Chemical Name: 5-[1,2-Dihydro-2-oxo-3H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-propanoic acid
Biological ActivitySU 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.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
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.
SU6668 is a potent antiangiogenic and antitumor agent that induces regression of established tumors.
Laird et al.
Cancer Res., 2000;60:4152
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.
Citations for SU 6668
The citations listed below are publications that use Tocris products. Selected citations for SU 6668 include:
2 Citations: Showing 1 - 2
Chemical inhibition reveals differential requirements of signaling pathways in krasV12- and Myc-induced liver tumors in transgenic zebrafish.
Authors: Yan Et al.
Sci Rep 2017;7:45796
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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