Phthalazinone pyrazole 是强效、选择性和口服生物可利用的 AuRORa-A 激酶抑制剂，IC50值为 0.031 μM。它抑制人胚胎干细胞向肝细胞样细胞分化过程中的上皮间质转化。它还可阻止有丝分裂并随后通过增殖细胞的凋亡抑制肿瘤生长。

Phthalazinone pyrazole is potent, selective, and orally bioavailable inhibitor of Aurora-A kinase. Aurora-A is overexpressed in a variety of tumor types and displays oncogenic activity.

Phthalazinone pyrazole potently inhibited the activity of Aurora A kinase with an IC50 of 31 nM. It showed no inhibitory effect on Aurora B kinase at doses up to 100 μM. Phthalazinone pyrazole inhibited the proliferation of HCT116, Colo205, and MCF-7 cells with IC50 values of 7.8, 2.9, and 1.6 μM, respectively [1].

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C18H15N5O

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DMSO:10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years