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SU6668 (Orantinib) | KDR/FGFR/PDGFR inhibitor

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Price:
$89.00
Catalog #:
C7866-5
Quantity:


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.

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