Compounds > pg 545
Page last updated: 2024-11-13

pg 545

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Description

PG 545: an anti-angiogenesis agent with heparanase inhibitory activity; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID57412324
MeSH IDM0557348

Synonyms (9)

Synonym
pg-545
99N289ZQ8L ,
pixatimod sodium
1144492-69-2
pg 545
.beta.-d-glucopyranoside, (3.beta.,5.alpha.)-cholestan-3-yl o-2,3,4,6-tetra-o-sulfo-.alpha.-d-glucopyranosyl-(1->4)-o-2,3,6-tri-o-sulfo-.alpha.-d-glucopyranosyl-(1->4)-o-2,3,6-tri-o-sulfo-.alpha.-d-glucopyranosyl-(1->4)-, 2,3,6-tris(hydrogen sulfate), sod
((2r,3r,4s,5r,6r)-2-((2r,3r,4s,5r,6r)-6-((2r,3r,4s,5r,6r)-6-((2r,3r,4s,5r,6r)-6-(((3s,5s,8r,9s,10s,13r,14s,17r)-17-((1r)-1,5-dimethylhexyl)-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1h-cyclopenta(a)phenanthren-3-yl)oxy)-4,5-disu
beta-d-glucopyranoside, (3beta,5alpha)-cholestan-3-yl o-2,3,4,6-tetra-o-sulfo-alpha-d-glucopyranosyl-(1->4)-o-2,3,6-tri-o-sulfo-alpha-d-glucopyranosyl-(1->4)-o-2,3,6-tri-o-sulfo-alpha-d-glucopyranosyl-(1->4)-, 2,3,6-tris(hydrogen sulfate)
unii-99n289zq8l

Research Excerpts

Compound-Compound Interactions

ExcerptReferenceRelevance
" Collectively, our findings suggest that PG545 exerts anti-tumor activity by disrupting Wnt/β-catenin signaling and combination with gemcitabine should be considered as a novel therapeutic strategy for pancreatic cancer treatment."( The heparan sulfate mimetic PG545 interferes with Wnt/β-catenin signaling and significantly suppresses pancreatic tumorigenesis alone and in combination with gemcitabine.
Dredge, K; Hammond, E; Jung, DB; Jung, JH; Kim, B; Kim, EO; Kim, J; Kim, SH; Mukhopadhyay, D; Shridhar, V; Wang, E; Yun, M, 2015)		0.42
" Finally, the potential utility of pixatimod in combination with PD-1 inhibition was also investigated using the syngeneic 4T1."( Immunomodulatory activities of pixatimod: emerging nonclinical and clinical data, and its potential utility in combination with PD-1 inhibitors.
Bampton, D; Brennan, TV; Cullinane, C; Dredge, K; Hammond, E; Handley, P; Haynes, NM; Karoli, T; Lanksheer, F; Lin, L; Yang, Y, 2018)		0.48
"Pixatimod modulates innate immune cells but also enhances T cell infiltration in combination with anti-PD-1 therapy."( Immunomodulatory activities of pixatimod: emerging nonclinical and clinical data, and its potential utility in combination with PD-1 inhibitors.
Bampton, D; Brennan, TV; Cullinane, C; Dredge, K; Hammond, E; Handley, P; Haynes, NM; Karoli, T; Lanksheer, F; Lin, L; Yang, Y, 2018)		0.48

Dosage Studied

ExcerptRelevanceReference
" Pharmacokinetic (PK) data were also generated in tumour-bearing mice to gain an understanding of optimal dosing schedules and regimens."( PG545, a dual heparanase and angiogenesis inhibitor, induces potent anti-tumour and anti-metastatic efficacy in preclinical models.
Brandt, R; Bytheway, I; Dredge, K; Ferro, V; Gonda, TJ; Hammond, E; Handley, P; Smith, MT; Vincent, C, 2011)		0.37
" Preliminary pharmacokinetic analyses also revealed significant increases in half-life following iv dosing, ultimately supporting less frequent dosing regimens in preclinical tumor models compared with other HS mimetics."( Discovery of PG545: a highly potent and simultaneous inhibitor of angiogenesis, tumor growth, and metastasis.
Bytheway, I; Davis, K; Dredge, K; Ferro, V; Hammond, E; Handley, P; Harenberg, J; Johnstone, KD; Karoli, T; Li, CP; Liu, L; Rowley, J; Sarimaa, L; Wimmer, N, 2012)		0.38
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (3)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
HeparanaseHomo sapiens (human)Ki0.00610.00610.00700.0079AID672592
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Fibroblast growth factor 1Homo sapiens (human)Kd0.00800.00800.12400.2400AID672589
Fibroblast growth factor 2Homo sapiens (human)Kd0.39000.06100.22550.3900AID672590
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (112)

Processvia Protein(s)Taxonomy
positive regulation of cell population proliferationFibroblast growth factor 1Homo sapiens (human)
fibroblast growth factor receptor signaling pathwayFibroblast growth factor 1Homo sapiens (human)
angiogenesisFibroblast growth factor 1Homo sapiens (human)
organ inductionFibroblast growth factor 1Homo sapiens (human)
signal transductionFibroblast growth factor 1Homo sapiens (human)
positive regulation of cell population proliferationFibroblast growth factor 1Homo sapiens (human)
fibroblast growth factor receptor signaling pathwayFibroblast growth factor 1Homo sapiens (human)
anatomical structure morphogenesisFibroblast growth factor 1Homo sapiens (human)
positive regulation of endothelial cell migrationFibroblast growth factor 1Homo sapiens (human)
lung developmentFibroblast growth factor 1Homo sapiens (human)
positive regulation of cell migrationFibroblast growth factor 1Homo sapiens (human)
activation of protein kinase B activityFibroblast growth factor 1Homo sapiens (human)
cellular response to heatFibroblast growth factor 1Homo sapiens (human)
wound healingFibroblast growth factor 1Homo sapiens (human)
positive regulation of MAP kinase activityFibroblast growth factor 1Homo sapiens (human)
positive regulation of cholesterol biosynthetic processFibroblast growth factor 1Homo sapiens (human)
positive regulation of angiogenesisFibroblast growth factor 1Homo sapiens (human)
positive regulation of transcription by RNA polymerase IIFibroblast growth factor 1Homo sapiens (human)
epithelial cell proliferationFibroblast growth factor 1Homo sapiens (human)
positive regulation of cell divisionFibroblast growth factor 1Homo sapiens (human)
branch elongation involved in ureteric bud branchingFibroblast growth factor 1Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeFibroblast growth factor 1Homo sapiens (human)
mesonephric epithelium developmentFibroblast growth factor 1Homo sapiens (human)
regulation of endothelial tube morphogenesisFibroblast growth factor 1Homo sapiens (human)
positive regulation of intracellular signal transductionFibroblast growth factor 1Homo sapiens (human)
positive regulation of sprouting angiogenesisFibroblast growth factor 1Homo sapiens (human)
positive regulation of hepatocyte proliferationFibroblast growth factor 1Homo sapiens (human)
regulation of endothelial cell chemotaxis to fibroblast growth factorFibroblast growth factor 1Homo sapiens (human)
cell differentiationFibroblast growth factor 1Homo sapiens (human)
positive regulation of gene expressionFibroblast growth factor 1Homo sapiens (human)
animal organ morphogenesisFibroblast growth factor 1Homo sapiens (human)
regulation of cell migrationFibroblast growth factor 1Homo sapiens (human)
negative regulation of gene expressionFibroblast growth factor 2Homo sapiens (human)
negative regulation of fibroblast growth factor receptor signaling pathwayFibroblast growth factor 2Homo sapiens (human)
regulation of cell migration involved in sprouting angiogenesisFibroblast growth factor 2Homo sapiens (human)
regulation of blood vessel endothelial cell proliferation involved in sprouting angiogenesisFibroblast growth factor 2Homo sapiens (human)
regulation of endothelial cell chemotaxis to fibroblast growth factorFibroblast growth factor 2Homo sapiens (human)
positive regulation of cell population proliferationFibroblast growth factor 2Homo sapiens (human)
fibroblast growth factor receptor signaling pathwayFibroblast growth factor 2Homo sapiens (human)
positive regulation of cell fate specificationFibroblast growth factor 2Homo sapiens (human)
osteoblast differentiationFibroblast growth factor 2Homo sapiens (human)
branching involved in ureteric bud morphogenesisFibroblast growth factor 2Homo sapiens (human)
organ inductionFibroblast growth factor 2Homo sapiens (human)
endothelial cell proliferationFibroblast growth factor 2Homo sapiens (human)
positive regulation of endothelial cell proliferationFibroblast growth factor 2Homo sapiens (human)
cell migration involved in sprouting angiogenesisFibroblast growth factor 2Homo sapiens (human)
positive regulation of neuroblast proliferationFibroblast growth factor 2Homo sapiens (human)
transcription by RNA polymerase IIFibroblast growth factor 2Homo sapiens (human)
chemotaxisFibroblast growth factor 2Homo sapiens (human)
signal transductionFibroblast growth factor 2Homo sapiens (human)
Ras protein signal transductionFibroblast growth factor 2Homo sapiens (human)
nervous system developmentFibroblast growth factor 2Homo sapiens (human)
neuroblast proliferationFibroblast growth factor 2Homo sapiens (human)
fibroblast growth factor receptor signaling pathwayFibroblast growth factor 2Homo sapiens (human)
embryo development ending in birth or egg hatchingFibroblast growth factor 2Homo sapiens (human)
glial cell differentiationFibroblast growth factor 2Homo sapiens (human)
positive regulation of endothelial cell migrationFibroblast growth factor 2Homo sapiens (human)
negative regulation of fibroblast migrationFibroblast growth factor 2Homo sapiens (human)
growth factor dependent regulation of skeletal muscle satellite cell proliferationFibroblast growth factor 2Homo sapiens (human)
substantia nigra developmentFibroblast growth factor 2Homo sapiens (human)
cerebellar granule cell precursor proliferationFibroblast growth factor 2Homo sapiens (human)
positive regulation of cerebellar granule cell precursor proliferationFibroblast growth factor 2Homo sapiens (human)
hyaluronan catabolic processFibroblast growth factor 2Homo sapiens (human)
lung developmentFibroblast growth factor 2Homo sapiens (human)
paracrine signalingFibroblast growth factor 2Homo sapiens (human)
wound healingFibroblast growth factor 2Homo sapiens (human)
inner ear auditory receptor cell differentiationFibroblast growth factor 2Homo sapiens (human)
positive regulation of MAP kinase activityFibroblast growth factor 2Homo sapiens (human)
positive regulation of MAPK cascadeFibroblast growth factor 2Homo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transductionFibroblast growth factor 2Homo sapiens (human)
positive regulation of blood vessel endothelial cell migrationFibroblast growth factor 2Homo sapiens (human)
negative regulation of blood vessel endothelial cell migrationFibroblast growth factor 2Homo sapiens (human)
positive regulation of inner ear auditory receptor cell differentiationFibroblast growth factor 2Homo sapiens (human)
positive regulation of osteoblast differentiationFibroblast growth factor 2Homo sapiens (human)
regulation of angiogenesisFibroblast growth factor 2Homo sapiens (human)
positive regulation of angiogenesisFibroblast growth factor 2Homo sapiens (human)
positive regulation of DNA-templated transcriptionFibroblast growth factor 2Homo sapiens (human)
positive regulation of transcription by RNA polymerase IIFibroblast growth factor 2Homo sapiens (human)
regulation of retinal cell programmed cell deathFibroblast growth factor 2Homo sapiens (human)
embryonic morphogenesisFibroblast growth factor 2Homo sapiens (human)
response to axon injuryFibroblast growth factor 2Homo sapiens (human)
stem cell developmentFibroblast growth factor 2Homo sapiens (human)
positive chemotaxisFibroblast growth factor 2Homo sapiens (human)
release of sequestered calcium ion into cytosolFibroblast growth factor 2Homo sapiens (human)
regulation of cell cycleFibroblast growth factor 2Homo sapiens (human)
positive regulation of cell divisionFibroblast growth factor 2Homo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionFibroblast growth factor 2Homo sapiens (human)
positive regulation of cardiac muscle cell proliferationFibroblast growth factor 2Homo sapiens (human)
canonical Wnt signaling pathwayFibroblast growth factor 2Homo sapiens (human)
corticotropin hormone secreting cell differentiationFibroblast growth factor 2Homo sapiens (human)
thyroid-stimulating hormone-secreting cell differentiationFibroblast growth factor 2Homo sapiens (human)
chondroblast differentiationFibroblast growth factor 2Homo sapiens (human)
mammary gland epithelial cell differentiationFibroblast growth factor 2Homo sapiens (human)
angiogenesis involved in coronary vascular morphogenesisFibroblast growth factor 2Homo sapiens (human)
negative regulation of wound healingFibroblast growth factor 2Homo sapiens (human)
ERK1 and ERK2 cascadeFibroblast growth factor 2Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeFibroblast growth factor 2Homo sapiens (human)
cellular response to mechanical stimulusFibroblast growth factor 2Homo sapiens (human)
stem cell proliferationFibroblast growth factor 2Homo sapiens (human)
positive regulation of cell migration involved in sprouting angiogenesisFibroblast growth factor 2Homo sapiens (human)
positive regulation of canonical Wnt signaling pathwayFibroblast growth factor 2Homo sapiens (human)
positive regulation of lens fiber cell differentiationFibroblast growth factor 2Homo sapiens (human)
positive regulation of miRNA transcriptionFibroblast growth factor 2Homo sapiens (human)
positive regulation of neuroepithelial cell differentiationFibroblast growth factor 2Homo sapiens (human)
positive regulation of sprouting angiogenesisFibroblast growth factor 2Homo sapiens (human)
positive regulation of vascular associated smooth muscle cell proliferationFibroblast growth factor 2Homo sapiens (human)
lymphatic endothelial cell migrationFibroblast growth factor 2Homo sapiens (human)
positive regulation of epithelial tube formationFibroblast growth factor 2Homo sapiens (human)
positive regulation of vascular endothelial cell proliferationFibroblast growth factor 2Homo sapiens (human)
regulation of endothelial cell chemotaxis to fibroblast growth factorFibroblast growth factor 2Homo sapiens (human)
positive regulation of endothelial cell chemotaxis to fibroblast growth factorFibroblast growth factor 2Homo sapiens (human)
positive regulation of DNA biosynthetic processFibroblast growth factor 2Homo sapiens (human)
negative regulation of stem cell proliferationFibroblast growth factor 2Homo sapiens (human)
positive regulation of stem cell proliferationFibroblast growth factor 2Homo sapiens (human)
positive regulation of stem cell differentiationFibroblast growth factor 2Homo sapiens (human)
positive regulation of endothelial cell chemotaxisFibroblast growth factor 2Homo sapiens (human)
regulation of cell migrationFibroblast growth factor 2Homo sapiens (human)
positive regulation of gene expressionFibroblast growth factor 2Homo sapiens (human)
animal organ morphogenesisFibroblast growth factor 2Homo sapiens (human)
cell differentiationFibroblast growth factor 2Homo sapiens (human)
positive regulation of cell population proliferationFibroblast growth factor 2Homo sapiens (human)
proteoglycan metabolic processHeparanaseHomo sapiens (human)
cell-matrix adhesionHeparanaseHomo sapiens (human)
response to organic substanceHeparanaseHomo sapiens (human)
positive regulation of vascular endothelial growth factor productionHeparanaseHomo sapiens (human)
positive regulation of blood coagulationHeparanaseHomo sapiens (human)
heparan sulfate proteoglycan catabolic processHeparanaseHomo sapiens (human)
heparin metabolic processHeparanaseHomo sapiens (human)
positive regulation of osteoblast proliferationHeparanaseHomo sapiens (human)
regulation of hair follicle developmentHeparanaseHomo sapiens (human)
positive regulation of hair follicle developmentHeparanaseHomo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionHeparanaseHomo sapiens (human)
establishment of endothelial barrierHeparanaseHomo sapiens (human)
vascular wound healingHeparanaseHomo sapiens (human)
protein transmembrane transportHeparanaseHomo sapiens (human)
angiogenesis involved in wound healingHeparanaseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (16)

Processvia Protein(s)Taxonomy
fibroblast growth factor receptor bindingFibroblast growth factor 1Homo sapiens (human)
integrin bindingFibroblast growth factor 1Homo sapiens (human)
protein bindingFibroblast growth factor 1Homo sapiens (human)
growth factor activityFibroblast growth factor 1Homo sapiens (human)
heparin bindingFibroblast growth factor 1Homo sapiens (human)
Hsp70 protein bindingFibroblast growth factor 1Homo sapiens (human)
S100 protein bindingFibroblast growth factor 1Homo sapiens (human)
fibroblast growth factor receptor bindingFibroblast growth factor 2Homo sapiens (human)
cytokine activityFibroblast growth factor 2Homo sapiens (human)
integrin bindingFibroblast growth factor 2Homo sapiens (human)
protein bindingFibroblast growth factor 2Homo sapiens (human)
growth factor activityFibroblast growth factor 2Homo sapiens (human)
heparin bindingFibroblast growth factor 2Homo sapiens (human)
chemokine bindingFibroblast growth factor 2Homo sapiens (human)
nuclear receptor coactivator activityFibroblast growth factor 2Homo sapiens (human)
chemoattractant activityFibroblast growth factor 2Homo sapiens (human)
identical protein bindingFibroblast growth factor 2Homo sapiens (human)
receptor-receptor interactionFibroblast growth factor 2Homo sapiens (human)
beta-glucuronidase activityHeparanaseHomo sapiens (human)
protein bindingHeparanaseHomo sapiens (human)
heparanase activityHeparanaseHomo sapiens (human)
syndecan bindingHeparanaseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (14)

Processvia Protein(s)Taxonomy
extracellular regionFibroblast growth factor 1Homo sapiens (human)
extracellular spaceFibroblast growth factor 1Homo sapiens (human)
nucleoplasmFibroblast growth factor 1Homo sapiens (human)
cytosolFibroblast growth factor 1Homo sapiens (human)
cell cortexFibroblast growth factor 1Homo sapiens (human)
extracellular matrixFibroblast growth factor 1Homo sapiens (human)
cytoplasmFibroblast growth factor 1Homo sapiens (human)
extracellular spaceFibroblast growth factor 1Homo sapiens (human)
nucleusFibroblast growth factor 1Homo sapiens (human)
extracellular regionFibroblast growth factor 2Homo sapiens (human)
extracellular spaceFibroblast growth factor 2Homo sapiens (human)
extracellular spaceFibroblast growth factor 2Homo sapiens (human)
cytoplasmFibroblast growth factor 2Homo sapiens (human)
nucleusFibroblast growth factor 2Homo sapiens (human)
extracellular regionHeparanaseHomo sapiens (human)
nucleusHeparanaseHomo sapiens (human)
nucleoplasmHeparanaseHomo sapiens (human)
lysosomeHeparanaseHomo sapiens (human)
lysosomal membraneHeparanaseHomo sapiens (human)
specific granule lumenHeparanaseHomo sapiens (human)
lysosomal lumenHeparanaseHomo sapiens (human)
intracellular membrane-bounded organelleHeparanaseHomo sapiens (human)
membrane raftHeparanaseHomo sapiens (human)
extracellular spaceHeparanaseHomo sapiens (human)
extracellular matrixHeparanaseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (25)

Assay IDTitleYearJournalArticle
AID672665Antiangiogenic activity in HUVEC cells assessed as inhibition of tube formation after 18 hrs by matrigel assay2012Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
Discovery of PG545: a highly potent and simultaneous inhibitor of angiogenesis, tumor growth, and metastasis.
AID672671Anticoagulant activity in pooled human plasma assessed as prolongation of the recalcification time at 0.1 mg/ml by Heptest assay2012Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
Discovery of PG545: a highly potent and simultaneous inhibitor of angiogenesis, tumor growth, and metastasis.
AID672593Antiangiogenic activity in FGF1-stimulated HUVEC cells after 72 hrs by CellTiter assay2012Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
Discovery of PG545: a highly potent and simultaneous inhibitor of angiogenesis, tumor growth, and metastasis.
AID672674Selectivity index, ratio of LC50 for Sprague-Dawley aorta to antiangiogenic IC50 for Sprague-Dawley aorta2012Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
Discovery of PG545: a highly potent and simultaneous inhibitor of angiogenesis, tumor growth, and metastasis.
AID672592Inhibition of human recombinant heparanase after 2 to 24 hrs by WST1 dye based fondaparinux assay2012Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
Discovery of PG545: a highly potent and simultaneous inhibitor of angiogenesis, tumor growth, and metastasis.
AID672595Antiangiogenic activity in VEGF-stimulated HUVEC cells after 72 hrs by CellTiter assay2012Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
Discovery of PG545: a highly potent and simultaneous inhibitor of angiogenesis, tumor growth, and metastasis.
AID672662Antiangiogenic activity in VEGF-stimulated HMVEC cells after 72 hrs by CellTiter assay2012Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
Discovery of PG545: a highly potent and simultaneous inhibitor of angiogenesis, tumor growth, and metastasis.
AID672667Cytotoxicity against Sprague-Dawley rat aorta2012Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
Discovery of PG545: a highly potent and simultaneous inhibitor of angiogenesis, tumor growth, and metastasis.
AID672668Cytotoxicity against Sprague-Dawley rat aorta assessed as VEGF-induced microvessel formation measured 6 days post compound treatment grown on fresh medium containing VEGF2012Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
Discovery of PG545: a highly potent and simultaneous inhibitor of angiogenesis, tumor growth, and metastasis.
AID672657Potency index, ratio of IC50 for PI-88 to compound IC50 for FGF1-stimulated HUVEC cells after 72 hrs by CellTiter assay2012Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
Discovery of PG545: a highly potent and simultaneous inhibitor of angiogenesis, tumor growth, and metastasis.
AID672666Antiangiogenic activity in Sprague-Dawley rat aorta assessed as inhibition of tube formation measured up to 8 days by matrigel assay2012Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
Discovery of PG545: a highly potent and simultaneous inhibitor of angiogenesis, tumor growth, and metastasis.
AID672672Cytotoxicity against HUVEC2012Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
Discovery of PG545: a highly potent and simultaneous inhibitor of angiogenesis, tumor growth, and metastasis.
AID672670Anticoagulant activity in pooled human plasma assessed as activated partial thromboplastin time at 0.1 mg/ml2012Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
Discovery of PG545: a highly potent and simultaneous inhibitor of angiogenesis, tumor growth, and metastasis.
AID672589Binding affinity to FGF-1 by surface plasmon resonance assay2012Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
Discovery of PG545: a highly potent and simultaneous inhibitor of angiogenesis, tumor growth, and metastasis.
AID672661Antiangiogenic activity in FGF2-stimulated HMVEC cells after 72 hrs by CellTiter assay2012Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
Discovery of PG545: a highly potent and simultaneous inhibitor of angiogenesis, tumor growth, and metastasis.
AID672590Binding affinity to FGF-2 by surface plasmon resonance assay2012Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
Discovery of PG545: a highly potent and simultaneous inhibitor of angiogenesis, tumor growth, and metastasis.
AID672669Elimination half life in Sprague-Dawley rat at 10 mg/kg, sc using [3H]-labeled compound administered as three bolus doses at 96 hrs interval2012Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
Discovery of PG545: a highly potent and simultaneous inhibitor of angiogenesis, tumor growth, and metastasis.
AID672663Antiangiogenic activity in HUVEC cells assessed as inhibition of tube formation at 10 uM after 18 hrs by matrigel assay2012Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
Discovery of PG545: a highly potent and simultaneous inhibitor of angiogenesis, tumor growth, and metastasis.
AID672658Potency index, ratio of IC50 for PI-88 to compound IC50 for FGF2-stimulated HUVEC cells after 72 hrs by CellTiter assay2012Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
Discovery of PG545: a highly potent and simultaneous inhibitor of angiogenesis, tumor growth, and metastasis.
AID672659Potency index, ratio of IC50 for PI-88 to compound IC50 for VEGF-stimulated HUVEC cells after 72 hrs by CellTiter assay2012Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
Discovery of PG545: a highly potent and simultaneous inhibitor of angiogenesis, tumor growth, and metastasis.
AID672660Antiangiogenic activity in FGF1-stimulated HMVEC cells after 72 hrs by CellTiter assay2012Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
Discovery of PG545: a highly potent and simultaneous inhibitor of angiogenesis, tumor growth, and metastasis.
AID672594Antiangiogenic activity in FGF2-stimulated HUVEC cells after 72 hrs by CellTiter assay2012Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
Discovery of PG545: a highly potent and simultaneous inhibitor of angiogenesis, tumor growth, and metastasis.
AID672591Binding affinity to VEGFR by surface plasmon resonance assay2012Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
Discovery of PG545: a highly potent and simultaneous inhibitor of angiogenesis, tumor growth, and metastasis.
AID672673Selectivity index, ratio of LC50 for HUVEC to antiangiogenic IC50 for HUVEC2012Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
Discovery of PG545: a highly potent and simultaneous inhibitor of angiogenesis, tumor growth, and metastasis.
AID672664Antiangiogenic activity in Sprague-Dawley rat aorta assessed as inhibition of tube formation dosed daily at 10 uM measured up to 8 days by matrigel assay2012Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
Discovery of PG545: a highly potent and simultaneous inhibitor of angiogenesis, tumor growth, and metastasis.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (26)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's21 (80.77)24.3611
2020's5 (19.23)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 53.51

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 very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index53.51 (24.57)
Research Supply Index3.37 (2.92)
Research Growth Index4.52 (4.65)
Search Engine Demand Index166.42 (26.88)
Search Engine Supply Index3.99 (0.95)

This Compound (53.51)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials2 (7.69%)5.53%
Reviews2 (7.69%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other22 (84.62%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
niacinamide
nicotinamide : A pyridinecarboxamide that is pyridine in which the hydrogen at position 3 is replaced by a carboxamide group.		2.0710pyridine alkaloid;
pyridinecarboxamide;
vitamin B3		anti-inflammatory agent;
antioxidant;
cofactor;
EC 2.4.2.30 (NAD(+) ADP-ribosyltransferase) inhibitor;
EC 3.5.1.98 (histone deacetylase) inhibitor;
Escherichia coli metabolite;
geroprotector;
human urinary metabolite;
metabolite;
mouse metabolite;
neuroprotective agent;
Saccharomyces cerevisiae metabolite;
Sir2 inhibitor
deoxycytidine
[no description available]		2.1110pyrimidine 2'-deoxyribonucleosideEscherichia coli metabolite;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
paclitaxel
Taxus: Genus of coniferous yew trees or shrubs, several species of which have medicinal uses. Notable is the Pacific yew, Taxus brevifolia, which is used to make the anti-neoplastic drug taxol (PACLITAXEL).		3.511taxane diterpenoid;
tetracyclic diterpenoid		antineoplastic agent;
human metabolite;
metabolite;
microtubule-stabilising agent
gemcitabine
gemcitabine : A 2'-deoxycytidine having geminal fluoro substituents in the 2'-position. An inhibitor of ribonucleotide reductase, gemcitabine is used in the treatment of various carcinomas, particularly non-small cell lung cancer, pancreatic cancer, bladder cancer and breast cancer.		2.1110organofluorine compound;
pyrimidine 2'-deoxyribonucleoside		antimetabolite;
antineoplastic agent;
antiviral drug;
DNA synthesis inhibitor;
EC 1.17.4.1 (ribonucleoside-diphosphate reductase) inhibitor;
environmental contaminant;
immunosuppressive agent;
photosensitizing agent;
prodrug;
radiosensitizing agent;
xenobiotic
sorafenib
[no description available]		2.0710(trifluoromethyl)benzenes;
aromatic ether;
monochlorobenzenes;
phenylureas;
pyridinecarboxamide		angiogenesis inhibitor;
anticoronaviral agent;
antineoplastic agent;
EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor;
ferroptosis inducer;
tyrosine kinase inhibitor
beta-escin
[no description available]		9.22262
glycolipids
[no description available]		2.2510
phosphomannopentaose sulfate
phosphomannopentaose sulfate: structure in first source		2.520
heparitin sulfate
Heparitin Sulfate: A heteropolysaccharide that is similar in structure to HEPARIN. It accumulates in individuals with MUCOPOLYSACCHARIDOSIS.		4.3550
ConditionIndicatedRelationship StrengthStudiesTrials
Angiogenesis, Pathologic
[description not available]		02.7830
Cancer of Ovary
[description not available]		0421
Ovarian Neoplasms
Tumors or cancer of the OVARY. These neoplasms can be benign or malignant. They are classified according to the tissue of origin, such as the surface EPITHELIUM, the stromal endocrine cells, and the totipotent GERM CELLS.		0421
Benign Neoplasms
[description not available]		06.5752
Neoplasms
New abnormal growth of tissue. Malignant neoplasms show a greater degree of anaplasia and have the properties of invasion and metastasis, compared to benign neoplasms.		06.5752
Cancer of Endometrium
[description not available]		02.2510
Endometrial Neoplasms
Tumors or cancer of ENDOMETRIUM, the mucous lining of the UTERUS. These neoplasms can be benign or malignant. Their classification and grading are based on the various cell types and the percent of undifferentiated cells.		02.2510
Body Weight
The mass or quantity of heaviness of an individual. It is expressed by units of pounds or kilograms.		02.2510
Alloxan Diabetes
[description not available]		02.2510
Neuroretinitis
[description not available]		02.2510
Diabetic Retinopathy
Disease of the RETINA as a complication of DIABETES MELLITUS. It is characterized by the progressive microvascular complications, such as ANEURYSM, interretinal EDEMA, and intraocular PATHOLOGIC NEOVASCULARIZATION.		02.2510
Retinitis
Inflammation of the RETINA. It is rarely limited to the retina, but is commonly associated with diseases of the choroid (CHORIORETINITIS) and of the OPTIC DISK (neuroretinitis).		02.2510
Acute Kidney Failure
[description not available]		02.1510
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		03.3960
Injury, Ischemia-Reperfusion
[description not available]		02.1510
Reperfusion Injury
Adverse functional, metabolic, or structural changes in tissues that result from the restoration of blood flow to the tissue (REPERFUSION) following ISCHEMIA.		02.1510
Acute Kidney Injury
Abrupt reduction in kidney function. Acute kidney injury encompasses the entire spectrum of the syndrome including acute kidney failure; ACUTE KIDNEY TUBULAR NECROSIS; and other less severe conditions.		02.1510
Benign Neoplasms, Brain
[description not available]		02.1510
Invasiveness, Neoplasm
[description not available]		02.1510
Brain Neoplasms
Neoplasms of the intracranial components of the central nervous system, including the cerebral hemispheres, basal ganglia, hypothalamus, thalamus, brain stem, and cerebellum. Brain neoplasms are subdivided into primary (originating from brain tissue) and secondary (i.e., metastatic) forms. Primary neoplasms are subdivided into benign and malignant forms. In general, brain tumors may also be classified by age of onset, histologic type, or presenting location in the brain.		02.1510
Atherogenesis
[description not available]		02.5720
Atherosclerosis
A thickening and loss of elasticity of the walls of ARTERIES that occurs with formation of ATHEROSCLEROTIC PLAQUES within the ARTERIAL INTIMA.		02.5720
Disease Exacerbation
[description not available]		04.2131
Adenocarcinoma, Basal Cell
[description not available]		03.0910
Cancer of Pancreas
[description not available]		05.3460
Adenocarcinoma
A malignant epithelial tumor with a glandular organization.		03.0910
Pancreatic Neoplasms
Tumors or cancer of the PANCREAS. Depending on the types of ISLET CELLS present in the tumors, various hormones can be secreted: GLUCAGON from PANCREATIC ALPHA CELLS; INSULIN from PANCREATIC BETA CELLS; and SOMATOSTATIN from the SOMATOSTATIN-SECRETING CELLS. Most are malignant except the insulin-producing tumors (INSULINOMA).		05.3460
Atheroma
[description not available]		02.1710
Liver Steatosis
[description not available]		02.1710
Aortic Diseases
Pathological processes involving any part of the AORTA.		02.1710
Fatty Liver
Lipid infiltration of the hepatic parenchymal cells resulting in a yellow-colored liver. The abnormal lipid accumulation is usually in the form of TRIGLYCERIDES, either as a single large droplet or multiple small droplets. Fatty liver is caused by an imbalance in the metabolism of FATTY ACIDS.		02.1710
Carcinogenesis
The origin, production or development of cancer through genotypic and phenotypic changes which upset the normal balance between cell proliferation and cell death. Carcinogenesis generally requires a constellation of steps, which may occur quickly or over a period of many years.		02.5520
Germinoblastoma
[description not available]		02.8430
Lymphoma
A general term for various neoplastic diseases of the lymphoid tissue.		02.8430
Break-Bone Fever
[description not available]		02.2110
Viremia
The presence of viruses in the blood.		02.2110
Dengue
An acute febrile disease transmitted by the bite of AEDES mosquitoes infected with DENGUE VIRUS. It is self-limiting and characterized by fever, myalgia, headache, and rash. SEVERE DENGUE is a more virulent form of dengue.		02.2110
Alpha Virus Infections
[description not available]		02.2110
Metastase
[description not available]		02.7830
Carcinoma, Ductal, Pancreatic
[description not available]		02.520
Neoplasm Metastasis
The transfer of a neoplasm from one organ or part of the body to another remote from the primary site.		02.7830
Carcinoma, Pancreatic Ductal
Carcinoma that arises from the PANCREATIC DUCTS. It accounts for the majority of cancers derived from the PANCREAS.		02.520
Genital Herpes
[description not available]		02.1310
Herpes Genitalis
Infection of the genitals (GENITALIA) with HERPES SIMPLEX VIRUS in either the males or the females.		02.1310
Cell Transformation, Neoplastic
Cell changes manifested by escape from control mechanisms, increased growth potential, alterations in the cell surface, karyotypic abnormalities, morphological and biochemical deviations from the norm, and other attributes conferring the ability to invade, metastasize, and kill.		02.1510
Cancer of Colon
[description not available]		02.1510
Colonic Neoplasms
Tumors or cancer of the COLON.		02.1510
Colonic Polyps
Discrete tissue masses that protrude into the lumen of the COLON. These POLYPS are connected to the wall of the colon either by a stalk, pedunculus, or by a broad base.		02.1510
Cancer of Lung
[description not available]		02.0710
Experimental Mammary Neoplasms
[description not available]		02.0710
Lung Neoplasms
Tumors or cancer of the LUNG.		02.0710