasmic reticulumReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
endoplasmic reticulum lumenReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
plasma membraneReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
endosome membraneReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
receptor complexReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
plasma membraneReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (38)

Assay IDTitleYearJournalArticle
AID1612829Antiproliferative activity against human A549 cells after 72 hrs by CellTiter 96 aqueous one solution assay2019European journal of medicinal chemistry, Feb-01, Volume: 163The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series.
AID1556166Cytotoxicity against human HCT116 cells expressing wild type p53 incubated for 72 hrs by MTS assay2019European journal of medicinal chemistry, Sep-01, Volume: 177The synthesis and anticancer activity of 2-styrylquinoline derivatives. A p53 independent mechanism of action.
AID1612827Antiproliferative activity against p53-/- human HCT116 cells after 72 hrs by CellTiter 96 aqueous one solution assay2019European journal of medicinal chemistry, Feb-01, Volume: 163The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series.
AID252828Fold selectivity expressed as ratio of LC50 for Caki cells with non-mutant p53 to LC50 for C33A cells with a mutation at Cys 2732004Bioorganic & medicinal chemistry letters, Nov-15, Volume: 14, Issue:22
Identification and structure-activity relationship studies of 3-methylene-2-norbornanone as potent anti-proliferative agents presumably working through p53 mediated apoptosis.
AID1612811Inhibition of BRK (unknown origin) at 0.5 uM preincubated for 10 mins followed by substrate addition and measured after 1 hr by ADP-Glo luminescence assay relative to control2019European journal of medicinal chemistry, Feb-01, Volume: 163The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series.
AID1687671Induction of apoptosis in human MGC-803 cells assessed as decrease in Bcl-xL expression at 5 uM measured after 24 hrs by Western blot analysis
AID1556206Anticancer activity against human HCT116 cells assessed as inhibition of cell proliferation2019European journal of medicinal chemistry, Sep-01, Volume: 177The synthesis and anticancer activity of 2-styrylquinoline derivatives. A p53 independent mechanism of action.
AID1612816Inhibition of Lyn B (unknown origin) at 0.5 uM preincubated for 10 mins followed by substrate addition and measured after 1 hr by ADP-Glo luminescence assay relative to control2019European journal of medicinal chemistry, Feb-01, Volume: 163The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series.
AID1518692Inhibition of FLT3 ITD mutant (unknown origin) using TAMRA-Src-tide as substrate measured after 1 hr in presence of ATP at its Km concentration by IMAP-FP assay2019European journal of medicinal chemistry, Dec-15, Volume: 184Discovery and development of extreme selective inhibitors of the ITD and D835Y mutant FLT3 kinases.
AID1556167Cytotoxicity against human HCT116 cells deficient in p53 incubated for 72 hrs by MTS assay2019European journal of medicinal chemistry, Sep-01, Volume: 177The synthesis and anticancer activity of 2-styrylquinoline derivatives. A p53 independent mechanism of action.
AID1556169Cytotoxicity against human PANC1 cells harboring mutant TP53 gene incubated for 72 hrs by MTS assay2019European journal of medicinal chemistry, Sep-01, Volume: 177The synthesis and anticancer activity of 2-styrylquinoline derivatives. A p53 independent mechanism of action.
AID1687670Induction of apoptosis in human MGC-803 cells assessed as increase in Bim expression at 5 uM measured after 24 hrs by Western blot analysis
AID1612830Antiproliferative activity against human NHDF cells after 72 hrs by CellTiter 96 aqueous one solution assay2019European journal of medicinal chemistry, Feb-01, Volume: 163The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series.
AID1687668Induction of apoptosis in human MGC-803 cells assessed as decrease in Bcl-2 expression at 5 uM measured after 24 hrs by Western blot analysis
AID1612813Inhibition of CSK (unknown origin) at 0.5 uM preincubated for 10 mins followed by substrate addition and measured after 1 hr by ADP-Glo luminescence assay relative to control2019European journal of medicinal chemistry, Feb-01, Volume: 163The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series.
AID1612817Inhibition of SRC (unknown origin) at 0.5 uM preincubated for 10 mins followed by substrate addition and measured after 1 hr by ADP-Glo luminescence assay relative to control2019European journal of medicinal chemistry, Feb-01, Volume: 163The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series.
AID1687605Cytotoxicity against human A549 cells expressing wild type p53 assessed as reduction in cell viability preincubated for 48 hrs and measured after 4 hrs by MTT assay
AID249153Lethal concentration required to kill 50% Ramos RA1 cells of the human lymphocyte with a mutation at Asp 2542004Bioorganic & medicinal chemistry letters, Nov-15, Volume: 14, Issue:22
Identification and structure-activity relationship studies of 3-methylene-2-norbornanone as potent anti-proliferative agents presumably working through p53 mediated apoptosis.
AID1612828Antiproliferative activity against human MCF7 cells after 72 hrs by CellTiter 96 aqueous one solution assay2019European journal of medicinal chemistry, Feb-01, Volume: 163The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series.
AID252829Fold selectivity expressed as ratio of LC50 for Caki cells with non-mutant p53 to LC50 for Ramos RA1 cells with a mutation at Asp 2542004Bioorganic & medicinal chemistry letters, Nov-15, Volume: 14, Issue:22
Identification and structure-activity relationship studies of 3-methylene-2-norbornanone as potent anti-proliferative agents presumably working through p53 mediated apoptosis.
AID1687604Cytotoxicity against human PC-3 cells assessed as reduction in cell viability preincubated for 48 hrs and measured after 4 hrs by MTT assay
AID249152Lethal concentration required to kill 50% C33A cells of the human cervical cells with a mutation at Cys 2732004Bioorganic & medicinal chemistry letters, Nov-15, Volume: 14, Issue:22
Identification and structure-activity relationship studies of 3-methylene-2-norbornanone as potent anti-proliferative agents presumably working through p53 mediated apoptosis.
AID1612814Inhibition of Fyn A (unknown origin) at 0.5 uM preincubated for 10 mins followed by substrate addition and measured after 1 hr by ADP-Glo luminescence assay relative to control2019European journal of medicinal chemistry, Feb-01, Volume: 163The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series.
AID1612812Inhibition of BTK (unknown origin) at 0.5 uM preincubated for 10 mins followed by substrate addition and measured after 1 hr by ADP-Glo luminescence assay relative to control2019European journal of medicinal chemistry, Feb-01, Volume: 163The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series.
AID1556168Cytotoxicity against human NHDF cells incubated for 72 hrs by MTS assay2019European journal of medicinal chemistry, Sep-01, Volume: 177The synthesis and anticancer activity of 2-styrylquinoline derivatives. A p53 independent mechanism of action.
AID1612826Antiproliferative activity against p53+/+ human HCT116 cells after 72 hrs by CellTiter 96 aqueous one solution assay2019European journal of medicinal chemistry, Feb-01, Volume: 163The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series.
AID1556170Cytotoxicity against human AsPC1 cells deficit of P53 gene incubated for 72 hrs by MTS assay2019European journal of medicinal chemistry, Sep-01, Volume: 177The synthesis and anticancer activity of 2-styrylquinoline derivatives. A p53 independent mechanism of action.
AID1556171Cytotoxicity against human U251 cells harboring mutant TP53 gene incubated for 72 hrs by MTS assay2019European journal of medicinal chemistry, Sep-01, Volume: 177The synthesis and anticancer activity of 2-styrylquinoline derivatives. A p53 independent mechanism of action.
AID1687606Cytotoxicity against human HL-7702 cells expressing wild type p53 assessed as reduction in cell viability preincubated for 48 hrs and measured after 4 hrs by MTT assay
AID1687603Cytotoxicity against human DU145 cells expressing mutant type p53 assessed as reduction in cell viability preincubated for 48 hrs and measured after 4 hrs by MTT assay
AID249150Lethal concentration required to kill 50% Caki-1 cells of the human renal carcinoma with non-mutant wt p532004Bioorganic & medicinal chemistry letters, Nov-15, Volume: 14, Issue:22
Identification and structure-activity relationship studies of 3-methylene-2-norbornanone as potent anti-proliferative agents presumably working through p53 mediated apoptosis.
AID1612815Inhibition of LCK (unknown origin) at 0.5 uM preincubated for 10 mins followed by substrate addition and measured after 1 hr by ADP-Glo luminescence assay relative to control2019European journal of medicinal chemistry, Feb-01, Volume: 163The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series.
AID1687669Induction of apoptosis in human MGC-803 cells assessed as increase in Bax expression at 5 uM measured after 24 hrs by Western blot analysis
AID1687672Induction of apoptosis in human MGC-803 cells assessed as decrease in Bak expression at 5 uM measured after 24 hrs by Western blot analysis
AID1687665Antitumor activity against human PLC/PRF/5 cells xenografted in mouse assessed as tumor growth inhibition at 30 mg/kg
AID1687601Cytotoxicity against human T-24 cells expressing wild type p53 assessed as reduction in cell viability preincubated for 48 hrs and measured after 4 hrs by MTT assay
AID1687602Cytotoxicity against human MGC-803 cells expressing mutant type p53 assessed as reduction in cell viability preincubated for 48 hrs and measured after 4 hrs by MTT assay
AID1612810Inhibition of ABL1 (unknown origin) at 0.5 uM preincubated for 10 mins followed by substrate addition and measured after 1 hr by ADP-Glo luminescence assay relative to control2019European journal of medicinal chemistry, Feb-01, Volume: 163The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (59)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's2 (3.39)18.2507
2000's25 (42.37)29.6817
2010's28 (47.46)24.3611
2020's4 (6.78)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews7 (11.11%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other56 (88.89%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]