BAY-876 is the first highly selective GLUT1 inhibitor with IC50 of 0.002 uM.
CAS：1799753-84-6
分子式：C24H16F4N6O2
分子量：496.42
纯度：98%
存储：Store at -20°C

Background:

BAY-876 is an oral and selective GLUT1 inhibitor with an IC50 of 2 nM[1]. BAY-876 shows good metabolic stability in vitro and high oral bioavailability in vivo. BAY-876 is sufficient to block basal and stress-regulated glycolysis, anchorage-dependent and independent growth of ovarian cancer cells[2].

BAY-876 (25-75 nM; 24 and 72 hours) has the growth-inhibitory effect and leads to a dose-dependent decrease in numbers of SKOV-3 and OVCAR-3 cells[2].

BAY-876 (Oral administration; 1.5-4.5 mg/kg/day for 28 days) causes a clear dose-dependent inhibition of tumorigenicity in mice[2].

参考文献:
[1]. Siebeneicher H et al. Identification and Optimization of the First Highly Selective GLUT1 Inhibitor BAY-876. ChemMedChem. 2016 Aug 23.
[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).