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SynKinase
AT9283
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| Product Details | |
|---|---|
| Synonyms | AT-9283 |
| Product Type | Chemical |
| Properties | |
| Formula | C19H23N7O2 |
| MW | 381.4 |
| CAS | 896466-04-9 |
| Purity Chemicals | ≥95% |
| Appearance | Solid. |
| Solubility | Soluble in DMSO or ethanol. |
| Declaration | Manufactured by SynKinase. |
| Other Product Data |
Target: Aurora A | Kinase Group: Other | Substrate: Serine-Threonine Click here for Original Manufacturer Product Datasheet Our product description may differ slightly from the original manufacturers product datasheet. |
| InChi Key | LOLPPWBBNUVNQZ-UHFFFAOYSA-N |
| Shipping and Handling | |
| Shipping | AMBIENT |
| Short Term Storage | +4°C |
| Long Term Storage | -20°C |
| Use/Stability | Stable for at least 2 years after receipt when stored at -20°C. |
| Documents | |
| MSDS |
 Download PDF |
| Product Specification Sheet | |
| Datasheet |
Download PDF |
Description
Aurora kinases play a key role in the regulation of mitosis and in recent years have become attractive targets for the treatment of cancer. AT9283 is a powerful inhibitor of Aurora A and B kinases as well as several other important kinases including JAK2 and Abl (T315I). AT9283 has also been shown effective in mouise xenograft models and has been studied as a possible clinical candidate. Effective IC(50) doses for Aurora kinases are in the low 2-3nM range, and inhibition of a number of other kinases including JAK2 has been reported at 1-10nM.
Product References
- Fragment-based discovery of the pyrazol-4-yl urea (AT9283), a multitargeted kinase inhibitor with potent aurora kinase activity: S. Howard, et al.; J. Med. Chem. 52, 379 (2009)
- Discovery and development of aurora kinase inhibitors as anticancer agents: J.R. Pollard & M. Mortimore; J. Med. Chem. 52, 2629 (2009)
- Design, synthesis, quantum chemical studies and biological activity evaluation of pyrazole-benzimidazole derivatives as potent Aurora A/B kinase inhibitors: Y. Zheng, et al.; Bioorg. Med. Chem. Lett. 23, 3523 (2013)