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) selectively inhibits the growth of FOXC2-HMLER cells while showing little toxicity to HMLER cells^[1].
FiVe1 (250 nM) results in a collapsed VIM filamentous structure in FOXC2-HMLER cells^[1].
FiVe1 (1 μM for multinucleation test; 24 h for multinucleation test) inhibits the growth of multiple soft tissue sarcoma (STS) cell lines (HT1080, SW684, RD, GCT, SW872, SW982) and promotes multinucleation in these cell lines, respectively^[1].
FiVe1 (72 h) inhibits the growth of HUVECs and human lung fibroblasts (HLFs), with IC₅₀ values of 1.70 μM and 2.32 μM, respectively^[1].
FiVe1 inhibits the growth of HT-1080 fibrosarcoma cells, with an IC₅₀ of 1.6 μM^[2].
FiVe1 (0.2 μM; 72 h) significantly sensitizes both A2780 and A2780cis cells towards Cisplatin (HY-17394)^[3].

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

359.25

C₁₈H₁₆Cl₂N₄

932359-76-7

Solid

Light yellow to brown

ClC1=CC(N2CCN(C3=C4C=CC=C(Cl)C4=NN=C3)CC2)=CC=C1

Room temperature in continental US; may vary elsewhere.

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

• [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]