WZB117-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEWZB117Cat. No.: HY-19331CAS No.: 1223397-11-2分式: CHFO分量: 368.31作靶点: Others作通路: Others储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 150 mg/mL (407.27 mM)* means soluble, but saturation unk

2、nown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.7151 mL 13.5755 mL 27.1510 mL5 mM 0.5430 mL 2.7151 mL 5.4302 mL10 mM 0.2715 mL 1.3576 mL 2.7151 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清的储备液可以根据储存条件，适当保存；

3、以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (6.79 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (6.79 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oil1/3 Master of Small Molecules 您边的抑制剂师ww

4、w.MedChemESolubility: 2.5 mg/mL (6.79 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 WZB117种葡萄糖转运蛋 1 (Glut1) 抑制剂，可下调糖酵解，诱导细胞周 期停滞，并在体内外抑制癌细胞长。IC50 & Target Glut1 1体外研究 Glucose uptake assays show that WZB117 inhibits glucose transport in cancer cells in a dose-dependentmanner. The inhibition of glucose tr

5、ansport induced by WZB117 occurres within 1 minute after the assaystarted, suggesting that the inhibitory activity is likely to be via a direct and fast mechanism. Cell viabilityassay shows that WZB117 inhibits cancer cell proliferation with an IC50 of approximately 10 M. Theinhibitory activity of W

6、ZB117 on cancer cell growth is also confirmed with a clonogenic assay, which alsoindicates that the inhibition is irreversible in nature. WZB117 treatment results in significantly more cellgrowth inhibition in lung cancer A549 cells than in nontumorigenic lung NL20 cells. Similar results are alsoobs

7、erved in breast cancer MCF7 cells and their nontumorigenic MCF12A cells. When WZB117 is added tocancer cells grown under hypoxic conditions, more cell growth inhibition is observed than under normoxicconditions 1.体内研究 The animal study shows that after daily intraperitoneal injection of WZB117 at 10

8、mg/kg body weight, thesizes 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 treatmentand never grow back even at the end of the study. Body weight measurement and an

9、alysis reveal that themice treated with WZB117 lost about 1 to 2 grams of body weight compared with the mock-treated mice withmost of the weight loss in the fat tissue. Blood counts and analysis of mice at the end of the study show thatlymphocytes and platelets are changed in the compound-treated mi

10、ce compared with the vehicle-treatedmice, but the cell counts remained in the normal ranges. One of the concerns for using glucose transportinhibitors is that the inhibitor might produce hyperglycemia in the treated mice 1.PROTOCOLCell Assay 1 Human non-small cell lung cancer (NSCLC) cell lines H129

11、9 and A549, human breast ductal carcinomaMCF7, as well as human nontumorigenic NL20 lung and MCF12A breast cells are maintained in cell culturemedia. Cells are treated with WZB117 for 24 or 48 hours. WZB117 (10 M) is used in the experiments unlessotherwise noted. Mock-treated and glucose deprivation

12、 samples served as negative and positive controls,respectively. In glucose deprivation, Dulbeccos Modified Eagles Media (DMEM) with reduced glucoseconcentration (2 mM or 8% of glucose concentration in the regular cell culture medium) is prepared by mixingglucose-free DMEM with regular DMEM 1.MCE has

13、 not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice 12/3 Master of Small Molecules 您边的抑制剂师www.MedChemEAdministration 1 Male NU/J nude mice of 6 to 8 weeks of age are used. To determine the in vivo anticancer efficacy ofWZB117 on human tumor xenograft g

14、rowth, NSCLC A549 cells in exponential growth phase are harvested,washed, precipitated, and resuspended in PBS. Each mouse is injected subcutaneously with 5106 cancercells in the flank. Compound treatment started 3 days after the cancer cells injection and when all tumorsbecome palpable. Tumor celli

15、njected mice are randomly divided into 2 groups: control group (n=10) treatedwith PBS/DMSO (1:1, v/v) and WZB117 treatment group (n=10) treated with WZB117 (10 mg/kg bodyweight) dissolved in PBS/DMSO solution (1:1, v/v). Mice are given intraperitoneal injection with eitherPBS/DMSO vehicle or WZB117

16、(10 mg/kg) daily for 10 weeks. Tumor sizes are measured every 7 days withcalipers, and tumor volume is calculated 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Liu Y, et al. A small-molecule inhibitor of glucose transporter 1 downregulates glycolysis, induces cell-cycle arrest, and inhibits cancercell growth in vitro and in v