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Litronesib

Chemical Structure : Litronesib

CAS No.: 910634-41-2

Litronesib (LY2523355, LY-2523355)

Catalog No.: PC-27673Not For Human Use, Lab Use Only.

Litronesib ((R)-Litronesib, LY2523355) is a potent, selective and allosteric inhibitor of mitosis-specific kinesin Eg5 (Kif11, Kinesin Spindle Protein, KSP), inhibits microtubule (MT)-stimulated Eg5 ATPase activity with IC50 of 26 nM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Litronesib ((R)-Litronesib, LY2523355) is a potent, selective and allosteric inhibitor of mitosis-specific kinesin Eg5 (Kif11, Kinesin Spindle Protein, KSP), inhibits microtubule (MT)-stimulated Eg5 ATPase activity with IC50 of 26 nM.
Litronesib ((R)-Litronesib, LY2523355) kills cancer cells during mitotic arrest, causes a dose-dependent increase of cells with 4N DNA content.
Litronesib ((R)-Litronesib, LY2523355) also inhibits Eg5 localization to the mitotic spindle.
Litronesib ((R)-Litronesib, LY2523355) shows potent, broad-spectrum anticancer activity in vitro at low concentrations (IC50 values ranging from 0.4 nM to14 nM) against a panel of 21 cancer cell lines, SAC has an essential role in mitotic arrest and subsequent cell killing by Litronesib.
Litronesib ((R)-Litronesib, LY2523355) has broad-spectrum antitumor activity in vivo, which is is associated with mitotic arrest and death of cancer cells.

Physicochemical Properties

M.Wt 511.70
Formula C23H37N5O4S2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(R)-N-(5-(((2-(Ethylamino)ethyl)sulfonamido)methyl)-5-phenyl-4-pivaloyl-4,5-dihydro-1,3,4-thiadiazol-2-yl)pivalamide

References

1. Ye XS, et al. Mol Cancer Ther. 2015 Nov;14(11):2463-72.

2. Wakui H, et al. Cancer Chemother Pharmacol. 2014 Jul;74(1):15-23.

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