BAY-876 |
| カタログ番号GC19061 |
BAY-876 は、IC50 が 2 nM の経口活性で選択的なグルコーストランスポーター 1 (GLUT1) 阻害剤です。 BAY-876 は、GLUT2、GLUT3、および GLUT4 よりも GLUT1 に対して 130 倍以上選択的です。 BAY-876 は、解糖代謝と卵巣がんの増殖を強力に阻害します。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1799753-84-6
Sample solution is provided at 25 µL, 10mM.
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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].
References:
[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).
Average Rating: 5 (Based on Reviews and 9 reference(s) in Google Scholar.)
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