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Submit ReviewSU 6668
Description: PDGFR, VEGFR and FGFR inhibitor
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
Purity: ≥99% (HPLC)
Biological Activity for SU 6668
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 for SU 6668
| M. Wt | 310.35 |
| Formula | C18H18N2O3 |
| Storage | Store at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 252916-29-3 |
| PubChem ID | 5329099 |
| InChI Key | NHFDRBXTEDBWCZ-ZROIWOOFSA-N |
| Smiles | O=C2NC1=CC=CC=C1/C2=C/C3=C(C)C(CCC(O)=O)=C(C)N3 |
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.
Product Datasheets for SU 6668
References for SU 6668
References are publications that support the biological activity of the product.
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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Keywords: SU 6668, SU 6668 supplier, FGFR, VEGFR, PDGFR, inhibitors, inhibits, Fibroblast, Growth, Factor, Receptors, Receptor, Tyrosine, Kinases, RTKs, Platelet, Derived, Vascular, Endothelial, KDR, Flt, SU6668, TSU68, Orantinib, 3335, Tocris Bioscience
2 Citations for SU 6668
Citations are publications that use Tocris products. Selected citations for SU 6668 include:
Yan et al (2017) Chemical inhibition reveals differential requirements of signaling pathways in krasV12- and Myc-induced liver tumors in transgenic zebrafish. Sci Rep 7 45796 PMID: 28378824
Mathew et al (2015) Feedback circuitry between miR-218 repression and RTK activation in glioblastoma. Mol Biol Cell 8 ra42 PMID: 25943352
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Angiogenesis in Cancer Poster
This poster summarizes the pathogenesis of angiogenesis in cancer, as well as some of the main angiogenesis therapeutic targets.