BAY-876-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEBAY-876Cat. No.: HY-100017CAS No.: 1799753-84-6分式: CHFNO分量: 496.42作靶點(diǎn): Others作通路: Others儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 100 mg/mL (201.44 mM)H2O : 90% (20% SBE-CD in saline)

2、Solubility: 10 mg/mL (20.14 mM); Suspended solution; Need ultrasonic2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 10 mg/mL (20.14 mM); Clear solution1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 BAY-876種服有效，選擇性 GLUT1 抑制劑，IC50 為 2 nM。 BAY-876 在體外顯出良好的代謝穩(wěn)定性和體內(nèi)的服物利度。 BAY-876

3、可以阻斷基礎(chǔ)和應(yīng)激調(diào)節(jié)的糖酵解以及卵巢癌細(xì)胞的貼壁依賴性和獨(dú)長(zhǎng)。IC50 & Target IC50: 2 nM (GLUT1) 1體外研究 BAY-876 (25-75 nM; 24 and 72 hours) has the growth-inhibitory effect and leads to a dose-dependentdecrease in numbers of SKOV-3 and OVCAR-3 cells 2.Cell Proliferation Assay 2Cell Line: SKOV-3 and OVCAR-3 cellsConcentration: 25, 5

4、0, 75 nMIncubation Time: 24 and 72 hoursResult: Led to a dose-dependent decrease in numbers of SKOV-3 and OVCAR-3 cells.體內(nèi)研究 BAY-876 (Oral administration; 1.5-4.5 mg/kg/day for 28 days) causes a clear dose-dependent inhibition oftumorigenicity in mice 2.Animal Model: Female NOD-scid IL2rgnull (NSG)

5、mice carrying SKOV-3 subcutaneous (s.c.) xenografts2Dosage: 1.5, 3, 4.5 mg/kgAdministration: Oral administration; daily; for 28 daysResult: Caused a clear dose-dependent inhibition of tumorigenicity.REFERENCES1. Siebeneicher H et al. Identification and Optimization of the First Highly Selective GLUT

6、1 Inhibitor BAY-876. ChemMedChem. 2016 Aug23.2. Ma Y, et al. Ovarian Cancer Relies on Glucose Transporter 1 to Fuel Glycolysis and Growth: Anti-Tumor Activity of BAY-876. Cancers(Basel). 2018 Dec 31;11(1).McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.Tel: 400-820