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]