Phthalazinone pyrazole is a potent, selective, and orally active inhibitor of Aurora-A kinase with anIC₅₀of 0.031 μM. Phthalazinone pyrazole can arrests mitosis and subsequently inhibit tumor growth viaapoptosisof 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].

Phthalazinone pyrazole (1 and 10 μM; 30 hours) enhances the proliferative capacity of HLCs^[2].
Phthalazinone pyrazole (1, 10, and 100 μM; 5 days) enhances hepatic morphological changes in differentiated HLCs without cytotoxicity^[2].
Phthalazinone pyrazole (1 and 10 μM; 5 and 17 days) suppresses the EMT and induced maturation of HLCs through the inhibition of the AKT signaling pathway by the off target effect with concomitant upregulation of HNF4α rather than direct inhibition of Aurora-A. The result is confirmed by western blot and qPCR^[2].

317.34

Solid

C₁₈H₁₅N₅O

880487-62-7

Room temperature in continental US; may vary elsewhere.

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

DMSO : ≥ 11.11 mg/mL(35.01 mM)

*"≥" means soluble, but saturation unknown.

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