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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.
Solubility Data for SU 6668
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| 1eq. NaOH | 31.03 | 100 | |
| DMSO | 31.03 | 100 |
Preparing Stock Solutions for SU 6668
The following data is based on the product molecular weight 310.35. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 3.22 mL | 16.11 mL | 32.22 mL |
| 5 mM | 0.64 mL | 3.22 mL | 6.44 mL |
| 10 mM | 0.32 mL | 1.61 mL | 3.22 mL |
| 50 mM | 0.06 mL | 0.32 mL | 0.64 mL |
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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
If you know of a relevant reference for SU 6668, please let us know.
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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:
Mathew et al (2015) Feedback circuitry between miR-218 repression and RTK activation in glioblastoma. Mol Biol Cell 8 ra42 PMID: 25943352
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
Do you know of a great paper that uses SU 6668 from Tocris? Please let us know.
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Cancer Research Product Guide
A collection of over 750 products for cancer research, the guide includes research tools for the study of:
- Cancer Metabolism
- Epigenetics in Cancer
- Receptor Signaling
- Cell Cycle and DNA Damage Repair
- Angiogenesis
- Invasion and Metastasis
Angiogenesis in Cancer Poster
Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the pathogenesis of angiogenesis in cancer, as well as some of the main angiogenesis therapeutic targets.