Page last updated: 2024-11-06

elliptinium

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

Description

elliptinium: synthetic ellipticine deriv; RN given refers to parent cpd; structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID42723
CHEMBL ID16699
CHEBI ID135147
SCHEMBL ID17212470
MeSH IDM0089986

Synonyms (28)

Synonym
2-methyl-9-hydroxyellipticinium
9-hydroxy-2-methyl ellipticinium
brn 4153069
6h-pyrido(4,3-b)carbazolium, 9-hydroxy-2,5,11-trimethyl-
9-hydroxy-2-methylellipticinium
9-hydroxy-2,5,11-trimethyl-6h-pyrido(4,3-b)carbazolium
nsc 264137
nsc 264-137
NCI60_002117
9-hydroxy-2,5,11-trimethyl-6h-pyrido[4,3-b]carbazolium, acetate
2,5,11-trimethyl-6h-pyrido[4,3-b]carbazol-2-ium-9-ol
elliptinium
CHEBI:135147
CHEMBL16699 ,
elliptinium cation
elliptinium ion
9-hydroxy-2,5,11-trimethyl-6h-pyrido[4,3-b]carbazol-2-ium(hum)
(nmhe)9-hydroxy-2,5,11-trimethyl-6h-pyrido[4,3-b]carbazol-2-ium
9-hydroxy-2,5,11-trimethyl-6h-pyrido[4,3-b]carbazol-2-ium
bdbm50004235
58337-34-1
1f1959s062 ,
unii-1f1959s062
nsc-264137 ion
elliptinium [who-dd]
SCHEMBL17212470
Q3723538
DTXSID20866685

Research Excerpts

Overview

Elliptinium acetate (EA) is a new anti-cancer compound displaying cytostatic activity against various malignancies including hepatoma.

ExcerptReferenceRelevance
"Elliptinium acetate (EA) is a new anti-cancer compound displaying cytostatic activity against various malignancies including hepatoma. "( Conjugates of elliptinium acetate with mouse monoclonal anti-alpha-fetoprotein antibodies or Fab fragments: in vitro cytotoxic effects upon human hepatoma cell lines.
Alberici, GF; Bohuon, C; Dessaux, JJ; Fournier, J; Gros, P; Manil, L; Mondesir, JM; Pallardy, M, 1988
)
2.08

Effects

Elliottinium acetate has modest but definite activity as salvage treatment of breast cancer. Elliptinium has modest activity in advanced renal cell cancer.

ExcerptReferenceRelevance
"Elliptinium acetate has modest but definite activity as salvage treatment of breast cancer."( Phase II study of elliptinium acetate salvage treatment of advanced breast cancer.
Azab, M; Le Chevalier, T; Mondésir, JM; Rouëssé, J; Spielmann, M; Turpin, F, 1993
)
1.34
"Elliptinium has modest activity in advanced renal cell cancer and does not produce myelosuppression."( Phase II trial of elliptinium in advanced renal cell carcinoma.
Amiel, JL; Caillé, P; Droz, JP; Ducret, JP; Goodman, A; Kerbrat, P; Mondesir, JM; Rouëssé, J; Spielman, M; Theodore, C,
)
1.19

Toxicity

ExcerptReferenceRelevance
" The major side effect is nephrotoxicity."( Nephrotoxicity of an ellipticine derivative (N2-methyl-9-hydroxyellipticinium acetate) in rat: a defect of urinary concentrating ability.
Fillastre, JP; Moulin, B; Raguenez-Viotte, G; Thomas, N, 1991
)
0.28
" Toxic side effects are nausea and vomiting (one-third of the patients), hypertension (less than 10% of the patients), muscular cramp (one-third of the patients), fatigue which can be very pronounced (in most patients after 3 months of treatment), mouth dryness, and mycosis of the tongue and esophagus (less than 20% of the patients)."( Antitumor activity, pharmacology, and toxicity of ellipticines, ellipticinium, and 9-hydroxy derivatives: preliminary clinical trials of 2-methyl-9-hydroxy ellipticinium (NSC 264-137).
Amiel, JL; Dat-Xuong, N; Garnier, H; Juret, P; Le Pecq, JB; Paoletti, C; Rouesse, J, 1980
)
0.26

Pharmacokinetics

ExcerptReferenceRelevance
" In the case of 2,5-diaziridinyl-3,6-bis(carboethoxyamine)-1,4-benzoquinone, we observed about an 80-fold difference between its in vitro half-life of 40."( Application of in vivo and in vitro pharmacokinetics for physiologically relevant drug exposure in a human tumor clonogenic cell assay.
Ali-Osman, F; Dougherty, D; Giblin, J; Rosenblum, ML, 1987
)
0.27
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
carbazoles
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (3)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Mast/stem cell growth factor receptor KitHomo sapiens (human)IC50 (µMol)0.20500.00070.470810.0000AID255004; AID255976; AID255987; AID256551
Platelet-derived growth factor receptor alphaHomo sapiens (human)IC50 (µMol)0.70000.00010.491210.0000AID254810
Fibroblast growth factor receptor 3Homo sapiens (human)IC50 (µMol)0.50000.00040.28638.6200AID254753
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (124)

Processvia Protein(s)Taxonomy
ovarian follicle developmentMast/stem cell growth factor receptor KitHomo sapiens (human)
myeloid progenitor cell differentiationMast/stem cell growth factor receptor KitHomo sapiens (human)
lymphoid progenitor cell differentiationMast/stem cell growth factor receptor KitHomo sapiens (human)
immature B cell differentiationMast/stem cell growth factor receptor KitHomo sapiens (human)
mast cell chemotaxisMast/stem cell growth factor receptor KitHomo sapiens (human)
positive regulation of dendritic cell cytokine productionMast/stem cell growth factor receptor KitHomo sapiens (human)
glycosphingolipid metabolic processMast/stem cell growth factor receptor KitHomo sapiens (human)
inflammatory responseMast/stem cell growth factor receptor KitHomo sapiens (human)
signal transductionMast/stem cell growth factor receptor KitHomo sapiens (human)
spermatogenesisMast/stem cell growth factor receptor KitHomo sapiens (human)
spermatid developmentMast/stem cell growth factor receptor KitHomo sapiens (human)
germ cell migrationMast/stem cell growth factor receptor KitHomo sapiens (human)
regulation of cell shapeMast/stem cell growth factor receptor KitHomo sapiens (human)
visual learningMast/stem cell growth factor receptor KitHomo sapiens (human)
male gonad developmentMast/stem cell growth factor receptor KitHomo sapiens (human)
positive regulation of phospholipase C activityMast/stem cell growth factor receptor KitHomo sapiens (human)
cytokine-mediated signaling pathwayMast/stem cell growth factor receptor KitHomo sapiens (human)
stem cell population maintenanceMast/stem cell growth factor receptor KitHomo sapiens (human)
lamellipodium assemblyMast/stem cell growth factor receptor KitHomo sapiens (human)
actin cytoskeleton organizationMast/stem cell growth factor receptor KitHomo sapiens (human)
hemopoiesisMast/stem cell growth factor receptor KitHomo sapiens (human)
T cell differentiationMast/stem cell growth factor receptor KitHomo sapiens (human)
erythrocyte differentiationMast/stem cell growth factor receptor KitHomo sapiens (human)
melanocyte differentiationMast/stem cell growth factor receptor KitHomo sapiens (human)
positive regulation of pseudopodium assemblyMast/stem cell growth factor receptor KitHomo sapiens (human)
positive regulation of mast cell cytokine productionMast/stem cell growth factor receptor KitHomo sapiens (human)
somatic stem cell population maintenanceMast/stem cell growth factor receptor KitHomo sapiens (human)
embryonic hemopoiesisMast/stem cell growth factor receptor KitHomo sapiens (human)
ectopic germ cell programmed cell deathMast/stem cell growth factor receptor KitHomo sapiens (human)
intracellular signal transductionMast/stem cell growth factor receptor KitHomo sapiens (human)
hematopoietic stem cell migrationMast/stem cell growth factor receptor KitHomo sapiens (human)
megakaryocyte developmentMast/stem cell growth factor receptor KitHomo sapiens (human)
Fc receptor signaling pathwayMast/stem cell growth factor receptor KitHomo sapiens (human)
Kit signaling pathwayMast/stem cell growth factor receptor KitHomo sapiens (human)
erythropoietin-mediated signaling pathwayMast/stem cell growth factor receptor KitHomo sapiens (human)
regulation of cell population proliferationMast/stem cell growth factor receptor KitHomo sapiens (human)
positive regulation of tyrosine phosphorylation of STAT proteinMast/stem cell growth factor receptor KitHomo sapiens (human)
negative regulation of programmed cell deathMast/stem cell growth factor receptor KitHomo sapiens (human)
mast cell degranulationMast/stem cell growth factor receptor KitHomo sapiens (human)
positive regulation of MAPK cascadeMast/stem cell growth factor receptor KitHomo sapiens (human)
pigmentationMast/stem cell growth factor receptor KitHomo sapiens (human)
tongue developmentMast/stem cell growth factor receptor KitHomo sapiens (human)
positive regulation of Notch signaling pathwayMast/stem cell growth factor receptor KitHomo sapiens (human)
positive regulation of receptor signaling pathway via JAK-STATMast/stem cell growth factor receptor KitHomo sapiens (human)
response to cadmium ionMast/stem cell growth factor receptor KitHomo sapiens (human)
protein autophosphorylationMast/stem cell growth factor receptor KitHomo sapiens (human)
positive regulation of long-term neuronal synaptic plasticityMast/stem cell growth factor receptor KitHomo sapiens (human)
digestive tract developmentMast/stem cell growth factor receptor KitHomo sapiens (human)
stem cell differentiationMast/stem cell growth factor receptor KitHomo sapiens (human)
epithelial cell proliferationMast/stem cell growth factor receptor KitHomo sapiens (human)
detection of mechanical stimulus involved in sensory perception of soundMast/stem cell growth factor receptor KitHomo sapiens (human)
positive regulation of DNA-binding transcription factor activityMast/stem cell growth factor receptor KitHomo sapiens (human)
negative regulation of developmental processMast/stem cell growth factor receptor KitHomo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionMast/stem cell growth factor receptor KitHomo sapiens (human)
cell chemotaxisMast/stem cell growth factor receptor KitHomo sapiens (human)
mast cell differentiationMast/stem cell growth factor receptor KitHomo sapiens (human)
mast cell proliferationMast/stem cell growth factor receptor KitHomo sapiens (human)
positive regulation of mast cell proliferationMast/stem cell growth factor receptor KitHomo sapiens (human)
melanocyte migrationMast/stem cell growth factor receptor KitHomo sapiens (human)
melanocyte adhesionMast/stem cell growth factor receptor KitHomo sapiens (human)
positive regulation of pyloric antrum smooth muscle contractionMast/stem cell growth factor receptor KitHomo sapiens (human)
regulation of bile acid metabolic processMast/stem cell growth factor receptor KitHomo sapiens (human)
positive regulation of colon smooth muscle contractionMast/stem cell growth factor receptor KitHomo sapiens (human)
positive regulation of small intestine smooth muscle contractionMast/stem cell growth factor receptor KitHomo sapiens (human)
positive regulation of vascular associated smooth muscle cell differentiationMast/stem cell growth factor receptor KitHomo sapiens (human)
negative regulation of reproductive processMast/stem cell growth factor receptor KitHomo sapiens (human)
positive regulation of cell migrationMast/stem cell growth factor receptor KitHomo sapiens (human)
positive regulation of MAP kinase activityMast/stem cell growth factor receptor KitHomo sapiens (human)
multicellular organism developmentMast/stem cell growth factor receptor KitHomo sapiens (human)
B cell differentiationMast/stem cell growth factor receptor KitHomo sapiens (human)
hematopoietic progenitor cell differentiationMast/stem cell growth factor receptor KitHomo sapiens (human)
cellular response to reactive oxygen speciesPlatelet-derived growth factor receptor alphaHomo sapiens (human)
luteinizationPlatelet-derived growth factor receptor alphaHomo sapiens (human)
in utero embryonic developmentPlatelet-derived growth factor receptor alphaHomo sapiens (human)
cell activationPlatelet-derived growth factor receptor alphaHomo sapiens (human)
hematopoietic progenitor cell differentiationPlatelet-derived growth factor receptor alphaHomo sapiens (human)
estrogen metabolic processPlatelet-derived growth factor receptor alphaHomo sapiens (human)
positive regulation of cell population proliferationPlatelet-derived growth factor receptor alphaHomo sapiens (human)
negative regulation of platelet activationPlatelet-derived growth factor receptor alphaHomo sapiens (human)
positive regulation of phospholipase C activityPlatelet-derived growth factor receptor alphaHomo sapiens (human)
peptidyl-tyrosine phosphorylationPlatelet-derived growth factor receptor alphaHomo sapiens (human)
signal transduction involved in regulation of gene expressionPlatelet-derived growth factor receptor alphaHomo sapiens (human)
extracellular matrix organizationPlatelet-derived growth factor receptor alphaHomo sapiens (human)
lung developmentPlatelet-derived growth factor receptor alphaHomo sapiens (human)
adrenal gland developmentPlatelet-derived growth factor receptor alphaHomo sapiens (human)
positive regulation of cell migrationPlatelet-derived growth factor receptor alphaHomo sapiens (human)
male genitalia developmentPlatelet-derived growth factor receptor alphaHomo sapiens (human)
regulation of actin cytoskeleton organizationPlatelet-derived growth factor receptor alphaHomo sapiens (human)
Leydig cell differentiationPlatelet-derived growth factor receptor alphaHomo sapiens (human)
platelet-derived growth factor receptor-alpha signaling pathwayPlatelet-derived growth factor receptor alphaHomo sapiens (human)
positive regulation of cell proliferation by VEGF-activated platelet derived growth factor receptor signaling pathwayPlatelet-derived growth factor receptor alphaHomo sapiens (human)
wound healingPlatelet-derived growth factor receptor alphaHomo sapiens (human)
odontogenesis of dentin-containing toothPlatelet-derived growth factor receptor alphaHomo sapiens (human)
protein autophosphorylationPlatelet-derived growth factor receptor alphaHomo sapiens (human)
platelet-derived growth factor receptor signaling pathwayPlatelet-derived growth factor receptor alphaHomo sapiens (human)
positive regulation of fibroblast proliferationPlatelet-derived growth factor receptor alphaHomo sapiens (human)
embryonic digestive tract morphogenesisPlatelet-derived growth factor receptor alphaHomo sapiens (human)
embryonic cranial skeleton morphogenesisPlatelet-derived growth factor receptor alphaHomo sapiens (human)
embryonic skeletal system morphogenesisPlatelet-derived growth factor receptor alphaHomo sapiens (human)
positive regulation of calcium-mediated signalingPlatelet-derived growth factor receptor alphaHomo sapiens (human)
white fat cell differentiationPlatelet-derived growth factor receptor alphaHomo sapiens (human)
positive regulation of chemotaxisPlatelet-derived growth factor receptor alphaHomo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionPlatelet-derived growth factor receptor alphaHomo sapiens (human)
cardiac myofibril assemblyPlatelet-derived growth factor receptor alphaHomo sapiens (human)
roof of mouth developmentPlatelet-derived growth factor receptor alphaHomo sapiens (human)
face morphogenesisPlatelet-derived growth factor receptor alphaHomo sapiens (human)
cell chemotaxisPlatelet-derived growth factor receptor alphaHomo sapiens (human)
retina vasculature development in camera-type eyePlatelet-derived growth factor receptor alphaHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadePlatelet-derived growth factor receptor alphaHomo sapiens (human)
platelet aggregationPlatelet-derived growth factor receptor alphaHomo sapiens (human)
cellular response to amino acid stimulusPlatelet-derived growth factor receptor alphaHomo sapiens (human)
metanephric glomerular capillary formationPlatelet-derived growth factor receptor alphaHomo sapiens (human)
regulation of mesenchymal stem cell differentiationPlatelet-derived growth factor receptor alphaHomo sapiens (human)
cell surface receptor protein tyrosine kinase signaling pathwayPlatelet-derived growth factor receptor alphaHomo sapiens (human)
positive regulation of kinase activityPlatelet-derived growth factor receptor alphaHomo sapiens (human)
multicellular organism developmentPlatelet-derived growth factor receptor alphaHomo sapiens (human)
positive regulation of cell population proliferationFibroblast growth factor receptor 3Homo sapiens (human)
fibroblast growth factor receptor signaling pathwayFibroblast growth factor receptor 3Homo sapiens (human)
MAPK cascadeFibroblast growth factor receptor 3Homo sapiens (human)
skeletal system developmentFibroblast growth factor receptor 3Homo sapiens (human)
endochondral ossificationFibroblast growth factor receptor 3Homo sapiens (human)
chondrocyte differentiationFibroblast growth factor receptor 3Homo sapiens (human)
endochondral bone growthFibroblast growth factor receptor 3Homo sapiens (human)
cell surface receptor signaling pathway via JAK-STATFibroblast growth factor receptor 3Homo sapiens (human)
cell-cell signalingFibroblast growth factor receptor 3Homo sapiens (human)
positive regulation of cell population proliferationFibroblast growth factor receptor 3Homo sapiens (human)
fibroblast growth factor receptor signaling pathwayFibroblast growth factor receptor 3Homo sapiens (human)
positive regulation of phospholipase activityFibroblast growth factor receptor 3Homo sapiens (human)
bone mineralizationFibroblast growth factor receptor 3Homo sapiens (human)
chondrocyte proliferationFibroblast growth factor receptor 3Homo sapiens (human)
positive regulation of tyrosine phosphorylation of STAT proteinFibroblast growth factor receptor 3Homo sapiens (human)
positive regulation of MAPK cascadeFibroblast growth factor receptor 3Homo sapiens (human)
negative regulation of developmental growthFibroblast growth factor receptor 3Homo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionFibroblast growth factor receptor 3Homo sapiens (human)
bone morphogenesisFibroblast growth factor receptor 3Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeFibroblast growth factor receptor 3Homo sapiens (human)
bone maturationFibroblast growth factor receptor 3Homo sapiens (human)
fibroblast growth factor receptor apoptotic signaling pathwayFibroblast growth factor receptor 3Homo sapiens (human)
cell surface receptor protein tyrosine kinase signaling pathwayFibroblast growth factor receptor 3Homo sapiens (human)
multicellular organism developmentFibroblast growth factor receptor 3Homo sapiens (human)
positive regulation of kinase activityFibroblast growth factor receptor 3Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (21)

Processvia Protein(s)Taxonomy
protease bindingMast/stem cell growth factor receptor KitHomo sapiens (human)
protein tyrosine kinase activityMast/stem cell growth factor receptor KitHomo sapiens (human)
transmembrane receptor protein tyrosine kinase activityMast/stem cell growth factor receptor KitHomo sapiens (human)
stem cell factor receptor activityMast/stem cell growth factor receptor KitHomo sapiens (human)
protein bindingMast/stem cell growth factor receptor KitHomo sapiens (human)
ATP bindingMast/stem cell growth factor receptor KitHomo sapiens (human)
cytokine bindingMast/stem cell growth factor receptor KitHomo sapiens (human)
SH2 domain bindingMast/stem cell growth factor receptor KitHomo sapiens (human)
protein homodimerization activityMast/stem cell growth factor receptor KitHomo sapiens (human)
metal ion bindingMast/stem cell growth factor receptor KitHomo sapiens (human)
growth factor bindingMast/stem cell growth factor receptor KitHomo sapiens (human)
protein kinase activityPlatelet-derived growth factor receptor alphaHomo sapiens (human)
transmembrane receptor protein tyrosine kinase activityPlatelet-derived growth factor receptor alphaHomo sapiens (human)
platelet-derived growth factor alpha-receptor activityPlatelet-derived growth factor receptor alphaHomo sapiens (human)
vascular endothelial growth factor receptor activityPlatelet-derived growth factor receptor alphaHomo sapiens (human)
platelet-derived growth factor receptor bindingPlatelet-derived growth factor receptor alphaHomo sapiens (human)
protein bindingPlatelet-derived growth factor receptor alphaHomo sapiens (human)
ATP bindingPlatelet-derived growth factor receptor alphaHomo sapiens (human)
vascular endothelial growth factor bindingPlatelet-derived growth factor receptor alphaHomo sapiens (human)
protein homodimerization activityPlatelet-derived growth factor receptor alphaHomo sapiens (human)
protein-containing complex bindingPlatelet-derived growth factor receptor alphaHomo sapiens (human)
platelet-derived growth factor bindingPlatelet-derived growth factor receptor alphaHomo sapiens (human)
protein tyrosine kinase activityFibroblast growth factor receptor 3Homo sapiens (human)
fibroblast growth factor receptor activityFibroblast growth factor receptor 3Homo sapiens (human)
protein bindingFibroblast growth factor receptor 3Homo sapiens (human)
ATP bindingFibroblast growth factor receptor 3Homo sapiens (human)
fibroblast growth factor bindingFibroblast growth factor receptor 3Homo sapiens (human)
identical protein bindingFibroblast growth factor receptor 3Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (23)

Processvia Protein(s)Taxonomy
fibrillar centerMast/stem cell growth factor receptor KitHomo sapiens (human)
acrosomal vesicleMast/stem cell growth factor receptor KitHomo sapiens (human)
extracellular spaceMast/stem cell growth factor receptor KitHomo sapiens (human)
plasma membraneMast/stem cell growth factor receptor KitHomo sapiens (human)
cell-cell junctionMast/stem cell growth factor receptor KitHomo sapiens (human)
external side of plasma membraneMast/stem cell growth factor receptor KitHomo sapiens (human)
cytoplasmic side of plasma membraneMast/stem cell growth factor receptor KitHomo sapiens (human)
plasma membraneMast/stem cell growth factor receptor KitHomo sapiens (human)
receptor complexMast/stem cell growth factor receptor KitHomo sapiens (human)
nucleusPlatelet-derived growth factor receptor alphaHomo sapiens (human)
nucleoplasmPlatelet-derived growth factor receptor alphaHomo sapiens (human)
cytoplasmPlatelet-derived growth factor receptor alphaHomo sapiens (human)
endoplasmic reticulum membranePlatelet-derived growth factor receptor alphaHomo sapiens (human)
Golgi apparatusPlatelet-derived growth factor receptor alphaHomo sapiens (human)
plasma membranePlatelet-derived growth factor receptor alphaHomo sapiens (human)
microvillusPlatelet-derived growth factor receptor alphaHomo sapiens (human)
ciliumPlatelet-derived growth factor receptor alphaHomo sapiens (human)
external side of plasma membranePlatelet-derived growth factor receptor alphaHomo sapiens (human)
membranePlatelet-derived growth factor receptor alphaHomo sapiens (human)
cell junctionPlatelet-derived growth factor receptor alphaHomo sapiens (human)
protein-containing complexPlatelet-derived growth factor receptor alphaHomo sapiens (human)
receptor complexPlatelet-derived growth factor receptor alphaHomo sapiens (human)
plasma membranePlatelet-derived growth factor receptor alphaHomo sapiens (human)
focal adhesionFibroblast growth factor receptor 3Homo sapiens (human)
extracellular regionFibroblast growth factor receptor 3Homo sapiens (human)
endoplasmic reticulumFibroblast growth factor receptor 3Homo sapiens (human)
Golgi apparatusFibroblast growth factor receptor 3Homo sapiens (human)
plasma membraneFibroblast growth factor receptor 3Homo sapiens (human)
cell surfaceFibroblast growth factor receptor 3Homo sapiens (human)
transport vesicleFibroblast growth factor receptor 3Homo sapiens (human)
receptor complexFibroblast growth factor receptor 3Homo sapiens (human)
plasma membraneFibroblast growth factor receptor 3Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (33)

Assay IDTitleYearJournalArticle
AID117798The effect on NADH oxidation in the presence of MPO-H2O2.1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Bioactivation of the antitumor drugs 9-hydroxyellipticine and derivatives by a peroxidase-hydrogen peroxide system.
AID143741Compound was evaluated for inhibitory activity against N 417 human lung cancer cell line1992Journal of medicinal chemistry, Dec-25, Volume: 35, Issue:26
N-methylcarbamate derivatives of ellipticine and olivacine with cytotoxic activity against four human lung cancer cell lines.
AID96662Dose that reduces the L1210 leukemia cell growth in vitro by 50% after 48 hr as compared to controls1984Journal of medicinal chemistry, Sep, Volume: 27, Issue:9
Potential antitumor agents: synthesis and biological properties of aliphatic amino acid 9-hydroxyellipticinium derivatives.
AID137546Percent median survival time of mice injected with P388 leukemia, at a subcutaneous compound dose of 20 mg/kg1999Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12
Synthesis of 9-O-substituted derivatives of 9-hydroxy-5, 6-dimethyl-6H-pyrido[4,3-b]carbazole-1-carboxylic acid (2-(dimethylamino)ethyl)amide and their 10- and 11-methyl analogues with improved antitumor activity.
AID132189Percent Increase in life span (ILS) over controls (10e5 L1210 leukemia cells) at LD0/2 by ip administration of the drug into mouse (single injection 2 hr after cell grafting)1984Journal of medicinal chemistry, Sep, Volume: 27, Issue:9
Potential antitumor agents: synthesis and biological properties of aliphatic amino acid 9-hydroxyellipticinium derivatives.
AID96665Growth inhibitory activity against L1210 lymphocytic leukemia cells.1983Journal of medicinal chemistry, Oct, Volume: 26, Issue:10
Autoxidation of the antitumor drug 9-hydroxyellipticine and its derivatives.
AID134221Compound tested in vivo for highest nontoxic lethal dose administered intraperitoneally that reduces the L1210 leukemia cell growth1984Journal of medicinal chemistry, Sep, Volume: 27, Issue:9
Potential antitumor agents: synthesis and biological properties of aliphatic amino acid 9-hydroxyellipticinium derivatives.
AID116287Increase in life span over controls (10e5 cells) in mice after intraperitoneal treatment of the compound.1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Bioactivation of the antitumor drugs 9-hydroxyellipticine and derivatives by a peroxidase-hydrogen peroxide system.
AID99082Inhibition of murine L1210 leukemia cell proliferation measured by the MTT assay1999Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12
Synthesis of 9-O-substituted derivatives of 9-hydroxy-5, 6-dimethyl-6H-pyrido[4,3-b]carbazole-1-carboxylic acid (2-(dimethylamino)ethyl)amide and their 10- and 11-methyl analogues with improved antitumor activity.
AID98677In vitro concentration required for growth inhibition of murine L1210 tumor cell1980Journal of medicinal chemistry, Nov, Volume: 23, Issue:11
Structure-activity relationships in a series of newly synthesized 1-amino-substituted ellipticine derivatives.
AID26756DNA binding dissociation constant as KD1984Journal of medicinal chemistry, Apr, Volume: 27, Issue:4
Interactions of antitumor drugs with natural DNA: 1H NMR study of binding mode and kinetics.
AID135241Long-term survivors among 7 mice infected with B16 melanoma, scored on day 60 at 20 mg/kg dose1999Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12
Synthesis of 9-O-substituted derivatives of 9-hydroxy-5, 6-dimethyl-6H-pyrido[4,3-b]carbazole-1-carboxylic acid (2-(dimethylamino)ethyl)amide and their 10- and 11-methyl analogues with improved antitumor activity.
AID68798Compound was evaluated for the effective dose, as compared to controls against Escherichia coli TA98; Not tested1984Journal of medicinal chemistry, Sep, Volume: 27, Issue:9
Potential antitumor agents: synthesis and biological properties of aliphatic amino acid 9-hydroxyellipticinium derivatives.
AID137403Percent median survival time of mice injected with B16 melanoma, at a subcutaneous compound dose of 0.5 mg/kg1999Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12
Synthesis of 9-O-substituted derivatives of 9-hydroxy-5, 6-dimethyl-6H-pyrido[4,3-b]carbazole-1-carboxylic acid (2-(dimethylamino)ethyl)amide and their 10- and 11-methyl analogues with improved antitumor activity.
AID78564Compound was evaluated for inhibitory activity against H69 human lung cancer cell line1992Journal of medicinal chemistry, Dec-25, Volume: 35, Issue:26
N-methylcarbamate derivatives of ellipticine and olivacine with cytotoxic activity against four human lung cancer cell lines.
AID54618Apparent binding constant (Kapp) for calf thymus DNA was measured by competition with ethidium bromide1984Journal of medicinal chemistry, Sep, Volume: 27, Issue:9
Potential antitumor agents: synthesis and biological properties of aliphatic amino acid 9-hydroxyellipticinium derivatives.
AID78720Compound was evaluated for inhibitory activity against H 358 human lung cancer cell line1992Journal of medicinal chemistry, Dec-25, Volume: 35, Issue:26
N-methylcarbamate derivatives of ellipticine and olivacine with cytotoxic activity against four human lung cancer cell lines.
AID255987Inhibitory concentration against IL-3 independent Ba/F3 Kit cell line with SCF (kit-ligand)2005Journal of medicinal chemistry, Oct-06, Volume: 48, Issue:20
Molecular modeling of wild-type and D816V c-Kit inhibition based on ATP-competitive binding of ellipticine derivatives to tyrosine kinases.
AID255004Inhibitory concentration against c-Kit wild type expressed in recombinant baculovirus2005Journal of medicinal chemistry, Oct-06, Volume: 48, Issue:20
Molecular modeling of wild-type and D816V c-Kit inhibition based on ATP-competitive binding of ellipticine derivatives to tyrosine kinases.
AID255976Inhibitory concentration against IL-3 independent Ba/F3 Kit D816V cell line2005Journal of medicinal chemistry, Oct-06, Volume: 48, Issue:20
Molecular modeling of wild-type and D816V c-Kit inhibition based on ATP-competitive binding of ellipticine derivatives to tyrosine kinases.
AID39258Inhibition of murine B16 melanoma cell proliferation measured by the MTT assay1999Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12
Synthesis of 9-O-substituted derivatives of 9-hydroxy-5, 6-dimethyl-6H-pyrido[4,3-b]carbazole-1-carboxylic acid (2-(dimethylamino)ethyl)amide and their 10- and 11-methyl analogues with improved antitumor activity.
AID254810Inhibitory activity against Platelet-derived growth factor receptor alpha2005Journal of medicinal chemistry, Oct-06, Volume: 48, Issue:20
Molecular modeling of wild-type and D816V c-Kit inhibition based on ATP-competitive binding of ellipticine derivatives to tyrosine kinases.
AID97904Compound was tested for its cytotoxic activity against murine leukemia L1210 cells in mice after intraperitoneal treatment, expressed as LD0 (highest nonlethal dose).1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Bioactivation of the antitumor drugs 9-hydroxyellipticine and derivatives by a peroxidase-hydrogen peroxide system.
AID256551Inhibitory concentration against c-Kit D816V type expressed in recombinant baculovirus2005Journal of medicinal chemistry, Oct-06, Volume: 48, Issue:20
Molecular modeling of wild-type and D816V c-Kit inhibition based on ATP-competitive binding of ellipticine derivatives to tyrosine kinases.
AID137556Percent median survival time of mice injected with P388 leukemia, at a subcutaneous compound dose of 7.5 mg/kg1999Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12
Synthesis of 9-O-substituted derivatives of 9-hydroxy-5, 6-dimethyl-6H-pyrido[4,3-b]carbazole-1-carboxylic acid (2-(dimethylamino)ethyl)amide and their 10- and 11-methyl analogues with improved antitumor activity.
AID254753Inhibitory activity against Fibroblast growth factor receptor 32005Journal of medicinal chemistry, Oct-06, Volume: 48, Issue:20
Molecular modeling of wild-type and D816V c-Kit inhibition based on ATP-competitive binding of ellipticine derivatives to tyrosine kinases.
AID135227Long-term survivors among 6 mice infected with P388 leukemia, scored on day 60 at 20 mg/kg dose1999Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12
Synthesis of 9-O-substituted derivatives of 9-hydroxy-5, 6-dimethyl-6H-pyrido[4,3-b]carbazole-1-carboxylic acid (2-(dimethylamino)ethyl)amide and their 10- and 11-methyl analogues with improved antitumor activity.
AID1666491Binding affinity to 5' FAM/3' TAMRA (G4C2)8 G-quadruplex DNA (unknown origin) by FRET assay2020Bioorganic & medicinal chemistry letters, 02-15, Volume: 30, Issue:4
Emerging small-molecule therapeutic approaches for amyotrophic lateral sclerosis and frontotemporal dementia.
AID68796Compound was evaluated for the effective dose, as compared to controls against Escherichia coli BL 1011984Journal of medicinal chemistry, Sep, Volume: 27, Issue:9
Potential antitumor agents: synthesis and biological properties of aliphatic amino acid 9-hydroxyellipticinium derivatives.
AID78722Compound was evaluated for inhibitory activity against H 460 human lung cancer cell line1992Journal of medicinal chemistry, Dec-25, Volume: 35, Issue:26
N-methylcarbamate derivatives of ellipticine and olivacine with cytotoxic activity against four human lung cancer cell lines.
AID117502The effect on oxygen consumed in the presence of MPO-H2O2.1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Bioactivation of the antitumor drugs 9-hydroxyellipticine and derivatives by a peroxidase-hydrogen peroxide system.
AID96644Compound was tested for its antitumor activity against murine leukemia L1210 cells in vitro, expressed as ID501981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Bioactivation of the antitumor drugs 9-hydroxyellipticine and derivatives by a peroxidase-hydrogen peroxide system.
AID135238Long-term survivors among 6 mice infected with P388 leukemia, scored on day 60 at 7.5 mg/kg dose1999Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12
Synthesis of 9-O-substituted derivatives of 9-hydroxy-5, 6-dimethyl-6H-pyrido[4,3-b]carbazole-1-carboxylic acid (2-(dimethylamino)ethyl)amide and their 10- and 11-methyl analogues with improved antitumor activity.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (125)

TimeframeStudies, This Drug (%)All Drugs %
pre-199089 (71.20)18.7374
1990's33 (26.40)18.2507
2000's2 (1.60)29.6817
2010's0 (0.00)24.3611
2020's1 (0.80)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 16.67

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index16.67 (24.57)
Research Supply Index4.97 (2.92)
Research Growth Index4.01 (4.65)
Search Engine Demand Index15.26 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (16.67)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials8 (5.93%)5.53%
Reviews5 (3.70%)6.00%
Case Studies6 (4.44%)4.05%
Observational0 (0.00%)0.25%
Other116 (85.93%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]