ELR-510444

Catalog No.S3725

ELR-510444 Chemical Structure

Molecular Weight(MW): 368.47

ELR-510444 is a novel microtubule disruptor with potential antivascular effects and in vivo antitumor efficacy, causing a loss of cellular microtubules and the formation of aberrant mitotic spindles and leading to mitotic arrest and apoptosis of cancer cells.

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Biological Activity

Description ELR-510444 is a novel microtubule disruptor with potential antivascular effects and in vivo antitumor efficacy, causing a loss of cellular microtubules and the formation of aberrant mitotic spindles and leading to mitotic arrest and apoptosis of cancer cells.
Targets
Microtubule [1]
()
In vitro

ELR510444 has potent microtubule-disrupting activity, causing a loss of cellular microtubules and the formation of aberrant mitotic spindles and leading to mitotic arrest and apoptosis of cancer cells. ELR510444 potently inhibits cell proliferation with an IC(50) value of 30.9 nM in MDA-MB-231 cells, inhibits the rate and extent of purified tubulin assembly, and displaces colchicine from tubulin, indicating that the drug directly interacts with tubulin at the colchicine-binding site. ELR510444 is not a substrate for the P-glycoprotein drug transporter and retains activity in βIII-tubulin-overexpressing cell lines, suggesting that it circumvents both clinically relevant mechanisms of drug resistance to this class of agents[1].

In vivo ELR510444 shows potent antitumor activity in the MDA-MB-231 xenograft model. A low concentration of ELR510444 (30 nM) rapidly alters endothelial cell shape[1].

Protocol

Cell Research:[1]
+ Expand
  • Cell lines: 2H-11 tumor endothelial cells
  • Concentrations: 1-100 nM
  • Incubation Time: 1 h
  • Method: 2H-11 cells are plated on glass coverslips and allowed to attach and grow for 24 h. Drugs are then added for 1 h, and cells are fixed with paraformaldehyde and permeabilized with Triton X-100. F-Actin and DNA are stained with tetramethylrhodamine B isothiocyanate-conjugated phalloidin and DAPI, respectively.
    (Only for Reference)
Animal Research:[1]
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  • Animal Models: BALB/c nude mice
  • Formulation: 10% DMSO with 10% Cremophor in water.
  • Dosages: 3, 6, and 12.5 mg/kg
  • Administration: s.c.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 73 mg/mL (198.11 mM)
Ethanol 24 mg/mL (65.13 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 368.47
Formula

C19H16N2O2S2

CAS No. 1233948-35-0
Storage powder
in solvent
Synonyms N/A

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID