SU 6668

Cat. No. 3335

SU 6668 C18H18N2O3 [252916-29-3]

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Alternative 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.

Certificate of Analysis / Product Datasheet / Safety Datasheet

References are publications that support the products' biological activity.

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

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

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.

If you know of a relevant reference for SU 6668 please let us know.

Citations are publications that use Tocris products. Selected citations for SU 6668 include:

Mathew et al (2015) Feedback circuitry between miR-218 repression and RTK activation in glioblastoma. Mol Biol Cell 8 ra42. PMID: 25943352.

Do you know of a great paper that uses SU 6668 from Tocris? If so please let us know.

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Keywords: SU 6668, supplier, FGFR, VEGFR, PDGFR, inhibitors, inhibits, Fibroblast, Growth, Factor, Receptors, Receptor, Tyrosine, Kinases, RTKs, Platelet, Derived, Vascular, Endothelial, KDR, Flt, SU6668, Tocris Bioscience, PDGFR Inhibitor products

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