Phthalazinone pyrazole

Phthalazinone pyrazole is a potent, selective, and orally active inhibitor of Aurora-A kinase with an IC50 of 0.031 μM. Phthalazinone pyrazole can arrests mitosis and subsequently inhibit tumor growth via apoptosis of proliferating cells. Phthalazinone pyrazole suppresses the epithelial-mesenchymal transition (EMT) during the differentiation of hepatocyte-like cells (HLCs) from human embryonic stem cells[1][2].

Product Specifications

CAS Number

[880487-62-7]

UNSPSC

12352005

Target

Apoptosis; Aurora Kinase; Mitosis

Type

Reference compound

Related Pathways

Apoptosis; Cell Cycle/DNA Damage; Epigenetics

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/phthalazinone-pyrazole.html

Purity

98.0

Solubility

DMSO : ≥ 11.11 mg/mL

Smiles

O=C1C2=CC=CC=C2C(NC3=NNC(C)=C3)=NN1C4=CC=CC=C4

Molecular Formula

C18H15N5O

Molecular Weight

317.34

References & Citations

[1]Prime ME, et al. Phthalazinone pyrazoles as potent, selective, and orally bioavailable inhibitors of Aurora-A kinase. J Med Chem. 2011;54 (1) :312-319. |[2]Choi YJ, et al. Phthalazinone Pyrazole Enhances the Hepatic Functions of Human Embryonic Stem Cell-Derived Hepatocyte-Like Cells via Suppression of the Epithelial-Mesenchymal Transition. Stem Cell Rev Rep. 2018;14 (3) :438-450.