ZM-447439

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

ZM-447439 是一种有效的、选择性的 Aurora A 和 Aurora B 双重抑制剂，IC50 分别为 110 和 130 nM。

ZM-447439 is a potent, selective dual Aurora A and Aurora B inhibitor with IC50 of 110 and 130 nM, respectively; prevents anaplastic thyroid cancer cell growth and tumorigenicity, inhibits the growth and tumorigenicity of a panel of ATC derived cell lines (CAL-62, 8305C, 8505C and BHT-101) with IC50 of 0.5-5 uM; ZM447439-treated cells exit mitosis with normal kinetics, accelerates first meiosis in mouse oocytes by overriding the spindle assembly checkpoint.Blood Cancer Discontinued.

Cells treated with ZM-447439 progress through interphase, enter mitosis normally, and assemble bipolar spindles. However, chromosome alignment, segregation, and cytokinesis all fail. ZM-447439 inhibits cell division and inhibit mitotic phosphorylation of histone H3. ZM-447439 prevents chromosome alignment and segregation. ZM-447439 compromises spindle checkpoint function. ZM-447439 inhibits kinetochore localization of BubR1, Mad2, and Cenp-E. Inhibition of Aurora kinase by ZM-447439 reduces histone H3 phosphorylation at Ser10 in Hep2 carcinoma cells. Multipolar spindles are induced in these ZM-treated G2/M-arrested cells with accumulation of 4N/8N DNA, similar to cells with genetically suppressed Aurora-B. ZM-447439 treatment induces cell apoptosis. ZM-447439 inhibition of Aurora kinase is potently in association with decrease of Akt phosphorylation at Ser473 and its substrates GSK3α/β phosphorylation at Ser21 and Ser9.

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ZM447439 | ZM 447439

Cell Cycle/DNA Damage

Aurora Kinase

Aurora A| Aurora B| MEK1| Lck| Src

Cancer

Blood cancer

331771-20-1

513.5875

C29H31N5O4

>98% (HPLC)

10 mM in DMSO

O=C(NC1=CC=C(NC2=C3C=C(OC)C(OCCCN4CCOCC4)=CC3=NC=N2)C=C1)C5=CC=CC=C5

Benzamide, N-[4-[[6-methoxy-7-[3-(4-morpholinyl)propoxy]-4-quinazolinyl]amino]phenyl]-

(-20℃)

With Ice Pack

≥ 2 years