Home Cytoskeletal Signaling Microtubule Associated inhibitor ELR-510444 For research use only.

ELR-510444

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.

ELR-510444 Chemical Structure

ELR-510444 Chemical Structure

CAS: 1233948-35-0

Purity & Quality Control

Batch: S372501 DMSO] 73 mg/mL] false] Ethanol] 24 mg/mL] false] Water] Insoluble] false Purity: 98.64%
98.64

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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
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].
Cell Research 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.
In Vivo
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].
Animal Research Animal Models BALB/c nude mice
Dosages 3, 6, and 12.5 mg/kg
Administration s.c.

Chemical Information & Solubility

Molecular Weight 368.47 Formula

C19H16N2O2S2
CAS No. 1233948-35-0 SDF Download ELR-510444 SDF
Smiles CC1=CC=C(C=C1)S(=O)(=O)NC2=C(C=CC(=C2)C3=CC=C(S3)C#N)C
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 73 mg/mL ( (198.11 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 24 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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