Lexibulin

Lexibulin (CYT-997) is a potent and orally active tubulin polymerisation inhibitor with IC50s of 10-100 nM in cancer cell lines; with potent cytotoxic and vascular disrupting activity in vitro and in vivo[1][2]. Lexibulin induces cell apoptosis and induces mitochondrial ROS generation in GC cells[3].

Product Specifications

CAS Number

[917111-44-5]

Product Name Alternative

CYT-997

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Apoptosis; Microtubule/Tubulin; Reactive Oxygen Species (ROS)

Type

Reference compound

Related Pathways

Apoptosis; Cell Cycle/DNA Damage; Cytoskeleton; Immunology/Inflammation; Metabolic Enzyme/Protease; NF-κB

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/Lexibulin.html

Concentration

10mM

Purity

99.10

Solubility

DMSO : ≥ 100 mg/mL

Smiles

CCC[C@H](NC1=C(C)C=NC(C2=CC=C(NC(NCC)=O)C(OC)=C2)=N1)C3=CN=CC=C3

Molecular Formula

C24H30N6O2

Molecular Weight

434.53

Precautions

H302, H315, H319, H335

References & Citations

[1]Burns CJ, et al. CYT997: a novel orally active tubulin polymerization inhibitor with potent cytotoxic and vascular disrupting activity in vitro and in vivo. Mol Cancer Ther. 2009 Nov;8 (11) :3036-45.|[2]Monaghan K, et al. CYT997 causes apoptosis in human multiple myeloma. Invest New Drugs. 2011 Apr;29 (2) :232-8.|[3]Ya Cao, wt al. Mitochondrial ROS Accumulation Inhibiting JAK2/STAT3 Pathway Is a Critical Modulator of CYT997-induced Autophagy and Apoptosis in Gastric Cancer. J Exp Clin Cancer Res. 2020 Jun 23;39 (1) :119.