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Chemical Compound Review

KST-1A1459     [(2S)-1-[(2S)-2-benzyl-3- methoxy-5-oxo-2H...

Synonyms: KST-1A1460, AR-1A3120, AR-1A3121, AC1L4M1X, AC1Q5BE8, ...
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Disease relevance of NSC 617668


High impact information on NSC 617668


Biological context of NSC 617668


Anatomical context of NSC 617668


Gene context of NSC 617668

  • Despite its potency and the loss of microtubules in treated cells, the interaction of dolastatin 15 with tubulin in vitro was weak [2].
  • All four SCLC cell lines underwent G2/M arrest within 24 hours of exposure to dolastatin 15, and three had morphologic evidence of apoptosis after 48 hours [4].
  • Following extraction from plasma, using a solid-phase C18 cartridge, capillary zone electrophoresis was used to separate, detect and quantitate dolastatin-10 using the structurally related compound dolastatin-15 as the internal standard [14].

Analytical, diagnostic and therapeutic context of NSC 617668


  1. Phase I and pharmacokinetic study of the water-soluble dolastatin 15 analog LU103793 in patients with advanced solid malignancies. Villalona-Calero, M.A., Baker, S.D., Hammond, L., Aylesworth, C., Eckhardt, S.G., Kraynak, M., Fram, R., Fischkoff, S., Velagapudi, R., Toppmeyer, D., Razvillas, B., Jakimowicz, K., Von Hoff, D.D., Rowinsky, E. J. Clin. Oncol. (1998) [Pubmed]
  2. Dolastatin 15, a potent antimitotic depsipeptide derived from Dolabella auricularia. Interaction with tubulin and effects of cellular microtubules. Bai, R., Friedman, S.J., Pettit, G.R., Hamel, E. Biochem. Pharmacol. (1992) [Pubmed]
  3. Activity of the dolastatin analogue, LU103793, in malignant melanoma. Smyth, J., Boneterre, M.E., Schellens, J., Calvert, H., Greim, G., Wanders, J., Hanauske, A. Ann. Oncol. (2001) [Pubmed]
  4. Dolastatin 15 induces apoptosis and BCL-2 phosphorylation in small cell lung cancer cell lines. Ali, M.A., Rosati, R., Pettit, G.R., Kalemkerian, G.P. Anticancer Res. (1998) [Pubmed]
  5. Growth inhibition of human lymphoma cell lines by the marine products, dolastatins 10 and 15. Beckwith, M., Urba, W.J., Longo, D.L. J. Natl. Cancer Inst. (1993) [Pubmed]
  6. Antineoplastic dolastatins: potent inhibitors of hematopoietic progenitor cells. Jacobsen, S.E., Ruscetti, F.W., Longo, D.L., Keller, J.R. J. Natl. Cancer Inst. (1991) [Pubmed]
  7. A phase I study of the dolastatin-15 analogue tasidotin (ILX651) administered intravenously daily for 5 consecutive days every 3 weeks in patients with advanced solid tumors. Ebbinghaus, S., Rubin, E., Hersh, E., Cranmer, L.D., Bonate, P.L., Fram, R.J., Jekunen, A., Weitman, S., Hammond, L.A. Clin. Cancer Res. (2005) [Pubmed]
  8. Phase I and pharmacokinetic study of the dolastatin-15 analogue tasidotin (ILX651) administered intravenously on days 1, 3, and 5 every 3 weeks in patients with advanced solid tumors. Cunningham, C., Appleman, L.J., Kirvan-Visovatti, M., Ryan, D.P., Regan, E., Vukelja, S., Bonate, P.L., Ruvuna, F., Fram, R.J., Jekunen, A., Weitman, S., Hammond, L.A., Eder, J.P. Clin. Cancer Res. (2005) [Pubmed]
  9. Suppression of microtubule dynamics by binding of cemadotin to tubulin: possible mechanism for its antitumor action. Jordan, M.A., Walker, D., de Arruda, M., Barlozzari, T., Panda, D. Biochemistry (1998) [Pubmed]
  10. Antineoplastic agents 360. Synthesis and cancer cell growth inhibitory studies of dolastatin 15 structural modifications. Pettit, G.R., Flahive, E.J., Boyd, M.R., Bai, R., Hamel, E., Pettit, R.K., Schmidt, J.M. Anticancer Drug Des. (1998) [Pubmed]
  11. Dolastatin 15 binds in the vinca domain of tubulin as demonstrated by Hummel-Dreyer chromatography. Cruz-Monserrate, Z., Mullaney, J.T., Harran, P.G., Pettit, G.R., Hamel, E. Eur. J. Biochem. (2003) [Pubmed]
  12. The bcl-2 and p53 oncoproteins can be modulated by bryostatin 1 and dolastatins in human diffuse large cell lymphoma. Maki, A., Diwakaran, H., Redman, B., al-Asfar, S., Pettit, G.R., Mohammad, R.M., al-Katib, A. Anticancer Drugs (1995) [Pubmed]
  13. Diazonamide A and a synthetic structural analog: disruptive effects on mitosis and cellular microtubules and analysis of their interactions with tubulin. Cruz-Monserrate, Z., Vervoort, H.C., Bai, R., Newman, D.J., Howell, S.B., Los, G., Mullaney, J.T., Williams, M.D., Pettit, G.R., Fenical, W., Hamel, E. Mol. Pharmacol. (2003) [Pubmed]
  14. High-performance capillary electrophoresis measurement of dolastatin-10. Huie, W.R., Newman, R.A., Hutto, T., Madden, T. J. Chromatogr. B Biomed. Sci. Appl. (1997) [Pubmed]
  15. The dolastatins, a family of promising antineoplastic agents. Poncet, J. Curr. Pharm. Des. (1999) [Pubmed]
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