Home Cytoskeletal Signaling Microtubule Associated inhibitor ELR-510444

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ELR-510444 Microtubule Associated inhibitor

Cat.No.S3725

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 Microtubule Associated inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 368.47

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Quality Control

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

Solubility

In vitro
Batch:

DMSO : 73 mg/mL (198.11 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 24 mg/mL

Water : Insoluble

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In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Chemical Information, Storage & Stability

Molecular Weight 368.47 Formula

C19H16N2O2S2

 Storage (From the date of receipt)
CAS No. 1233948-35-0 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CC1=CC=C(C=C1)S(=O)(=O)NC2=C(C=CC(=C2)C3=CC=C(S3)C#N)C

Mechanism of Action

Targets/IC50/Ki
Microtubule
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.
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.
References

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