GW2974

GW2974 is a potent dual inhibitor of EGFR and HER2 with IC₅₀ value of 0.007 μM and 0.016 μM, respectively. GW2974 demonstrates in vitro inhibition of the EGFR and HER2 and inhibits the growth of tumor cell. GW2974 can be used for glioblastoma multiforme (GBM) disease research^[1][2]. In Vitro:GW2974 (0.5-50 μM, 3 h) has an obvious cytotoxicity appeared at 10 μM or above and inhibits cell proliferation of U87MG and U251MG cells at 0.5-5 μM after 24 h treatment^[1].
GW2974 (0.5-5 μM, 24 h) has a dose-related role in GBM cell invasion and migration^[1].
GW2974 (0.001-100 μM, 24 h) inhibits BT474, HN5, N87 cells growth^[2].
In Vivo:GW2974 (30 mg/kg, 100 mg/kg for Oral gavage, once a day) inhibits GBM growth, invasion, and angiogenesis in dose of 30 mg/kg but abrogated the inhibitory effect of low-dose GW2974 on tumor invasion in dose of 100 mg/kg in GBM xenograft mice model^[1].
GW2974 (10 mg/kg, 30 mg/kg, Oral gavage, twice a day) inhibits the growth of tumor in CD-1 nude mice (HN5) and C.B-17 SCID mice (BT474) models in a dosed dependent manner^[2].