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- Molecular Target
- Tyrosine Kinase
- PDGFR family
- SU6668 (Orantinib) | KDR/FGFR/PDGFR inhibitor
Product Description
SU-6668 (TSU-68) is an ATP-competitive, oxindole-based inhibitor of Flk-1/KDR, PDGFRb, and FGFR1 phosphorylation with Ki values of 2.1, 0.008, and 1.2 uM, respectively. [1] At these inhibitory levels, it was shown that SU-6668 induces antiangiogenic and proapoptotic effects in vivo. [2, 3]. Oral administration of SU6668 induced tumor regression in A431, PC-3, NCI-HT29, and Colo205 cell lines, and tumor stasis in SF767T glioma and NCI-H460 cell lines. [2]
In human myeloid leukemia cell lines and acute myeloid leukemia blasts, SU6668 was shown to inhibit the stem cell factor-induced phosphorylation of c-kit and ERK1/2 and induced apoptosis. [4]
Technical information:
| Chemical Formula: | C18H18N2O3 | |
| CAS #: | 252916-29-3 | |
| Molecular Weight: | 310.35 | |
| Purity: | >98% | |
| Appearance: | Orange | |
| Chemical Name: | (Z)-3-(2,4-dimethyl-5-((2-oxoindolin-3-ylidene)methyl)-1H-pyrrol-3-yl)propanoic acid | |
| Solubility: | Up to 100 mM in DMSO | |
| Synonyms: | SU6668, SU-6668, Orantinib, TSU 68 |
Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.
Reference:
| 1. | Laird et al., SU6668 is a potent antiangiogenic and antitumor agent that induces regression of established tumors. Cancer Res. 2000, 60, 4152-4160. Pubmed ID: 10945623 |
| 2. | Laird et al., SU6668 inhibits Flk-1/KDR and PDGFRbeta in vivo, resulting in rapid apoptosis of tumor vasculature and tumor regression in mice. FASEB, 2002, 16(7), 681-690. Pubmed ID: 11978732 |
| 3. | Marzola et al., In vivo assessment of antiangiogenic activity of SU6668 in an experimental colon carcinoma model. Clin. Cancer Res. 2004, 10, 739-750. Pubmed ID: 14760097 |
| 4. | Smolich et al., The antiangiogenic protein kinase inhibitors SU5416 and SU6668 inhibit the SCF receptor (c-kit) in a human myeloid leukemia cell line and in acute myeloid leukemia blasts. Blood, 2001, 97, 1413-1421. Pubmed ID: 11978732 |
Other Information:
Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.
