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Chemical Compound Review

CHEMBL9619     ethylN-[5-amino-8-(4- methylphenyl)-4,7,10...

Synonyms: AG-H-30507, NSC-341932, LS-48921, CTK5E9851, NSC341932, ...
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Disease relevance of CI 980


High impact information on CI 980

  • Although the interactions of CI 980 with microtubules in vitro are not very different from other drugs, it is a most potent cellular microtubule and mitotic inhibitor [1].
  • Inhibition of microtubules and cell cycle arrest by a new 1-deaza-7,8-dihydropteridine antitumor drug, CI 980, and by its chiral isomer, NSC 613863 [1].
  • CI-980 is a chemotherapeutic agent currently in Phase II trials that arrests cellular division by binding to tubulin [6].
  • CI-980 (NSC 613862) is one of a novel class of 1,2-dihydropyrido[3, 4-b]pyrazines that inhibits tubulin polymerization, presumably by binding to the colchicine binding site of tubulin [2].
  • Kinetics of association and dissociation of two enantiomers, NSC 613863 (R)-(+) and NSC 613862 (S)-(-) (CI 980), to tubulin [7].

Biological context of CI 980

  • 7. It is concluded that in guinea-pig papillary muscles, CI-980 produces a use-dependent inhibition of Vmax and a reverse use-dependent prolongation of the ventricular action potential, thus exhibiting class I and class III antiarrhythmic actions, respectively [8].
  • CI-980 is a synthetic mitotic inhibitor that binds to tubulin at the colchicine binding site and inhibits the polymerization of tubulin and blocks cell cycle progression in mitosis [4].
  • 6. The curve relating membrane potential and Vmax was shifted by CI-980 (10(-5) M) in the hyperpolarizing direction by 2.3 +/- 1.1 mV [8].
  • Because of its extensive tissue distribution in animals and its favorable activity against multidrug resistant (MDR)-cells compared with other mitotic inhibitors, such as vincristine, we examined the membrane transport properties of CI-980 [9].
  • In addition, induction of apoptosis in response to CI-980 correlates with the presence of a functional mitotic checkpoint and the extent of microtubule depolymerization [10].

Anatomical context of CI 980


Gene context of CI 980

  • CI-980 is a synthetic mitotic inhibitor that binds to the colchicine binding site of tubulin [13].
  • Urine samples must be pretreated with bovine serum albumin (BSA) to minimize the binding of CI-980 to glass and some plastics [14].
  • CI-980 and PD 080658, internal standard, were isolated from 2-ml samples of human plasma and urine by solid-phase extraction with Bond-Elut C18 cartridges [14].

Analytical, diagnostic and therapeutic context of CI 980


  1. Inhibition of microtubules and cell cycle arrest by a new 1-deaza-7,8-dihydropteridine antitumor drug, CI 980, and by its chiral isomer, NSC 613863. de Ines, C., Leynadier, D., Barasoain, I., Peyrot, V., Garcia, P., Briand, C., Rener, G.A., Temple, C. Cancer Res. (1994) [Pubmed]
  2. Phase I and pharmacological study of CI-980, a novel synthetic antimicrotubule agent. Rowinsky, E.K., Long, G.S., Noe, D.A., Grochow, L.B., Bowling, M.K., Sartorius, S.E., Donehower, R.C. Clin. Cancer Res. (1997) [Pubmed]
  3. Phase II trial of CI-980 in patients with disseminated malignant melanoma and no prior chemotherapy. A Southwest Oncology Group study. Whitehead, R.P., Unger, J.M., Flaherty, L.E., Eckardt, J.R., Taylor, S.A., Didolkar, M.S., Samlowski, W., Sondak, V.K. Investigational new drugs. (2001) [Pubmed]
  4. Phase II study of CI-980 (NSC 635370) in patients with previously treated advanced soft-tissue sarcomas. Patel, S.R., Burgess, M.A., Papadopolous, N.E., Sidhu, G., Gray, R., Plager, C., Jenkins, J., Benjamin, R.S. Investigational new drugs. (1998) [Pubmed]
  5. CI-980 in advanced melanoma and hormone refractory prostate cancer. Ryan, C.W., Shulman, K.L., Richards, J.M., Kugler, J.W., Sosman, J.A., Ansari, R.H., Vokes, E.E., Vogelzang, N.J. Investigational new drugs. (2000) [Pubmed]
  6. Neurotoxicity of CI-980, a novel mitotic inhibitor. Meyers, C.A., Kudelka, A.P., Conrad, C.A., Gelke, C.K., Grove, W., Pazdur, R. Clin. Cancer Res. (1997) [Pubmed]
  7. Kinetics of association and dissociation of two enantiomers, NSC 613863 (R)-(+) and NSC 613862 (S)-(-) (CI 980), to tubulin. Barbier, P., Peyrot, V., Dumortier, C., D'Hoore, A., Rener, G.A., Engelborghs, Y. Biochemistry (1996) [Pubmed]
  8. Electrophysiological effects of CI-980, a tubulin binding agent, on guinea-pig papillary muscles. Pérez, O., Valenzuela, C., Delpón, E., Tamargo, J. Br. J. Pharmacol. (1997) [Pubmed]
  9. Cellular transport of CI-980. Hook, K.E., Przybranowski, S.A., Leopold, W.R. Investigational new drugs. (1996) [Pubmed]
  10. Differential spindle assembly checkpoint response in human lung adenocarcinoma cells. Weitzel, D.H., Vandré, D.D. Cell Tissue Res. (2000) [Pubmed]
  11. Tubulin binding agent CI-980 has positive inotropic and local anesthetic actions. Chevalier, P., Kuznetsov, V., Robinson, R.B., Rosen, M.R. J. Cardiovasc. Pharmacol. (1994) [Pubmed]
  12. A phase II study of CI-980 in previously untreated extensive small cell lung cancer: an Ohio State University phase II research consortium study. Thomas, J.P., Moore, T., Kraut, E.H., Balcerzak, S.P., Galloway, S., Vandre, D.D. Cancer Invest. (2002) [Pubmed]
  13. A phase I trial and pharmacokinetic evaluation of CI-980 in patients with advanced solid tumors. Sklarin, N.T., Lathia, C.D., Benson, L., Grove, W.R., Thomas, S., Roca, J., Einzig, A.I., Wiernik, P.H. Investigational new drugs. (1997) [Pubmed]
  14. High-performance liquid chromatographic assay for CI-980, a novel 1-deaza-7,8-dihydropteridine anticancer agent, in human plasma and urine. Bullen, W.W., Whitfield, L.R., Walter, G.A., Brodfuehrer, J.I. J. Chromatogr. B, Biomed. Appl. (1995) [Pubmed]
  15. Simultaneous combination of microtubule depolymerizing and stabilizing agents acts at low doses. Garcia, P., Braguer, D., Carles, G., Briand, C. Anticancer Drugs (1995) [Pubmed]
  16. Determination of the anticancer agent CI-980 in plasma by achiral liquid chromatography on a Pirkle-type stationary phase. Markoglou, N., Wainer, I.W. J. Chromatogr. B Biomed. Sci. Appl. (1997) [Pubmed]
  17. Phase II trial of intravenous CI-980 (NSC 370147) in patients with metastatic colorectal carcinoma. Model for prospective evaluation of neurotoxicity. Pazdur, R., Meyers, C., Diaz-Canton, E., Abbruzzese, J.L., Patt, Y., Grove, W., Ajani, J. Am. J. Clin. Oncol. (1997) [Pubmed]
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