CFI-400437

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

CFI-400437 

CFI-400437 吲哚醌衍生的、ATP 竞争性的 PLK4 抑制剂 (IC50 值为 0.6 nM)。

CFI-400437

CFI-400437 Chemical Structure

CAS No. : 1169211-37-3

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生物活性

CFI-400437 is an indolinone-derived, ATP-competitive kinase inhibitor with high selectivity for PLK4 (IC50 of 0.6 nM)[1].

体外研究
(In Vitro)

CFI-400437 is a potent inhibitor of MCF-7, MDA-MB-468 and MDA-MB231 cell growth[1].
CFI-400437 inhibits Aurora A, Aurora B, KDR and FLT-3 with IC50s of 0.37, 0.21, 0.48, and 0.18 µM, respectively, i.e. two orders of magnitude higher than its IC50 of 0.6 nM against PLK4[1].
CFI-400437 inhibits both AURKB and AURKC at concentrations <15 nm[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

CFI-400437 (25 mg/kg, ip, once daily for 21 d) exhibits antitumor activity against MDA-MB-468 breast cancer mouse xenograft model[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

492.57

Formula

C29H28N6O2
CAS 号

1169211-37-3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Radoslaw Laufer, et al. The discovery of PLK4 inhibitors: (E)-3-((1H-Indazol-6-yl)methylene)indolin-2-ones as novel antiproliferative agents. J Med Chem. 2013 Aug 8;56(15):6069-87.

    [2]. Amreena Suri, et al. Evaluation of Protein Kinase Inhibitors with PLK4 Cross-Over Potential in a Pre-Clinical Model of Cancer. Int J Mol Sci. 2019 Apr 29;20(9):2112.

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