Compounds > cevipabulin
Page last updated: 2024-11-12

cevipabulin

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

Cross-References

ID SourceID
PubMed CID11488110
CHEMBL ID1182714
SCHEMBL ID4042827
MeSH IDM0555369

Synonyms (30)

Synonym
CHEMBL1182714
cevipabulin ,
cevipabulin [inn]
849550-05-6
p14m0dws2j ,
tti-237
cevipabulin [who-dd]
SCHEMBL4042827
CS-4196
DTXSID00233997
5-chloro-6-{2,6-difluoro-4-[3-(methylamino)propoxy]phenyl}-n-[(1s)-2,2,2-trifluoro-1-methylethyl][1,2,4]triazolo[1,5-a]pyrimidin-7-amine
5-chloro-6-{2,6-difluoro-4-[3-(methylamino) propoxy]phenyl}-n-[(1s)-2,2,2-trifluoro-1-methylethyl][1,2,4]triazolo[1,5-a]pyrimidin-7-amine
5-chloro-6{2,6-difluoro-4-[3-(methylamino)propoxy]phenyl}-n-[(1s)-2,2,2-trifluoro-1-methylethyl][1,2,4]triazolo[1,5-a]pyrimidin-7-amine
HY-14949
J-690362
EX-A607
AKOS030526926
5-chloro-6-[2,6-difluoro-4-[3-(methylamino)propoxy]phenyl]-n-((1s)-2,2,2-trifluoro-1-methylethyl)-[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
5-chloro-6-{2,6-difluoro-4-[3-(methylamino)propoxy]phenyl}-n-[(2s)-1,1,1-trifluoropropan-2-yl]-[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
cevipabulin(tti 237)
mfcd09832720
DB12533
849550-05-6 (free base)
5-chloro-6-[2,6-difluoro-4-[3-(methylamino)propoxy]phenyl]-n-[(1s)-2,2,2-trifluoro-1- methylethyl]-[1,2,4]triazolo[1,5-a]pyrimidin-7-amine.
tti 237; tti-237; tti237; d06576; d 06576; d-06576
BCP28162
5-chloro-6-[2,6-difluoro-4-[3-(methylamino)propoxy]phenyl]-n-[(2s)-1,1,1-trifluoropropan-2-yl]-[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
(s)-5-chloro-6-(2,6-difluoro-4-(3-(methylamino)propoxy)phenyl)-n-(1,1,1-trifluoropropan-2-yl)-[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
Q27285989
MS-28564

Research Excerpts

Overview

Cevipabulin (TTI-237) is a novel, small synthetic molecule with an unusual biological mode of action.

ExcerptReferenceRelevance
"Cevipabulin (TTI-237) is a novel, small synthetic molecule with an unusual biological mode of action."( Cevipabulin (TTI-237): preclinical and clinical results for a novel antimicrotubule agent.
Ayral-Kaloustian, S; Beyer, C; Zhang, N, 2009)		2.52

Bioavailability

ExcerptReferenceRelevance
" This led to the identification of selected triazolopyrimidines and phenylpyrimidines that are orally bioavailable and brain-penetrant without disruption of Pgp function."( Brain-penetrant, orally bioavailable microtubule-stabilizing small molecules are potential candidate therapeutics for Alzheimer's disease and related tauopathies.
Ballatore, C; Brunden, KR; Cornec, AS; Gay, B; Hoye, AT; Hyde, E; James, MJ; Lee, VM; Lou, K; Smith, AB; Trojanowski, JQ; Yao, Y, 2014)		0.4

Dosage Studied

ExcerptRelevanceReference
" TTI-237 dosage was de-escalated to 22."( A phase I dose escalation study of TTI-237 in patients with advanced malignant solid tumors.
Arnold, SM; Bukowski, RM; Cooper, W; Gauthier, E; Lockhart, AC; Rothenberg, ML; Wang, KK; Wang-Gillam, A, 2012)		0.38
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (10)

Assay IDTitleYearJournalArticle
AID1182024Drug level in CD1 mouse plasma at 5 mg/kg, ip after 1 hr by LC-MS/MS system2014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
Brain-penetrant, orally bioavailable microtubule-stabilizing small molecules are potential candidate therapeutics for Alzheimer's disease and related tauopathies.
AID1182025Ratio of drug level in brain to plasma in CD1 mouse at 5 mg/kg, ip after 1 hr by LC-MS/MS system2014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
Brain-penetrant, orally bioavailable microtubule-stabilizing small molecules are potential candidate therapeutics for Alzheimer's disease and related tauopathies.
AID1496233Induction of microtubule disruption in HEK293 cells assessed as total alpha tubulin levels at 1 uM after 4 hrs by ELISA relative to control2018Bioorganic & medicinal chemistry letters, 07-01, Volume: 28, Issue:12
Design, synthesis and evaluation of photoactivatable derivatives of microtubule (MT)-active [1,2,4]triazolo[1,5-a]pyrimidines.
AID1182022Inhibition of human P-glycoprotein expressed in NCI/ADR-RES cells assessed as reduction of calcein-AM transport after 20 mins by fluorescence assay2014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
Brain-penetrant, orally bioavailable microtubule-stabilizing small molecules are potential candidate therapeutics for Alzheimer's disease and related tauopathies.
AID1496232Induction of microtubule stabilization in HEK293 cells assessed as increase in acetylated alpha tubulin levels at 10 uM after 4 hrs by ELISA relative to control2018Bioorganic & medicinal chemistry letters, 07-01, Volume: 28, Issue:12
Design, synthesis and evaluation of photoactivatable derivatives of microtubule (MT)-active [1,2,4]triazolo[1,5-a]pyrimidines.
AID1182023Drug level in CD1 mouse brain at 5 mg/kg, ip after 1 hr by LC-MS/MS system2014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
Brain-penetrant, orally bioavailable microtubule-stabilizing small molecules are potential candidate therapeutics for Alzheimer's disease and related tauopathies.
AID1496234Induction of microtubule disruption in HEK293 cells assessed as total alpha tubulin levels at 10 uM after 4 hrs by ELISA relative to control2018Bioorganic & medicinal chemistry letters, 07-01, Volume: 28, Issue:12
Design, synthesis and evaluation of photoactivatable derivatives of microtubule (MT)-active [1,2,4]triazolo[1,5-a]pyrimidines.
AID1182021Induction of microtubule stabilization in human QBI293 cells assessed as increase in acetylated alpha-tubulin at 100 nM after 4 hrs by immunofluorescence assay relative to control2014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
Brain-penetrant, orally bioavailable microtubule-stabilizing small molecules are potential candidate therapeutics for Alzheimer's disease and related tauopathies.
AID1496231Induction of microtubule stabilization in HEK293 cells assessed as increase in acetylated alpha tubulin levels at 1 uM after 4 hrs by ELISA relative to control2018Bioorganic & medicinal chemistry letters, 07-01, Volume: 28, Issue:12
Design, synthesis and evaluation of photoactivatable derivatives of microtubule (MT)-active [1,2,4]triazolo[1,5-a]pyrimidines.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (11)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's4 (36.36)29.6817
2010's5 (45.45)24.3611
2020's2 (18.18)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 21.42

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 Index21.42 (24.57)
Research Supply Index2.56 (2.92)
Research Growth Index4.68 (4.65)
Search Engine Demand Index18.60 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (21.42)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1 (9.09%)5.53%
Reviews1 (9.09%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other9 (81.82%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
verapamil
Verapamil: A calcium channel blocker that is a class IV anti-arrhythmia agent.. verapamil : A racemate comprising equimolar amounts of dexverapamil and (S)-verapamil. An L-type calcium channel blocker of the phenylalkylamine class, it is used (particularly as the hydrochloride salt) in the treatment of hypertension, angina pectoris and cardiac arrhythmia, and as a preventive medication for migraine.. 2-(3,4-dimethoxyphenyl)-5-{[2-(3,4-dimethoxyphenyl)ethyl](methyl)amino}-2-(propan-2-yl)pentanenitrile : A tertiary amino compound that is 3,4-dimethoxyphenylethylamine in which the hydrogens attached to the nitrogen are replaced by a methyl group and a 4-cyano-4-(3,4-dimethoxyphenyl)-5-methylhexyl group.		2.110aromatic ether;
nitrile;
polyether;
tertiary amino compound
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).		2.520taxane diterpenoid;
tetracyclic diterpenoid		antineoplastic agent;
human metabolite;
metabolite;
microtubule-stabilising agent
triazoles
Triazoles: Heterocyclic compounds containing a five-membered ring with two carbon atoms and three nitrogen atoms with the molecular formula C2H3N3.. triazoles : An azole in which the five-membered heterocyclic aromatic skeleton contains three N atoms and two C atoms.		6.07811,2,3-triazole
desoxyepothilone b
desoxyepothilone B: microtubule-targeted antitumor agent; lacking the epoxide of epothilone B; may be equiv to epothilone D. epothilone D : An epithilone that is epithilone C in which the hydrogen at position 13 of the oxacyclohexadec-13-ene-2,6-dione macrocycle has been replaced by a methyl group.		2.110epothilonemicrotubule-stabilising agent
cyclosporine
ramihyphin A: one of the metabolites produced by Fusarium sp. S-435; RN given refers to cpd with unknown MF		2.110homodetic cyclic peptideanti-asthmatic drug;
anticoronaviral agent;
antifungal agent;
antirheumatic drug;
carcinogenic agent;
dermatologic drug;
EC 3.1.3.16 (phosphoprotein phosphatase) inhibitor;
geroprotector;
immunosuppressive agent;
metabolite
2-(2,6-diisopropylphenyl)-5-hydroxy-1h-isoindole-1,3-dione
2-(2,6-diisopropylphenyl)-5-hydroxy-1H-isoindole-1,3-dione: structure in first source		2.110
guanosine triphosphate
Guanosine Triphosphate: Guanosine 5'-(tetrahydrogen triphosphate). A guanine nucleotide containing three phosphate groups esterified to the sugar moiety.		2.0510guanosine 5'-phosphate;
purine ribonucleoside 5'-triphosphate		Escherichia coli metabolite;
mouse metabolite;
uncoupling protein inhibitor
ConditionIndicatedRelationship StrengthStudiesTrials
Tauopathies
Neurodegenerative disorders involving deposition of abnormal tau protein isoforms (TAU PROTEINS) in neurons and glial cells in the brain. Pathological aggregations of tau proteins are associated with mutation of the tau gene on chromosome 17 in patients with ALZHEIMER DISEASE; DEMENTIA; PARKINSONIAN DISORDERS; progressive supranuclear palsy (SUPRANUCLEAR PALSY, PROGRESSIVE); and corticobasal degeneration.		02.5220
Acute Confusional Senile Dementia
[description not available]		02.5220
Alzheimer Disease
A degenerative disease of the BRAIN characterized by the insidious onset of DEMENTIA. Impairment of MEMORY, judgment, attention span, and problem solving skills are followed by severe APRAXIAS and a global loss of cognitive abilities. The condition primarily occurs after age 60, and is marked pathologically by severe cortical atrophy and the triad of SENILE PLAQUES; NEUROFIBRILLARY TANGLES; and NEUROPIL THREADS. (From Adams et al., Principles of Neurology, 6th ed, pp1049-57)		02.5220
Amyloid Deposits
[description not available]		02.2510
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		02.2510
Benign Neoplasms
[description not available]		04.7721
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.		16.7721
Carcinoma, Epidermoid
[description not available]		02.0410
Carcinoma, Squamous Cell
A carcinoma derived from stratified SQUAMOUS EPITHELIAL CELLS. It may also occur in sites where glandular or columnar epithelium is normally present. (From Stedman, 25th ed)		02.0410