STF-31 selectively kills RCCs by specifically targeting glucose uptake through GLUT1. STF-31 significantly inhibits lactate production and extracellular acidification in VHL-deficient cells by about 60%, and decreases glycolysis by decreasing glucose transport. In NAPRT1-expressing cells, STF-31 shows cytotoxicity by inhibiting the enzymatic activity of NAMPT. STF-31 is toxic to hPSCs and efficient for selective elimination of hPSCs from mixed cultures.
In vivo
In mice with VHL-deficient RCC xenografts, a more soluble analog of STF-31 (11.6 mg/kg, i.p.) markedly delays tumor growth.