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Product Details
Synonyms PHA-739358
Product Type Chemical


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

Click here for Original Manufacturer Product Datasheet
Our product description may differ slightly from the original manufacturers product datasheet.

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.
MSDS Download PDF
Product Specification Sheet
Datasheet Download PDF

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 References
  1. 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)
  2. 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)
  3. Splice Modulation Synergizes Cell Cycle Inhibition: A. Kelsey, et al.; ACS Chem. Biol. ahead of print (2020)
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