Danusertib

• Description :

  Danusertib is a pyrrolo-pyrazole and aurora kinase inhibitor with IC50 of 13, 79, and 61 nM for Aurora A, B, and C, respectively.

• Product Name Alternative :

  PHA-739358

• UNSPSC :

  12352005

• Hazard Statement :

  H302, H315, H319, H335

• Target :

  Aurora Kinase; Autophagy

• Type :

  Reference compound

• Related Pathways :

  Autophagy; Cell Cycle/DNA Damage; Epigenetics

• Applications :

  Cancer-Kinase/protease

• Field of Research :

  Cancer

• Assay Protocol :

  https://www.medchemexpress.com/Danusertib.html

• Purity :

  99.44

• Solubility :

  DMSO : 50 mg/mL (ultrasonic)

• Smiles :

  O=C(N1CC2=C(NN=C2NC(C3=CC=C(N4CCN(CC4)C)C=C3)=O)C1)[C@@H](C5=CC=CC=C5)OC

• Molecular Formula :

  C26H30N6O3

• Molecular Weight :

  474.55

• Precautions :

  H302, H315, H319, H335

• References & Citations :

  [1]Zi D, et al. Danusertib Induces Apoptosis, Cell Cycle Arrest, and Autophagy but Inhibits Epithelial to Mesenchymal Transition Involving PI3K/Akt/mTOR Signaling Pathway in Human Ovarian Cancer Cells. Int J Mol Sci. 2015 Nov 13;16 (11) :27228-51.|[2]Gontarewicz A, et al. Simultaneous targeting of Aurora kinases and Bcr-Abl kinase by the small molecule inhibitor PHA-739358 is effective against imatinib-resistant BCR-ABL mutations including T315I. Blood. 2008 Apr 15;111 (8) :4355-64.|[3]Fraedrich K, et al. Targeting Aurora Kinases with Danusertib (PHA-739358) Inhibits Growth of Liver Metastases from Gastroenteropancreatic Neuroendocrine Tumors in an Orthotopic Xenograft Model. Clin Cancer Res. 2012 Sep 1;18 (17) :4621-32. Epub 2012 Jul 2.

• Shipping Conditions :

  Room Temperature

• Storage Conditions :

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category :

  Reference compound1

• Clinical Information :

  Phase 2

• Isoform :

  Aurora A; Aurora B; Aurora C

• CAS Number :

  [827318-97-8]