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Chemical Compound Review

ABT-100     4-[(2S)-2-(4-cyanophenyl)-2- hydroxy-2-(3...

Synonyms: ABT100, SureCN2731728, ABT 100, AC1O52UD, A-409100, ...
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Disease relevance of ABT 100


High impact information on ABT 100

  • RESULTS: ABT-100 inhibited proliferation of cells in vitro carrying oncogenic H-Ras (EJ-1 bladder; IC(50) 2.2 nmol/L), Ki-Ras (DLD-1 colon, MDA-MB-231 breast, HCT-116 colon, and MiaPaCa-2 pancreatic; IC(50) range, 3.8-9.2 nmol/L), and wild-type Ras (PC-3 and DU-145; IC(50), 70 and 818 nmol/L, respectively) as well as clonogenic potential [3].
  • PURPOSE: To evaluate the preclinical pharmacokinetics, antitumor efficacy, and mechanism of action of a novel orally active farnesyltransferase inhibitor, ABT-100 [3].
  • RESULTS: ABT-100 inhibited HepG2 and Huh7 cell growth as well as the invading ability of Huh7 on Matrigel [1].
  • Furthermore, ABT-100 inhibited Akt-dependent p27(Kip1) phosphorylation and this event was associated with increased levels of p27(Kip1) in the nucleus and reduced activity of the cyclin-dependent kinase 2 [1].
  • ABT-100 shows 70% to 80% oral bioavailability in mice [3].

Biological context of ABT 100


Anatomical context of ABT 100


Gene context of ABT 100


Analytical, diagnostic and therapeutic context of ABT 100

  • Treatment with 25, 50 and 100 mg/kg ABT-100 BID increased allograft mean survival time (MST) to 12.8+/-3 days, 13.5+/-5 days and 13.8+/-3 days, respectively (vs 6.5+/-3 days for controls, p<0.001 by log rank) [4].


  1. Farnesyltransferase inhibitor, ABT-100, is a potent liver cancer chemopreventive agent. Carloni, V., Vizzutti, F., Pantaleo, P. Clin. Cancer Res. (2005) [Pubmed]
  2. A protein farnesyltransferase inhibitor ameliorates disease in a mouse model of progeria. Fong, L.G., Frost, D., Meta, M., Qiao, X., Yang, S.H., Coffinier, C., Young, S.G. Science (2006) [Pubmed]
  3. Antitumor activity of orally bioavailable farnesyltransferase inhibitor, ABT-100, is mediated by antiproliferative, proapoptotic, and antiangiogenic effects in xenograft models. Ferguson, D., Rodriguez, L.E., Palma, J.P., Refici, M., Jarvis, K., O'Connor, J., Sullivan, G.M., Frost, D., Marsh, K., Bauch, J., Zhang, H., Lin, N.H., Rosenberg, S., Sham, H.L., Joseph, I.B. Clin. Cancer Res. (2005) [Pubmed]
  4. Potent farnesyltransferase inhibitor ABT-100 abrogates acute allograft rejection. Si, M.S., Ji, P., Lee, M., Kwok, J., Kusumoto, J., Naasz, E., Ng, S.C., Imagawa, D.K. J. Heart Lung Transplant. (2005) [Pubmed]
  5. A highly potent and selective farnesyltransferase inhibitor ABT-100 in preclinical studies. Gu, W.Z., Joseph, I., Wang, Y.C., Frost, D., Sullivan, G.M., Wang, L., Lin, N.H., Cohen, J., Stoll, V.S., Jakob, C.G., Muchmore, S.W., Harlan, J.E., Holzman, T., Walten, K.A., Ladror, U.S., Anderson, M.G., Kroeger, P., Rodriguez, L.E., Jarvis, K.P., Ferguson, D., Marsh, K., Ng, S., Rosenberg, S.H., Sham, H.L., Zhang, H. Anticancer Drugs (2005) [Pubmed]
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