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SynKinase
Danusertib
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Specifications / Handling
| Product Details | |
|---|---|
| Synonyms | PHA-739358 |
| Product Type | Chemical |
| Properties | |
| Formula |
C26H30N6O3 |
| MW | 474.6 |
| CAS | 827318-97-8 |
| Purity Chemicals | ≥95% |
| Appearance | Solid. |
| Solubility | Soluble in DMSO or ethanol. |
| Declaration | Manufactured by SynKinase. |
| Other Product Data |
Target: Abl - Aurora A - BCR - FGFR | Kinase Group: Other | Substrate: Serine-Threonine |
| InChi Key | XKFTZKGMDDZMJI-HSZRJFAPSA-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 |
Scientific Background Information
Product Description
Aurora kinases are key regulators of protein phosphorylation during mitosis, and these serine/threonine kinases interact with other cellular proteins to help control chromosome assembly and segregation during mitosis. Aurora kinases are often highly expressed in malignancies and solid tumors. Danusertib (PHA-739358) is a small molecule pan- Aurora kinase inhibitor that also has activity against other cancer-relevant kinases such as Bcr-Abl tyrosine kinase. Other off target effects of danusertib include inhibition of receptor tyrosine kinases such as FGFR-1, and TrkA. Danusertib demonstrates nanomolar IC(50) values for the Aurora kinases all under 100nM and it also demonstrates potent anti-proliferation effects in cell proliferation assays with IC(50) values ranging from 20nM for A2780 cells to <200nM.
Product-specific References
- 1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazoles: identification of a potent Aurora kinase inhibitor with a favorable antitumor kinase inhibition profile: D. Fancelli, et al.; J. Med. Chem. 49, 7247 (2006)
- Targeting aurora kinases with danusertib (PHA-739358) inhibits growth of liver metastases from gastroenteropancreatic neuroendocrine tumors in an orthotopic xenograft model: K. Fraedrich, et al.; Clin. Cancer Res. 18, 4621 (2012)
- Splice Modulation Synergizes Cell Cycle Inhibition: A. Kelsey, et al.; ACS Chem. Biol. ahead of print (2020)
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