NP-G2-044 is a potent, orally active fascin inhibitor, with an IC50 of ~2 μM. NP-G2-044 blocks tumor metastasis and increases antitumor immune response[1][2].
NP-G2-044 inhibits the migration of MDA-MB-231 tumor cells with an IC50 ~10 μM. NP-G2-044 decreases filopodial formation resulting in decreased lamellipodial formation[1].
NP-G2-044 (100 mg/kg; i.p.; daily for 18 days) inhibits breast tumor metastasis in mouse models[1].Upon oral administration, NP-G2-044 targets and binds to fascin, thereby preventing the interaction of fascin with actin filaments, thereby preventing actin bundling and filopodia formation. By preventing actin cytoskeletal reorganization, the dynamic changes in cell shape that are necessary for tumor cell migration and invasion to occur are impaired, and tumor cell migration and metastasis are inhibited[3]. Animal Model: 6-8 week old female BALB/c mice (mouse model bearing 4T1 tumor cells)[1]
[1]. Han S, et al. Improving fascin inhibitors to block tumor cell migration and metastasis. Mol Oncol. 2016;10(7):966-980. [2]. Vincent Chung, et al. Abstract C053: NP-G2-044, a novel fascin inhibitor, blocks tumor metastasis and increases antitumor immune response. [3]. Fascin Inhibitor NP-G2-044.