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ELR510444

Catalog No.
B5870
Novel microtubule disruptor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$83.00
In stock
5mg
$79.00
In stock
10mg
$119.00
In stock
25mg
$231.00
In stock
For scientific research use only and should not be used for diagnostic or medical purposes.

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

Microtubules are involved in nucleic and cell organization, division of intracellular structure, and intracellular transport, as well as ciliary and flagellar motility. Microtubule-targeting agents are some of the most effective chemotherapeutic drugs used in the clinic today. ELR510444 is a novel microtubule disruptor with multiple mechanisms of action.

In vitro: ELR510444 has potent microtubuledisrupting activity, causing a loss of intracellular microtubules and the formation of aberrant mitotic spindles and leading to mitotic arrest and apoptosis of cancer cells. ELR510444 inhibited cell proliferation, inhibited the rate and extent of purified tubulin assembly potently, and displaced colchicine from tubulin, revealing that the drug directly interacts with tubulin at the colchicine-binding site [1].

In vivo: ELR510444 also shows potent antitumor activity in the MDA-MB-231 xenograft model with at least a 2-fold therapeutic window [1].

Clinical trial: Up to now, ELR510444 is still in the preclinical development stage.

Reference:
[1] Risinger AL, Westbrook CD, Encinas A, Mülbaier M, Schultes CM, Wawro S, Lewis JD, Janssen B, Giles FJ, Mooberry SL.  ELR510444, a novel microtubule disruptor with multiple mechanisms of action. J Pharmacol Exp Ther. 2011 Mar;336(3):652-60.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt368.47
Cas No.1233948-35-0
FormulaC19H16N2O2S2
Solubilityinsoluble in H2O; insoluble in EtOH; ≥11.9 mg/mL in DMSO
Chemical NameN-(5-(5-cyanothiophen-2-yl)-2-methylphenyl)-4-methylbenzenesulfonamide
SDFDownload SDF
Canonical SMILESCC1=CC=C(S(NC2=C(C=CC(C3=CC=C(S3)C#N)=C2)C)(=O)=O)C=C1
Shipping ConditionSmall Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips We do not recommend long-term storage for the solution, please use it up soon.

Quality Control

Chemical structure

ELR510444