WX-132-18B 

WX-132-18B is a tubulin inhibitor with an IC₅₀ of 0.45-0.99 nM. WX-132-18B selectively binds to the colchicine-binding site on tubulin, reduces microtubule content via depolymerization, and inhibits tubulin polymerization. WX-132-18B induces tumor cell cycle arrest, apoptosis and changes in nuclear membrane permeability, and decreases mitochondrial membrane potential. WX-132-18B exhibits antiproliferative activity against endothelial cells and human tumor cells, and inhibits the proliferation and growth of xenograft tumors in mice. WX-132-18B can be used in research related to sarcoma, non-small cell lung cancer, gastric cancer and breast cancer^[1][2].

WX-132-18B (72 h) potently inhibits the proliferation of HepG2, HeLa, A549, H460, BGC-823, MX-1, taxol-resistant MX-1/T, and HUVEC cells with IC₅₀ values ranging from 0.45 to 0.99 nM^[1].
WX-132-18B (1-10 nM; 24 h) reduces tubulin content and altering tubulin morphology with EC₅₀ values ranging from 2.99 to 9.43 nM^[1].
WX-132-18B (0.1-10 μM; 45 min pre-incubation with tubulin, 45 min incubation with colchicine) competitively binds to the colchicine-binding site on tubulin with an IC₅₀ of 0.47 μM^[1].
WX-132-18B (1-10 nM; 24-48 h) potently arrests A549 cells at the G2/M phase of the cell cycle within 24 h, induces concentration-dependent apoptosis in A549 cells after 48 h, and triggers concentration-dependent cytotoxicity in HepG2 cells at 24 h by increasing nuclear membrane permeability while reducing manganese superoxide dismutase levels and mitochondrial membrane potential^[1].
WX-132-18B (0.03-3 μM; per manufacturer instructions) exhibits high target selectivity, with no significant effect on 21 screened tumor-related signaling pathways and only weak, non-specific DNA damage (Rad51 foci induction) at high concentrations^[1].
WX-132-18B (compound 2) displays broad-spectrum and ultra-potent antiproliferative activity with low-to-subnanomolar GI₅₀ values across most NCI-60 human tumor cell lines, although its potency is decreased in HOP-92, MALME-3M, SK-MEL-28, UACC-257, OVCAR-5, and TK-10 cells. It also strongly inhibits the growth of A549, KB, and KB-VIN cells with GI₅₀ values of 2.20-3.20 nM^[2].
WX-132-18B (15 min preincubation; 20 min incubation with GTP) inhibits purified tubulin polymerization with an IC₅₀ of 0.77 μM^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

WX-132-18B (0.25-1.0 mg/kg; i.p.; twice a week; 3 weeks) dose-dependently inhibits sarcoma S180 xenograft growth in KM mice^[1].
WX-132-18B (0.25-1.0 mg/kg; i.p.; twice a week; 3 weeks) dose-dependently inhibits BGC-823 human gastric cancer xenograft growth in nude mice via inducing apoptosis, inhibiting cell proliferation, and suppressing angiogenesis^[1].
WX-132-18B (0.25-1.0 mg/kg; i.p.; once every 5 days; 3 weeks) dose-dependently inhibits H460 human non-small cell lung cancer xenograft growth in nude mice^[1].
WX-132-18B (compound 2) (0.25-1.0 mg/kg; i.v.; every 5 days; 3 weeks) exhibits dose-dependent in vivo antitumor activity against NCI-H460 xenografts^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

320.35

C₁₈H₁₆N₄O₂

1415262-07-5

O=C1NC2=CC(OC)=CC=C2N(C=3N=C(N=C4C=CC=CC43)C)C1

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Guan F, et al. WX-132-18B, a novel microtubule inhibitor, exhibits promising anti-tumor effects. Oncotarget. 2017 May 9;8(42):71782-71796.

  [2]. Cui MT, et al. In Vivo and Mechanistic Studies on Antitumor Lead 7-Methoxy-4-(2-methylquinazolin-4-yl)-3,4-dihydroquinoxalin-2(1H)-one and Its Modification as a Novel Class of Tubulin-Binding Tumor-Vascular Disrupting Agents. J Med Chem. 2017;60(13):5586-5598.  [Content Brief]