Page last updated: 2024-11-13

tas-115

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Description

4-(2-fluoro-4-((((2-phenylacetyl)amino)thioxomethyl)amino)phenoxy)-7-methoxy-N-methyl-6-quinolinecarboxamide: inhibits both VEGFR and MET kinase; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID44247727
CHEMBL ID3764045
SCHEMBL ID1132590
MeSH IDM000596327

Synonyms (36)

Synonym
4-(2-fluoro-4-(3-(2-phenylacetyl)thioureido)phenoxy)-7-methoxy-n-methylquinoline-6-carboxamide
S6764
ORRNXRYWGDUDOG-UHFFFAOYSA-N
SCHEMBL1132590
tas-115
pamufetinib
CHEMBL3764045 ,
bdbm50146163
HY-12423
CS-6820
4-[2-fluoro-4-[[[(2-phenylacetyl)amino]thioxomethyl]amino]-phenoxy]-7-methoxy-n-methyl-6-quinolinecarboxamide
tas 115 [who-dd]
tas 115
unii-h2ol3q4xrd
tas-115 free base
1190836-34-0 (free base)
ZB1546
1190836-34-0
pamufetinib [who-dd]
6-quinolinecarboxamide, 4-(2-fluoro-4-((((2-phenylacetyl)amino)thioxomethyl)amino)phenoxy)-7-methoxy-n-methyl-
H2OL3Q4XRD ,
pamufetinib [inn]
4-(2-fluoro-4-((((2-phenylacetyl)amino)thioxomethyl)amino)phenoxy)-7-methoxy-n-methyl-6-quinolinecarboxamide
EX-A2850
gtpl10460
tas115
4-[2-fluoro-4-[(2-phenylacetyl)carbamothioylamino]phenoxy]-7-methoxy-n-methylquinoline-6-carboxamide
SB16885
tas 115, tas115; pamufetinib
BCP34014
nsc-785306
nsc785306
A935727
B0084-475134
AC-35739
AKOS040740129

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" The most common adverse drug reactions (ADRs) were neutrophil count decreased (75%), aspartate aminotransferase increased (50%), and platelet count decreased (50%); 85% of patients had grade ≥ 3 ADRs."( Efficacy and safety of TAS-115, a novel oral multi-kinase inhibitor, in osteosarcoma: an expansion cohort of a phase I study.
Doi, T; Imura, Y; Iwata, S; Kawai, A; Kitano, S; Kobayashi, E; Naito, Y; Naka, N; Nakatani, F; Outani, H; Shimomura, A; Takahashi, S; Tamiya, H; Yamamoto, N; Yonemori, K, 2021
)
0.93

Dosage Studied

ExcerptRelevanceReference
" The fact that concomitant dosing of sunitinib (VEGFRs/FMS inhibition) with crizotinib (MET inhibition) exerted comparable inhibitory efficacy for bone destruction to TAS-115 also supports this notion."( High Potency VEGFRs/MET/FMS Triple Blockade by TAS-115 Concomitantly Suppresses Tumor Progression and Bone Destruction in Tumor-Induced Bone Disease Model with Lung Carcinoma Cells.
Fujioka, Y; Fujita, H; Gomori, A; Harada, N; Haruma, T; Hashimoto, A; Inada, M; Ito, K; Kataoka, Y; Matsuo, K; Oda, N; Sakuragi, M; Suzuki, T; Tanaka, K; Yamamoto-Yokoi, H; Yonekura, K, 2016
)
0.89
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (2)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Hepatocyte growth factor receptorHomo sapiens (human)IC50 (µMol)0.03200.00040.372210.0000AID1276909
Vascular endothelial growth factor receptor 2Homo sapiens (human)IC50 (µMol)0.03000.00000.48308.8000AID1276910
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (84)

Processvia Protein(s)Taxonomy
endothelial cell morphogenesisHepatocyte growth factor receptorHomo sapiens (human)
signal transductionHepatocyte growth factor receptorHomo sapiens (human)
cell surface receptor signaling pathwayHepatocyte growth factor receptorHomo sapiens (human)
negative regulation of autophagyHepatocyte growth factor receptorHomo sapiens (human)
positive regulation of microtubule polymerizationHepatocyte growth factor receptorHomo sapiens (human)
negative regulation of Rho protein signal transductionHepatocyte growth factor receptorHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIHepatocyte growth factor receptorHomo sapiens (human)
hepatocyte growth factor receptor signaling pathwayHepatocyte growth factor receptorHomo sapiens (human)
branching morphogenesis of an epithelial tubeHepatocyte growth factor receptorHomo sapiens (human)
positive chemotaxisHepatocyte growth factor receptorHomo sapiens (human)
negative regulation of stress fiber assemblyHepatocyte growth factor receptorHomo sapiens (human)
excitatory postsynaptic potentialHepatocyte growth factor receptorHomo sapiens (human)
establishment of skin barrierHepatocyte growth factor receptorHomo sapiens (human)
negative regulation of thrombin-activated receptor signaling pathwayHepatocyte growth factor receptorHomo sapiens (human)
semaphorin-plexin signaling pathwayHepatocyte growth factor receptorHomo sapiens (human)
negative regulation of hydrogen peroxide-mediated programmed cell deathHepatocyte growth factor receptorHomo sapiens (human)
negative regulation of guanyl-nucleotide exchange factor activityHepatocyte growth factor receptorHomo sapiens (human)
positive regulation of endothelial cell chemotaxisHepatocyte growth factor receptorHomo sapiens (human)
liver developmentHepatocyte growth factor receptorHomo sapiens (human)
cell surface receptor protein tyrosine kinase signaling pathwayHepatocyte growth factor receptorHomo sapiens (human)
phagocytosisHepatocyte growth factor receptorHomo sapiens (human)
multicellular organism developmentHepatocyte growth factor receptorHomo sapiens (human)
neuron differentiationHepatocyte growth factor receptorHomo sapiens (human)
positive regulation of kinase activityHepatocyte growth factor receptorHomo sapiens (human)
cell migrationHepatocyte growth factor receptorHomo sapiens (human)
pancreas developmentHepatocyte growth factor receptorHomo sapiens (human)
nervous system developmentHepatocyte growth factor receptorHomo sapiens (human)
branching involved in blood vessel morphogenesisVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of macroautophagyVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of mitochondrial depolarizationVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of mitochondrial fissionVascular endothelial growth factor receptor 2Homo sapiens (human)
angiogenesisVascular endothelial growth factor receptor 2Homo sapiens (human)
ovarian follicle developmentVascular endothelial growth factor receptor 2Homo sapiens (human)
vasculogenesisVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of protein phosphorylationVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of endothelial cell proliferationVascular endothelial growth factor receptor 2Homo sapiens (human)
lymph vessel developmentVascular endothelial growth factor receptor 2Homo sapiens (human)
cell migration involved in sprouting angiogenesisVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of mesenchymal cell proliferationVascular endothelial growth factor receptor 2Homo sapiens (human)
epithelial cell maturationVascular endothelial growth factor receptor 2Homo sapiens (human)
endocardium developmentVascular endothelial growth factor receptor 2Homo sapiens (human)
endothelium developmentVascular endothelial growth factor receptor 2Homo sapiens (human)
cell surface receptor protein tyrosine kinase signaling pathwayVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of cell population proliferationVascular endothelial growth factor receptor 2Homo sapiens (human)
regulation of cell shapeVascular endothelial growth factor receptor 2Homo sapiens (human)
mesenchymal cell proliferationVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of endothelial cell migrationVascular endothelial growth factor receptor 2Homo sapiens (human)
negative regulation of gene expressionVascular endothelial growth factor receptor 2Homo sapiens (human)
peptidyl-tyrosine phosphorylationVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of cell migrationVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of BMP signaling pathwayVascular endothelial growth factor receptor 2Homo sapiens (human)
embryonic hemopoiesisVascular endothelial growth factor receptor 2Homo sapiens (human)
cellular response to vascular endothelial growth factor stimulusVascular endothelial growth factor receptor 2Homo sapiens (human)
vascular endothelial growth factor receptor-2 signaling pathwayVascular endothelial growth factor receptor 2Homo sapiens (human)
peptidyl-tyrosine autophosphorylationVascular endothelial growth factor receptor 2Homo sapiens (human)
vascular endothelial growth factor signaling pathwayVascular endothelial growth factor receptor 2Homo sapiens (human)
surfactant homeostasisVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of MAPK cascadeVascular endothelial growth factor receptor 2Homo sapiens (human)
negative regulation of neuron apoptotic processVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of blood vessel endothelial cell migrationVascular endothelial growth factor receptor 2Homo sapiens (human)
cell fate commitmentVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of angiogenesisVascular endothelial growth factor receptor 2Homo sapiens (human)
protein autophosphorylationVascular endothelial growth factor receptor 2Homo sapiens (human)
vascular endothelial growth factor receptor signaling pathwayVascular endothelial growth factor receptor 2Homo sapiens (human)
lung alveolus developmentVascular endothelial growth factor receptor 2Homo sapiens (human)
post-embryonic camera-type eye morphogenesisVascular endothelial growth factor receptor 2Homo sapiens (human)
epithelial cell proliferationVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of positive chemotaxisVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of nitric-oxide synthase biosynthetic processVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of focal adhesion assemblyVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionVascular endothelial growth factor receptor 2Homo sapiens (human)
calcium ion homeostasisVascular endothelial growth factor receptor 2Homo sapiens (human)
blood vessel endothelial cell differentiationVascular endothelial growth factor receptor 2Homo sapiens (human)
vascular wound healingVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeVascular endothelial growth factor receptor 2Homo sapiens (human)
semaphorin-plexin signaling pathwayVascular endothelial growth factor receptor 2Homo sapiens (human)
stem cell proliferationVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of cell migration involved in sprouting angiogenesisVascular endothelial growth factor receptor 2Homo sapiens (human)
regulation of hematopoietic progenitor cell differentiationVascular endothelial growth factor receptor 2Homo sapiens (human)
regulation of bone developmentVascular endothelial growth factor receptor 2Homo sapiens (human)
cellular response to hydrogen sulfideVascular endothelial growth factor receptor 2Homo sapiens (human)
negative regulation of endothelial cell apoptotic processVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of stem cell proliferationVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of endothelial cell chemotaxisVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of vasculogenesisVascular endothelial growth factor receptor 2Homo sapiens (human)
regulation of MAPK cascadeVascular endothelial growth factor receptor 2Homo sapiens (human)
multicellular organism developmentVascular endothelial growth factor receptor 2Homo sapiens (human)
cell migrationVascular endothelial growth factor receptor 2Homo sapiens (human)
endothelial cell differentiationVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of kinase activityVascular endothelial growth factor receptor 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (16)

Processvia Protein(s)Taxonomy
protein tyrosine kinase activityHepatocyte growth factor receptorHomo sapiens (human)
protein bindingHepatocyte growth factor receptorHomo sapiens (human)
ATP bindingHepatocyte growth factor receptorHomo sapiens (human)
semaphorin receptor activityHepatocyte growth factor receptorHomo sapiens (human)
protein phosphatase bindingHepatocyte growth factor receptorHomo sapiens (human)
identical protein bindingHepatocyte growth factor receptorHomo sapiens (human)
molecular function activator activityHepatocyte growth factor receptorHomo sapiens (human)
hepatocyte growth factor receptor activityHepatocyte growth factor receptorHomo sapiens (human)
protein tyrosine kinase activityVascular endothelial growth factor receptor 2Homo sapiens (human)
transmembrane receptor protein tyrosine kinase activityVascular endothelial growth factor receptor 2Homo sapiens (human)
vascular endothelial growth factor receptor activityVascular endothelial growth factor receptor 2Homo sapiens (human)
integrin bindingVascular endothelial growth factor receptor 2Homo sapiens (human)
protein bindingVascular endothelial growth factor receptor 2Homo sapiens (human)
ATP bindingVascular endothelial growth factor receptor 2Homo sapiens (human)
coreceptor activityVascular endothelial growth factor receptor 2Homo sapiens (human)
growth factor bindingVascular endothelial growth factor receptor 2Homo sapiens (human)
vascular endothelial growth factor bindingVascular endothelial growth factor receptor 2Homo sapiens (human)
identical protein bindingVascular endothelial growth factor receptor 2Homo sapiens (human)
cadherin bindingVascular endothelial growth factor receptor 2Homo sapiens (human)
Hsp90 protein bindingVascular endothelial growth factor receptor 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (17)

Processvia Protein(s)Taxonomy
extracellular regionHepatocyte growth factor receptorHomo sapiens (human)
plasma membraneHepatocyte growth factor receptorHomo sapiens (human)
basal plasma membraneHepatocyte growth factor receptorHomo sapiens (human)
cell surfaceHepatocyte growth factor receptorHomo sapiens (human)
membraneHepatocyte growth factor receptorHomo sapiens (human)
postsynapseHepatocyte growth factor receptorHomo sapiens (human)
basal plasma membraneHepatocyte growth factor receptorHomo sapiens (human)
plasma membraneHepatocyte growth factor receptorHomo sapiens (human)
receptor complexHepatocyte growth factor receptorHomo sapiens (human)
extracellular regionVascular endothelial growth factor receptor 2Homo sapiens (human)
nucleusVascular endothelial growth factor receptor 2Homo sapiens (human)
endosomeVascular endothelial growth factor receptor 2Homo sapiens (human)
early endosomeVascular endothelial growth factor receptor 2Homo sapiens (human)
endoplasmic reticulumVascular endothelial growth factor receptor 2Homo sapiens (human)
Golgi apparatusVascular endothelial growth factor receptor 2Homo sapiens (human)
plasma membraneVascular endothelial growth factor receptor 2Homo sapiens (human)
external side of plasma membraneVascular endothelial growth factor receptor 2Homo sapiens (human)
cell junctionVascular endothelial growth factor receptor 2Homo sapiens (human)
membrane raftVascular endothelial growth factor receptor 2Homo sapiens (human)
anchoring junctionVascular endothelial growth factor receptor 2Homo sapiens (human)
sorting endosomeVascular endothelial growth factor receptor 2Homo sapiens (human)
plasma membraneVascular endothelial growth factor receptor 2Homo sapiens (human)
receptor complexVascular endothelial growth factor receptor 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (3)

Assay IDTitleYearJournalArticle
AID1276910Inhibition of recombinant N-terminal 6His-tagged VEGFR-2 (unknown origin) using FL-Peptide 22 as substrate after 90 mins by mobility shift assay2016European journal of medicinal chemistry, Jan-27, Volume: 108Recent advances in the development of dual VEGFR and c-Met small molecule inhibitors as anticancer drugs.
AID1276937Cytotoxicity against HUVEC assessed as inhibition of VEGF-independent growth after 72 hrs by CellTiter-Glo method2016European journal of medicinal chemistry, Jan-27, Volume: 108Recent advances in the development of dual VEGFR and c-Met small molecule inhibitors as anticancer drugs.
AID1276909Inhibition of recombinant N-terminal GST-tagged human Met using FLPeptide 2 as substrate after 90 mins by mobility shift assay2016European journal of medicinal chemistry, Jan-27, Volume: 108Recent advances in the development of dual VEGFR and c-Met small molecule inhibitors as anticancer drugs.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (15)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's9 (60.00)24.3611
2020's6 (40.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 32.38

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 Index32.38 (24.57)
Research Supply Index3.00 (2.92)
Research Growth Index4.62 (4.65)
Search Engine Demand Index35.22 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (32.38)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials4 (26.67%)5.53%
Reviews1 (6.67%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other10 (66.67%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]