Catalog Number: 3335
Alternate Names: TSU68, Orantinib
Chemical Name: 5-[1,2-Dihydro-2-oxo-3H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-propanoic acid
Biological Activity
ATP-competitive PDGFR, VEGF and FGFR inhibitor (IC50 values are 0.06, 2.43, 3.04 and > 100 μM at PDGFRβ, VEGFR2, FGFR1 and EGFR respectively). Inhibits proliferation of HUVEC and NIH3T3 cells in vitro (IC50 values are 0.41, 9.3 and 16.5 μM for VEGF, FGF and PDGF-stimulated growth respectively) and induces > 75% growth inhibition against a broad range of tumor types in vivo. Exhibits antiangiogenic, anti-inflammatory, antimetastatic and proapoptotic activity and is orally active.
Technical Data
  • M.Wt:
    310.35
  • Formula:
    C18H18N2O3
  • Solubility:
    Soluble to 100 mM in 1eq. NaOH and to 100 mM in DMSO
  • Purity:
    >99%
  • Storage:
    Store at RT
  • CAS No:
    252916-29-3
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. TSU68 prevents liver metastasis of colon cancer xenografts by modulating the premetastatic niche.
    Yamamoto M, Kikuchi H, Ohta M et al.
    Cancer Res.
  2. Design, synthesis, and evaluations of substituted 3-[(3- or 4-carboxyethylpyrrol-2-yl)methylidenyl]indolin-2-ones as inhibitors of VEGF, FGF, and PDGF receptor tyrosine kinases.
    Sun et al.
    J.Med.Chem., 1999;42:5120
  3. SU6668 is a potent antiangiogenic and antitumor agent that induces regression of established tumors.
    Laird et al.
    Cancer Res., 2000;60:4152
Citations:

The citations listed below are publications that use Tocris products. Selected citations for SU 6668 include:

1 Citations: Showing 1 - 1

  1. Feedback circuitry between miR-218 repression and RTK activation in glioblastoma.
    Authors: Mathew Et al.
    Mol Biol Cell 2015;8:ra42

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