ELR-510444

Catalog No.S3725 Batch:S372501

Technical Data

Formula	C₁₉H₁₆N₂O₂S₂
Molecular Weight	368.47	CAS No.	1233948-35-0
Solubility (25°C)*	In vitro	DMSO	73 mg/mL (198.11 mM)
		Ethanol	24 mg/mL (65.13 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or 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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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 (from reference)

Cell Assay:^{^[1]}	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.
Animal Study:^{^[1]}	Animal Models BALB/c nude mice Dosages 3, 6, and 12.5 mg/kg Administration s.c.

Cell Assay:^{^[1]}

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.

Animal Study:^{^[1]}

Animal Models
BALB/c nude mice
Dosages
3, 6, and 12.5 mg/kg
Administration
s.c.

References

[1] Risinger AL, et al. J Pharmacol Exp Ther. 2011, 336(3):652-60.

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SHIPPING AND STORAGE
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