LXQ-217 is an orally active SHP2 inhibitor with an IC50 of 2.01 μM, inducing apoptosis and inhibiting cell growth both in vivo and in vitro [1].

LXQ-217 exhibits inhibitory effects on A549, HCT116, HepG2, and MDA-MB-231 cells with IC50 values of 2.06, 3.88, 4.53, and 5.13 μM, respectively [1]. Treatment with concentrations of 2.5, 5, and 10 μM for 7 days reduces both the number and formation rate of colonies in A549 cells [1]. Incubation at 1.25 and 2.5 μM for 72 hours inhibits the migration of A549 cells [1]. Additionally, a 3-hour incubation at concentrations of 2.5, 5, and 10 μM increases the levels of cleaved PARP (C-parp), cleaved caspase9 (C-cas9), and cleaved caspase3 (C-cas3) proteins in A549 cells [1].

LXQ-217 (50, 100 mg/kg; orally administered for 14 days) effectively inhibited the growth of the A549 xenograft model in BALB/c nude mice, reducing both tumor weight and volume [1]. The animal model used was a BALB/c nude mouse with an A549 xenograft [1].