Page last updated: 2024-12-11

ac 7700

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

Description

AC 7700: a vascular disrupting agent; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID6918404
CHEMBL ID585539
SCHEMBL ID1419930
MeSH IDM0350356

Synonyms (32)

Synonym
rpr-258062a
cs-39-l-ser.hcl
ombrabulin hydrochloride
ac-7700 ,
ave-8062a
ac 7700
CHEMBL585539
D09787
ombrabulin hydrochloride (jan)
253426-24-3
ave 8062
propanamide, 2-amino-3-hydroxy-n-(2-methoxy-5-((1z)-2-(3,4,5-trimethoxyphenyl)ethenyl)phenyl)-, monohydrochloride, (2s)-
unii-kxz9ndo6h0
ave 8062a
kxz9ndo6h0 ,
ombrabulin hydrochloride [jan]
propanamide, 2-amino-3-hydroxy-n-(2-methoxy-5-((1z)-2-(3,4,5-trimethoxyphenyl)ethenyl)phenyl)-, hydrochloride (1:1), (2s)-
propanamide, 2-amino-3-hydroxy-n-(2-methoxy-5-((1z)-2-(3,4,5-trimethoxyphenyl)ethenyl)phenyl)-,monohydrochloride, (2s)-
SCHEMBL1419930
253609-44-8
DTXSID50426074
ombrabulin (hydrochloride)
CS-5451
HY-18256
AKOS030526753
(z)-n-[2-methoxy-5-[2-(3,4,5-trimethoxyphenyl)vinyl] phenyl]-l-serinamide hydrochloride
(2s)-2-amino-3-hydroxy-n-[2-methoxy-5-[(z)-2-(3,4,5-trimethoxyphenyl)ethenyl]phenyl]propanamide;hydrochloride
BCP29573
ac7700 (hydrochloride)
ave8062 (hydrochloride)
Q27282491
MS-27877

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" Close collaboration with cardiology colleagues for early indicators of serious cardiac adverse events will likely minimize toxicity while optimizing the therapeutic potential of VDAs and ultimately enhancing patient outcomes."( Cardiovascular toxicity profiles of vascular-disrupting agents.
Lenihan, DJ; Subbiah, IM; Tsimberidou, AM, 2011
)
0.37
" The most frequent related adverse events in this group were diarrhea, nausea, and hypertension."( An open-label, dose-escalation, safety, and pharmacokinetics phase I study of ombrabulin, a vascular disrupting agent, administered as a 30-min intravenous infusion every 3 weeks in Japanese patients with advanced solid tumors.
Fujisaka, Y; Hayashi, H; Kiyota, H; Kurata, T; Kuroda, S; Murakami, H; Nakagawa, K; Ono, A; Onozawa, Y; Takahashi, T; Tanaka, K; Watanabe, J; Yamamoto, N, 2014
)
0.4

Pharmacokinetics

ExcerptReferenceRelevance
" Safety, tumor response, pharmacokinetics, and pharmacodynamic biomarkers were evaluated."( Phase I safety, pharmacokinetic and pharmacodynamic evaluation of the vascular disrupting agent ombrabulin (AVE8062) in patients with advanced solid tumors.
Bahleda, R; Braghetti, A; Cohen, P; Delmonte, A; Farace, F; Hospitel, M; Lassau, N; Lorusso, P; Sessa, C; Soria, JC; Tolcher, A; Veyrat-Follet, C, 2013
)
0.39
"To determine ombrabulin's maximum tolerated dose and dose recommended for Japanese patients with advanced solid tumors and to assess its antitumor activity and overall safety and pharmacokinetic profiles."( An open-label, dose-escalation, safety, and pharmacokinetics phase I study of ombrabulin, a vascular disrupting agent, administered as a 30-min intravenous infusion every 3 weeks in Japanese patients with advanced solid tumors.
Fujisaka, Y; Hayashi, H; Kiyota, H; Kurata, T; Kuroda, S; Murakami, H; Nakagawa, K; Ono, A; Onozawa, Y; Takahashi, T; Tanaka, K; Watanabe, J; Yamamoto, N, 2014
)
0.4
" Pharmacokinetic parameters were comparable to those in non-Japanese patients."( An open-label, dose-escalation, safety, and pharmacokinetics phase I study of ombrabulin, a vascular disrupting agent, administered as a 30-min intravenous infusion every 3 weeks in Japanese patients with advanced solid tumors.
Fujisaka, Y; Hayashi, H; Kiyota, H; Kurata, T; Kuroda, S; Murakami, H; Nakagawa, K; Ono, A; Onozawa, Y; Takahashi, T; Tanaka, K; Watanabe, J; Yamamoto, N, 2014
)
0.4
" The safety and pharmacokinetic profiles were comparable between Japanese and Caucasian patients (funded by Sanofi; ClinicalTrials."( An open-label, dose-escalation, safety, and pharmacokinetics phase I study of ombrabulin, a vascular disrupting agent, administered as a 30-min intravenous infusion every 3 weeks in Japanese patients with advanced solid tumors.
Fujisaka, Y; Hayashi, H; Kiyota, H; Kurata, T; Kuroda, S; Murakami, H; Nakagawa, K; Ono, A; Onozawa, Y; Takahashi, T; Tanaka, K; Watanabe, J; Yamamoto, N, 2014
)
0.4
" Pharmacokinetic analyses did not show any relevant drug interactions."( A phase I pharmacokinetic study of the vascular disrupting agent ombrabulin (AVE8062) and docetaxel in advanced solid tumours.
Dieras, V; Eskens, FA; Fontaine, H; Hospitel, M; Oprea, C; Tosi, D; Tresca, P; Van der Gaast, A; Van Doorn, L; Veyrat-Follet, C, 2014
)
0.4
" Ombrabulin clearance was high with a short terminal half-life and a medium volume of distribution."( Phase I clinical and pharmacokinetic study of ombrabulin (AVE8062) combined with cisplatin/docetaxel or carboplatin/paclitaxel in patients with advanced solid tumors.
Bahleda, R; Capri, G; Daglish, B; Del Conte, G; Gianni, L; Hospitel, M; Oprea, C; Sessa, C; Soria, JC; Varga, A, 2014
)
0.4

Compound-Compound Interactions

ExcerptReferenceRelevance
" Ombrabulin was combined with two standard taxane/platinum doublets in a phase I study to determine the recommended combination doses."( Phase I clinical and pharmacokinetic study of ombrabulin (AVE8062) combined with cisplatin/docetaxel or carboplatin/paclitaxel in patients with advanced solid tumors.
Bahleda, R; Capri, G; Daglish, B; Del Conte, G; Gianni, L; Hospitel, M; Oprea, C; Sessa, C; Soria, JC; Varga, A, 2014
)
0.4
"5-35 mg/m2) in combination with docetaxel (60 or 75 mg/m2) and cisplatin (75 mg/m2), agents were administered 24 h apart every 3 weeks to Japanese patients with advanced solid tumors."( Phase 1 study of ombrabulin in combination with docetaxel and cisplatin in Japanese patients with advanced solid tumors.
Ecstein-Fraisse, E; Hida, T; Horiike, A; Horio, Y; Nishio, M; Satouchi, M; Sunaga, Y, 2018
)
0.48

Dosage Studied

ExcerptRelevanceReference
" This combination effect was found over wide dosage ranges of AC-7700 (20-80 mg/kg) and CDDP (2."( Combination effect of AC-7700, a novel combretastatin A-4 derivative, and cisplatin against murine and human tumors in vivo.
Ehara, S; Harada, K; Morinaga, Y; Nihei, Y; Suga, Y; Suzuki, M, 2003
)
0.32
[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)
Tubulin beta-2B chainBos taurus (cattle)IC50 (µMol)13.00000.25001.88388.7000AID1278670
Similar to alpha-tubulin isoform 1 Bos taurus (cattle)IC50 (µMol)13.00000.25001.87798.7000AID1278670
Similar to alpha-tubulin isoform 1 Bos taurus (cattle)IC50 (µMol)13.00000.25001.86568.7000AID1278670
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (3)

Processvia Protein(s)Taxonomy
microtubule-based processTubulin beta-2B chainBos taurus (cattle)
nervous system developmentTubulin beta-2B chainBos taurus (cattle)
positive regulation of axon guidanceTubulin beta-2B chainBos taurus (cattle)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (3)

Processvia Protein(s)Taxonomy
GTPase activityTubulin beta-2B chainBos taurus (cattle)
metal ion bindingTubulin beta-2B chainBos taurus (cattle)
protein heterodimerization activityTubulin beta-2B chainBos taurus (cattle)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (1)

Processvia Protein(s)Taxonomy
microtubule cytoskeletonTubulin beta-2B chainBos taurus (cattle)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (12)

Assay IDTitleYearJournalArticle
AID1278682Displacement of [3H]colchicine from bovine brain tubulin at 1 uM after 10 mins by scintillation counting analysis2016Bioorganic & medicinal chemistry, Mar-01, Volume: 24, Issue:5
Design, synthesis, and biological evaluation of water-soluble amino acid prodrug conjugates derived from combretastatin, dihydronaphthalene, and benzosuberene-based parent vascular disrupting agents.
AID1278670Inhibition of bovine brain tubulin polymerization preincubated for 15 mins by spectrophotometric analysis2016Bioorganic & medicinal chemistry, Mar-01, Volume: 24, Issue:5
Design, synthesis, and biological evaluation of water-soluble amino acid prodrug conjugates derived from combretastatin, dihydronaphthalene, and benzosuberene-based parent vascular disrupting agents.
AID1278675Cytotoxicity against human DU145 cells assessed as growth inhibition after 48 hrs by SRB assay2016Bioorganic & medicinal chemistry, Mar-01, Volume: 24, Issue:5
Design, synthesis, and biological evaluation of water-soluble amino acid prodrug conjugates derived from combretastatin, dihydronaphthalene, and benzosuberene-based parent vascular disrupting agents.
AID1278683Displacement of [3H]colchicine from bovine brain tubulin at 5 uM after 10 mins by scintillation counting analysis2016Bioorganic & medicinal chemistry, Mar-01, Volume: 24, Issue:5
Design, synthesis, and biological evaluation of water-soluble amino acid prodrug conjugates derived from combretastatin, dihydronaphthalene, and benzosuberene-based parent vascular disrupting agents.
AID443467Cytotoxicity against human HeLa cells by MTT assay2009Bioorganic & medicinal chemistry letters, Dec-15, Volume: 19, Issue:24
Synthesis and antitumor-evaluation of cyclopropyl-containing combretastatin analogs.
AID512071Antitumor activity against mouse 3LL cells transplanted in to BALB/c mouse assessed as tumor growth inhibition at 80 mg/kg, ip qd for 4 days2010Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17
Identification of CKD-516: a potent tubulin polymerization inhibitor with marked antitumor activity against murine and human solid tumors.
AID1278672Prodrug conversion assessed as porcine leucine aminopeptidase-mediated compound cleavage by HPLC analysis2016Bioorganic & medicinal chemistry, Mar-01, Volume: 24, Issue:5
Design, synthesis, and biological evaluation of water-soluble amino acid prodrug conjugates derived from combretastatin, dihydronaphthalene, and benzosuberene-based parent vascular disrupting agents.
AID1278673Cytotoxicity against human SKOV3 cells assessed as growth inhibition after 48 hrs by SRB assay2016Bioorganic & medicinal chemistry, Mar-01, Volume: 24, Issue:5
Design, synthesis, and biological evaluation of water-soluble amino acid prodrug conjugates derived from combretastatin, dihydronaphthalene, and benzosuberene-based parent vascular disrupting agents.
AID1278674Cytotoxicity against human NCI-H460 cells assessed as growth inhibition after 48 hrs by SRB assay2016Bioorganic & medicinal chemistry, Mar-01, Volume: 24, Issue:5
Design, synthesis, and biological evaluation of water-soluble amino acid prodrug conjugates derived from combretastatin, dihydronaphthalene, and benzosuberene-based parent vascular disrupting agents.
AID443468Cytotoxicity against human MCF7 cells by MTT assay2009Bioorganic & medicinal chemistry letters, Dec-15, Volume: 19, Issue:24
Synthesis and antitumor-evaluation of cyclopropyl-containing combretastatin analogs.
AID512072Antitumor activity against mouse 3LL cells transplanted in to BALB/c mouse assessed as tumor growth inhibition at 40 mg/kg, ip twice a week2010Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17
Identification of CKD-516: a potent tubulin polymerization inhibitor with marked antitumor activity against murine and human solid tumors.
AID1278671Activity at porcine leucine aminopeptidase by HPLC analysis2016Bioorganic & medicinal chemistry, Mar-01, Volume: 24, Issue:5
Design, synthesis, and biological evaluation of water-soluble amino acid prodrug conjugates derived from combretastatin, dihydronaphthalene, and benzosuberene-based parent vascular disrupting agents.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (27)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's2 (7.41)18.2507
2000's10 (37.04)29.6817
2010's15 (55.56)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 20.95

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 Index20.95 (24.57)
Research Supply Index3.58 (2.92)
Research Growth Index5.16 (4.65)
Search Engine Demand Index28.85 (26.88)
Search Engine Supply Index3.67 (0.95)

This Compound (20.95)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials7 (25.00%)5.53%
Reviews5 (17.86%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other16 (57.14%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]