Catalog Number: 6265
Chemical Name: 4-[2-[4-[(11R)-3,10-Dibromo-8-chloro-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl]-1-piperidinyl]-2-oxoethyl]-1-piperidinecarboxamide
Biological Activity
Potent farnesyl transferase inhibitor (IC50 = 1.9 nM). Inhibits farnesylation of RAS. Also inhibits Pgp transport (IC50 < 3 μM) and increases potency and anticancer activity when used in conjunction with cytotoxic Pgp substrates. Inhibits neovascularization by affecting cell motility. Orally bioavailable.
Technical Data
  • M.Wt:
  • Formula:
  • Solubility:
    Soluble to 10 mM in DMSO with gentle warming
  • Purity:
  • Storage:
    Store at -20°C
  • CAS No:
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. Phosphorylation of FADD by the kinase CK1α promotes KRASG12D-induced lung cancer.
    Bowman et al.
    Sci.Signal., 2015;8
  2. A high throughput phenotypic screening reveals compounds that counteract premature osteogenic differentiation of HGPS iPS-derived mesenchymal stem cells.
    Lo Cicero et al.
    Sci.Rep., 2016;6:34798
  3. Lonafarnib is a potential inhibitor for neovascularization.
    Sun et al.
    PLoS One., 2015;10:e0122830
  4. The farnesyl protein transferase inhibitor SCH66336 is a potent inhibitor of MDR1 product P-glycoprotein.
    Wang et al.
    Cancer.Res., 2001;61:7525
  5. Combination therapy with the farnesyl protein transferase inhibitor SCH66336 and SCH58500 (p53 adenovirus) in preclinical cancer models.
    Nielsen et al.
    Cancer Res., 1999;59:5896
  6. Farnesyltransferase and geranylgeranyltransferase I: structures, mechanism, inhibitors and molecular modeling.
    Shen et al.
    Drug Discov.Today., 2015;20:267

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