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SU 6668
- TSU 68 - Orantinib
- Soluble in 0.1N NaOH(aq) and DMSO
- MF: C18H18N2O3
- MW: 310.35
Description
SU 6668 is an ATP-competitive, orally bioavailable receptor tyrosine kinase inhibitor targeting PDGFR, VEGFR and FGFR signaling.
PDGF, VEGF and FGF receptors regulate tumor angiogenesis, stromal signaling, endothelial proliferation and tissue remodeling. SU 6668 is useful for studying multi-RTK pathway inhibition and angiogenesis-dependent cancer biology.
Key Features
- Multi-target RTK inhibitor
- Reported IC50 values include 0.06 μM for PDGFRβ, 2.43 μM for VEGFR2 and 3.04 μM for FGFR1
- Shows weak activity against EGFR in reported assays
- Orally bioavailable angiogenesis-pathway research compound
Applications
- PDGFR, VEGFR and FGFR signaling studies
- Angiogenesis and endothelial proliferation assays
- Tumor-stromal interaction models
- RTK selectivity and pathway-inhibition profiling
More Information
| Parent CAS No. | 252916-29-3 |
|---|---|
| Chemical Name | 3-(2,4-dimethyl-5-((2-oxoindolin-3-ylidene)methyl)-1H-pyrrol-3-yl)propanoic acid |
| SMILES | N1C(/C=C2/C3=C(NC/2=O)C=CC=C3)=C(C)C(CCC(O)=O)=C1C |
| MFCD | N.A. |
| InChi | InChI=1S/C18H18N2O3/c1-10-12(7-8-17(21)22)11(2)19-16(10)9-14-13-5-3-4-6-15(13)20-18(14)23/h3-6,9,19H,7-8H2,1-2H3,(H,20,23)(H,21,22)/b14-9- |
| InChiKey | NHFDRBXTEDBWCZ-ZROIWOOFSA-N |
| CID | 5329099 |
| Short Description | RTK inhibitor |
References
- L Sun et al. 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. 1999, 42(25), 5120-5130.
- AD Laird et al. SU6668 is a potent antiangiogenic and antitumor agent that induces regression of established tumors. Cancer Res. 2000, 60(15), 4152-4160.
- M Toi et al. A multicenter phase II study of TSU-68, an oral multiple tyrosine kinase inhibitor, in combination with docetaxel in metastatic breast cancer patients with anthracycline resistance. Breast Cancer. 2014, 21(1), 20-27.
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