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Chemical Compound Review

CHEMBL85156     6-[4-[2,2-bis(4- fluorophenyl)ethylamino]-1...

Synonyms: SureCN1527824, CHEBI:233701, LS-186957, LS-187603, S-9788, ...
 
 
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Disease relevance of S-9788

 

High impact information on S-9788

  • We conclude that S 9788 is a novel agent capable of reversing MDR in vitro and in vivo, and whose pharmacological profile warrants its selection as a candidate drug for eventual assessment in the clinic [1].
  • The activity of S 9788 depended on both the MDR cell line and the cytotoxic agent [1].
  • In vitro activity of S 9788 on a multidrug-resistant leukemic cell line and on normal hematopoietic cells-reversal of multidrug resistance by sera from phase I-treated patients [3].
  • In two treatment regimens (Q4D days 1, 5 and 9 and QD days 1-9), S 9788 enhanced the antitumor activity of vincristine in a dose-dependent manner, resulting in a complete circumvention of drug resistance for well-tolerated doses of S 9788 [4].
  • An association between reversal and P-glycoprotein (P-170) expression suggests that S 9788 exerts its activity through P-glycoprotein [2].
 

Associations of S-9788 with other chemical compounds

 

Analytical, diagnostic and therapeutic context of S-9788

References

  1. In vitro and in vivo circumvention of multidrug resistance by Servier 9788, a novel triazinoaminopiperidine derivative. Pierré, A., Dunn, T.A., Kraus-Berthier, L., Léonce, S., Saint-Dizier, D., Régnier, G., Dhainaut, A., Berlion, M., Bizzari, J.P., Atassi, G. Investigational new drugs. (1992) [Pubmed]
  2. Reversal of inherent multidrug-resistance in primary human renal cell carcinoma cell cultures by S 9788. Efferth, T., Dunn, T.A., Berlion, M., Langenbahn, H., Pommerenke, E.W., Volm, M. Anticancer Res. (1993) [Pubmed]
  3. In vitro activity of S 9788 on a multidrug-resistant leukemic cell line and on normal hematopoietic cells-reversal of multidrug resistance by sera from phase I-treated patients. Soudon, J., Berlion, M., Lucas, C., Haddad, P., Bizzari, J.P., Calvo, F. Cancer Chemother. Pharmacol. (1995) [Pubmed]
  4. In vivo evidence of complete circumvention of vincristine resistance by a new triazinoaminopiperidine derivative S 9788 in P388/VCR leukemia model. Cros, S., Guilbaud, N., Berlion, M., Dunn, T., Regnier, G., Dhainaut, A., Atassi, G., Bizzari, J.P. Cancer Chemother. Pharmacol. (1992) [Pubmed]
 
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