FiVe1 

FiVe1 is a vimentin (VIM) inhibitor. FiVe1 binds to the rod domain of VIM, causing metaphase VIM disassembly and hyperphosphorylation at Ser56, ultimately leading to mitotic catastrophe, multinucleation, and loss of stemness. FiVe1 has anticancer activity against soft tissue sarcomas. FiVe1 increases the sensitivity of ovarian cancer to Cisplatin (HY-17394). FiVe1 can be used for researches of mesenchymal cancers (including breast cancer and soft tissue sarcoma) and ovarian cancers^[1][2][3].

IC50: VIM^[1]

FiVe1 (2 μM; 72 h) 选择性抑制 FOXC2-HMLER 细胞的生长，同时对 HMLER 细胞几乎没有毒性^[1]。
FiVe1 (250 nM) 导致 FOXC2-HMLER 细胞中的 VIM 丝状结构塌陷^[1]。
FiVe1 (多核试验：1 μM；多核试验：24 h) 分别抑制多种软组织肉瘤 (STS) 细胞系 (HT1080、SW684、RD、GCT、SW872、SW982) 的生长，并促进这些细胞系的多核化^[1]。
FiVe1 (72 h) 抑制 HUVEC 和人肺成纤维细胞 (HLF) 的生长，IC₅₀ 值为分别为 1.70 μM 和 2.32 μM^[1]。
FiVe1 抑制 HT-1080 纤维肉瘤细胞的生长，IC₅₀ 为 1.6 μM^[2]。
FiVe1 (0.2 μM；72 h) 显著提高 A2780 和 A2780cis 细胞对 Cisplatin (HY-17394) 的敏感性^[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

359.25

C₁₈H₁₆Cl₂N₄

932359-76-7

固体

Light yellow to brown

Room temperature in continental US; may vary elsewhere.

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• [1]. Michael J Bollong, et al. A vimentin binding small molecule leads to mitotic disruption in mesenchymal cancers. Proc Natl Acad Sci U S A. 2017 Nov 14;114(46):E9903-E9912.  [Content Brief]

  [2]. Martínez-Peña F, et al. Synthesis and biological evaluation of novel FiVe1 derivatives as potent and selective agents for the treatment of mesenchymal cancers. Eur J Med Chem. 2022 Nov 15;242:114638.  [Content Brief]

  [3]. Möltgen S, et al. Cisplatin Protein Binding Partners and Their Relevance for Platinum Drug Sensitivity. Cells. 2020 May 26;9(6):1322.  [Content Brief]