Description
HS-173 is an imidazopyridine analog that acts as a PI3Kα inhibitor with an IC
50 value of 0.8 nM. It demonstrates antiproliferative activity in T47D, SK-BR-3, and MCF-7 cells with IC
50 values of 0.6, 1.5, and 7.8 μM, respectively. HS-173 is reported to induce apoptosis by arresting the cell cycle at the G
2/M phase and by activating caspases. It has also been shown to block VEGF-induced angiogenesis both
in vitro and
in vivo.
Uses
HS-173 is a potent PI3Kα inhibitor with anticancer activity.
in vitro
hs-173 inhibited the pi3k signaling pathway, and showed anti-proliferative effects on cancer cells. also, hs-173 induced cell cycle arrest at the g2/m phase and apoptosis. in addition, hs-173 decreased the expression hif-1a and vegf which play an important role in angiogenesis. this effect was confirmed by the suppression of tube formation and migration assay in vitro [1].
in vivo
hs-173 diminished blood vessel formation in the matrigel plug assay in mice. these results suggest that hs-173 has potent anti-angiogenic activity in vivo [1].
References
[1] lee h, jung kh, jeong y, hong s, hong ss. hs-173, a novel phosphatidylinositol 3-kinase (pi3k) inhibitor, has anti-tumor activity through promoting apoptosis and inhibiting angiogenesis. cancer lett. 2013 jan 1;328(1):152-9.
