Page last updated: 2024-11-07

s 9788

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

Description

S 9788: structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID107903
CHEMBL ID85156
SCHEMBL ID1527824
MeSH IDM0206997

Synonyms (15)

Synonym
CHEMBL85156 ,
n,n''-diallyl-6-{4-[2,2-bis-(4-fluoro-phenyl)-ethylamino]-piperidin-1-yl}-[1,3,5]triazine-2,4-diamine
bdbm50053888
n,n''-diallyl-6-{4-[2,2-bis-(4-fluoro-phenyl)-ethylamino]-piperidin-1-yl}-[1,3,5]triazine-2,4-diamine; h2o
s-9788
6-(4-(2,2-di(4-fluorophenyl)ethylamino)-1-piperidinyl)-n,n'-di-2-propenyl-1,3,5-triazine-2,4-diamine
1,3,5-triazine-2,4-diamine, 6-(4-((2,2-bis(4-fluorophenyl)ethyl)amino)-1-piperidinyl)-n,n'-di-2-propenyl-
s9788 ,
s 9788
6-[4-[2,2-bis(4-fluorophenyl)ethylamino]piperidin-1-yl]-2-n,4-n-bis(prop-2-enyl)-1,3,5-triazine-2,4-diamine
140945-01-3
SCHEMBL1527824
DTXSID80161502
GERNFWKTMKWULM-UHFFFAOYSA-N
n2,n4-diallyl-6-(4-((2,2-bis(4-fluorophenyl)ethyl)amino)piperidin-1-yl)-1,3,5-triazine-2,4-diamine

Research Excerpts

Overview

S 9788 is a novel triazinoaminopiperidine derivative which does not belong to any of the classes of compounds known to reverse multidrug resistance (MDR)

ExcerptReferenceRelevance
"S 9788 is a novel triazinoaminopiperidine derivative which does not belong to any of the classes of compounds known to reverse multidrug resistance (MDR). "( In vitro and in vivo circumvention of multidrug resistance by Servier 9788, a novel triazinoaminopiperidine derivative.
Atassi, G; Berlion, M; Bizzari, JP; Dhainaut, A; Dunn, TA; Kraus-Berthier, L; Léonce, S; Pierré, A; Régnier, G; Saint-Dizier, D, 1992
)
1.73

Pharmacokinetics

ExcerptReferenceRelevance
" Pharmacokinetic studies were performed in 24 patients."( Phase I clinical and pharmacokinetic study of S9788, a new multidrug-resistance reversal agent given alone and in combination with doxorubicin to patients with advanced solid tumors.
Ardiet, C; Barbet, N; Bastian, G; Catimel, G; Clavel, M; Dumortier, A; Evene, E; Foy, M; Froudarakis, M; Grossin, F; Guastalla, JP; Lucas, C; Mazier, B; Négrier, S; Rebattu, P; Sarkany, M; Tranchand, B, 1998
)
0.3
" The pharmacokinetic parameters of doxorubicin in this study were close to those usually described and were not influenced by escalation of the S9788 dose."( Phase I clinical and pharmacokinetic study of S9788, a new multidrug-resistance reversal agent given alone and in combination with doxorubicin to patients with advanced solid tumors.
Ardiet, C; Barbet, N; Bastian, G; Catimel, G; Clavel, M; Dumortier, A; Evene, E; Foy, M; Froudarakis, M; Grossin, F; Guastalla, JP; Lucas, C; Mazier, B; Négrier, S; Rebattu, P; Sarkany, M; Tranchand, B, 1998
)
0.3

Compound-Compound Interactions

ExcerptReferenceRelevance
" We conclude that S9788 administered at the doses and schedule used in this study results in relevant plasma concentrations in humans and can safely be administered in combination with doxorubicin."( Phase IB study of doxorubicin in combination with the multidrug resistance reversing agent S9788 in advanced colorectal and renal cell cancer.
Backx, A; Bleiberg, H; De Mulder, PH; Gerard, B; Hecquet, B; Lucas, C; Punt, CJ; Tueni, E; Van Oosterom, AT; Voest, EE, 1997
)
0.3
"The objectives of this phase I study were to evaluate the toxic effects and the maximum tolerated dose (MTD) of S9788, a new modifier of multidrug resistance (MDR), when given alone and in combination with doxorubicin to patients with advanced solid tumors; to achieve a potentially active plasma concentration of S9788; and to study the pharmacokinetics of both drugs."( Phase I clinical and pharmacokinetic study of S9788, a new multidrug-resistance reversal agent given alone and in combination with doxorubicin to patients with advanced solid tumors.
Ardiet, C; Barbet, N; Bastian, G; Catimel, G; Clavel, M; Dumortier, A; Evene, E; Foy, M; Froudarakis, M; Grossin, F; Guastalla, JP; Lucas, C; Mazier, B; Négrier, S; Rebattu, P; Sarkany, M; Tranchand, B, 1998
)
0.3
" S9788 was given alone as a 30-min infusion at day 1 and in combination with a 50-mg/m2 bolus of doxorubicin at days 8 and 29."( Phase I clinical and pharmacokinetic study of S9788, a new multidrug-resistance reversal agent given alone and in combination with doxorubicin to patients with advanced solid tumors.
Ardiet, C; Barbet, N; Bastian, G; Catimel, G; Clavel, M; Dumortier, A; Evene, E; Foy, M; Froudarakis, M; Grossin, F; Guastalla, JP; Lucas, C; Mazier, B; Négrier, S; Rebattu, P; Sarkany, M; Tranchand, B, 1998
)
0.3

Dosage Studied

ExcerptRelevanceReference
" In this situation, the selection of a correct assay dosage to study the MDR modulation mechanism was a problem."( Simultaneous determination of cytotoxic (adriamycin, vincristine) and modulator of resistance (verapamil, S 9788) drugs in human cells by high-performance liquid chromatography and ultraviolet detection.
Atassi, G; Dubois, J; Hanocq, M; Tassin, JP, 1997
)
0.51
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (21)

Assay IDTitleYearJournalArticle
AID154221Percent of cell viability of P388/VCR-20 murine leukemia cells remaining after inoculation with the modulator alone1996Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20
New purines and purine analogs as modulators of multidrug resistance.
AID53604Increase in adriamycin uptake in modulator-treated cells relative to untreated cells at a concentration of 10 uM1992Journal of medicinal chemistry, Jun-26, Volume: 35, Issue:13
New triazine derivatives as potent modulators of multidrug resistance.
AID94166Increase in adriamycin uptake in modulator-treated cells relative to untreated KB-A1 cells at a concentration of 5 uM1992Journal of medicinal chemistry, Jun-26, Volume: 35, Issue:13
New triazine derivatives as potent modulators of multidrug resistance.
AID121701Ratio of survival time of mice treated with VCR (0.25 mg/kg ip)+modulator given at the optimal dose of 200 mg/kg po/survival time of mice treated with VCR alone.1996Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20
New purines and purine analogs as modulators of multidrug resistance.
AID153489Antitumor activity of vincristine against P388 leukemia cell line in mice at a dose of 100 mg/kg.1992Journal of medicinal chemistry, Jun-26, Volume: 35, Issue:13
New triazine derivatives as potent modulators of multidrug resistance.
AID681334TP_TRANSPORTER: transepithelial transport in Caco 2 cell2004Pharmaceutical research, May, Volume: 21, Issue:5
Predicting P-glycoprotein effects on oral absorption: correlation of transport in Caco-2 with drug pharmacokinetics in wild-type and mdr1a(-/-) mice in vivo.
AID680486TP_TRANSPORTER: inhibition of JC-1 uptake (JC-1: ca 0.1 uM, S9788: 5 uM) in K562 and K562/ADR cells, flow cytometry1997Leukemia, Jul, Volume: 11, Issue:7
Functional assay of multidrug resistant cells using JC-1, a carbocyanine fluorescent probe.
AID53608In vitro activity in DC-3F/AD cell line Ratio of IC50(adriamycin alone) / IC50(adriamycin + modulator) at a concentration of 10 uM1992Journal of medicinal chemistry, Jun-26, Volume: 35, Issue:13
New triazine derivatives as potent modulators of multidrug resistance.
AID154130Antitumor activity of vincristine against P388/VCR leukemia in mice at a dose of 50 mg/kg1992Journal of medicinal chemistry, Jun-26, Volume: 35, Issue:13
New triazine derivatives as potent modulators of multidrug resistance.
AID154128Antitumor activity of vincristine against P388/VCR leukemia in mice at a dose of 100 mg/kg1992Journal of medicinal chemistry, Jun-26, Volume: 35, Issue:13
New triazine derivatives as potent modulators of multidrug resistance.
AID53605Increase in adriamycin uptake in modulator-treated cells relative to untreated cells at a concentration of 5 uM1992Journal of medicinal chemistry, Jun-26, Volume: 35, Issue:13
New triazine derivatives as potent modulators of multidrug resistance.
AID53606Compound was evaluated for in vitro activity in DC-3F/AD cell line (Ratio of IC50(adriamycin alone) / IC50(adriamycin + modulator) at a concentration of 5 uM1992Journal of medicinal chemistry, Jun-26, Volume: 35, Issue:13
New triazine derivatives as potent modulators of multidrug resistance.
AID153490Antitumor activity of vincristine against P388 leukemia cell line in mice at a dose of 50 mg/kg1992Journal of medicinal chemistry, Jun-26, Volume: 35, Issue:13
New triazine derivatives as potent modulators of multidrug resistance.
AID95582Inhibition of [3H]D-888 binding to L-type [Ca2+] channel of membranes from rat skeletal muscle1996Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20
New purines and purine analogs as modulators of multidrug resistance.
AID94173Percent of cell viability remaining after incubating the cells with the modulator alone1992Journal of medicinal chemistry, Jun-26, Volume: 35, Issue:13
New triazine derivatives as potent modulators of multidrug resistance.
AID150364MDR-reversal property tested in vitro on P388/VCR-20 cells, resistance was induced by vincristine1996Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20
New purines and purine analogs as modulators of multidrug resistance.
AID94163MDR-reversal property tested in vitro on KB-A1 cells, resistance was induced by adriamycin1996Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20
New purines and purine analogs as modulators of multidrug resistance.
AID53616Percent of cell viability remaining after incubating with a 10 uM concentration1992Journal of medicinal chemistry, Jun-26, Volume: 35, Issue:13
New triazine derivatives as potent modulators of multidrug resistance.
AID53614Percent of cell viability remaining after incubating the cells with the modulator alone a concentration of 5 uM1992Journal of medicinal chemistry, Jun-26, Volume: 35, Issue:13
New triazine derivatives as potent modulators of multidrug resistance.
AID94169In vitro activity in KB-A1 cell line activity expressed as fold reversion (Ratio of IC50(adriamycin alone) / IC50(adriamycin + modulator) at a concentration of 5 uM1992Journal of medicinal chemistry, Jun-26, Volume: 35, Issue:13
New triazine derivatives as potent modulators of multidrug resistance.
AID94168Percent of cell viability of KB-A1 human epidermoid carcinoma remaining after inoculation with the modulator alone1996Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20
New purines and purine analogs as modulators of multidrug resistance.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (44)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's40 (90.91)18.2507
2000's4 (9.09)29.6817
2010's0 (0.00)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: 10.16

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 weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index10.16 (24.57)
Research Supply Index3.99 (2.92)
Research Growth Index4.15 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (10.16)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials4 (8.16%)5.53%
Reviews3 (6.12%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other42 (85.71%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]