Danusertib

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 Specifications

CAS Number

[827318-97-8]

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.