SU 6668

Biological Activity

SU 6668 is an 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

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. 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
2. SU6668 is a potent antiangiogenic and antitumor agent that induces regression of established tumors.
   Laird et al.
   Cancer Res., 2000;60:4152
3. TSU68 prevents liver metastasis of colon cancer xenografts by modulating the premetastatic niche.
   Yamamoto M, Kikuchi H, Ohta M, Kawabata T, Hiramatsu Y, Kondo K, Baba M, Kamiya K, Tanaka T, Kitagawa M, Konno H
   Cancer Res., 2008-12-01;68(23):9754-62.

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