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SU 6668

Cat. No. 3335

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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.

Resources

Certificate of Analysis / Safety Data Sheet

Certificate of Analysis: View current batch

Safety Data Sheet: View Safety Data Sheet

References

Sun et al (1999) 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. J.Med.Chem. 42 5120. PMID: 10602697.

Laird et al (2000) SU6668 is a potent antiangiogenic and antitumor agent that induces regression of established tumors. Cancer Res. 60 4152. PMID: 10945623.

Yamamoto et al (2008) TSU68 prevents liver metastasis of colon cancer xenografts by modulating the premetastatic niche. Cancer Res. 68 9754. PMID: 19047154.

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