A-259745

A-259745 is an orally active antimitotic agent that binds to the colchicine-binding site of tubulin. A-259745 exhibits potent in vitro cytotoxic activity against both multi-drug-resistant and non-multi-drug-resistant cancer cell lines, with ED50 values of 0.018 μM against HCT-15 and 0.028 μM against NCI-H460 cell lines. A-259745 inhibits tubulin polymerization, disrupts the dynamic equilibrium of the mitotic spindle, arrests dividing cells in metaphase, and subsequently induces apoptosis. A-259745 shows dose-dependent antitumor efficacy in murine tumor models. A-259745 can be used for the study of cancer[1].

Product Specifications

CAS Number

[256934-83-5]

Product Name Alternative

A-289099

UNSPSC

12352005

Target

Apoptosis; Microtubule/Tubulin

Related Pathways

Apoptosis; Cell Cycle/DNA Damage; Cytoskeleton

Field of Research

Cancer

Smiles

CN1C=CC2=C1C=CC(C3=NCC(C4=CC(OC)=C(OC)C(OC)=C4)O3)=C2

Molecular Formula

C21H22N2O4

Molecular Weight

366.41

References & Citations

[1]Szczepankiewicz BG, et al. New antimitotic agents with activity in multi-drug-resistant cell lines and in vivo efficacy in murine tumor models. J Med Chem. 2001 Dec 6;44 (25) :4416-30.