WZB117

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

WZB117 (WZB-117) 是葡萄糖转运蛋白 1 (GLUT1) 的小分子抑制剂。

WZB117 (WZB-117) is a small-molecule inhibitor of glucose transporter 1 (GLUT1), inhibits glucose transport and cancer cell proliferation with IC50 of 10 uM; decreases in levels of Glut1 protein, intracellular ATP, and glycolytic enzymes in treated cancer cells, inhibits cancer growth in tumor-bearing nude mice; also inhibits the self-renewal and tumor-initiating capacity of cancer stem cells (CSCs).

Glucose uptake assays show that WZB117 inhibits glucose transport in cancer cells in a dose-dependent manner. The inhibition of glucose transport induced by WZB117 occurres within 1 minute after the assay started, suggesting that the inhibitory activity is likely to be via a direct and fast mechanism. Cell viability assay shows that WZB117 inhibits cancer cell proliferation with an IC50 of approximately 10 μM. The inhibitory activity of WZB117 on cancer cell growth is also confirmed with a clonogenic assay, which also indicates that the inhibition is irreversible in nature. WZB117 treatment results in significantly more cell growth inhibition in lung cancer A549 cells than in nontumorigenic lung NL20 cells. Similar results are also observed in breast cancer MCF7 cells and their nontumorigenic MCF12A cells. When WZB117 is added to cancer cells grown under hypoxic conditions, more cell growth inhibition is observed than under normoxic conditions.

The animal study shows that after daily intraperitoneal injection of WZB117 at 10 mg/kg body weight, the sizes of the compound-treated tumors are on average more than 70% smaller than those of the mock (PBS/DMSO)-treated tumors. Notably, 2 of the 10 compound-treated tumors disappear during the treatment and never grow back even at the end of the study. Body weight measurement and analysis reveal that the mice treated with WZB117 lost about 1 to 2 grams of body weight compared with the mock-treated mice with most of the weight loss in the fat tissue. Blood counts and analysis of mice at the end of the study show that lymphocytes and platelets are changed in the compound-treated mice compared with the vehicle-treated mice, but the cell counts remained in the normal ranges. One of the concerns for using glucose transport inhibitors is that the inhibitor might produce hyperglycemia in the treated mice.

WZB-117

Membrane Transporter/Ion Channel

GLUT

GLUT1

Cancer

——

1223397-11-2

368.316

C20H13FO6

>98% (HPLC)

DMSO: 36.8 mg/mL (100 mM); Ethanol: 36.8 mg/mL (100 mM) （ < 1 mg/ml refers to the product slightly soluble or insoluble )

FC1=C(OC(C2=CC=CC(O)=C2)=O)C(OC(C3=CC=CC(O)=C3)=O)=CC=C1

3-Fluoro-1,2-phenylene bis(3-hydroxybenzoate)

(-20℃)

With Ice Pack

≥ 2 years