AGI-24512 is a potent methionine adenosyltransferase 2α ( MAT2A ) inhibitor, with an IC 50 of 8 nM. AGI-24512 triggers DNA damage response. AGI-24512 can block proliferation of MTAP-deleted cancer cells in vitro . AGI-24512 can be used for researching anticancer
In Vitro
AGI-24512 (0-1 μM; 96 hours) blocks proliferation of MTAP (methylthioadenosine phosphorylase)-deleted HCT116 cancer cells with an IC 50 of 100 nM. AGI-24512 significantly increases in γH2AX-positive cells in MTAP -/- HCT116 cells. AGI-24512 inhibits PRMT5-mediated SDMA marks with an IC 50 of 95 nM in MTAP -/- cells. AGI-24512 leads to a dose-dependent decrease in SAM (S-adenosylmethionine) levels in the HCT116 MTAP- cell, with an IC 50 of 100 nM. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
AGI-24512 shows poor oral absorption and a short half-life in rats. MCE has not independently confirmed the accuracy of these methods. They are for reference only.