In Vitro: BT5528 shows high affinity on EphA2 with a Kb value of 19.1 nM, and activates EphA2 in EphA2-expressing cells with an EC50 value of 41.9 nM. BT5528 inhibits cancer cells growth with IC50s of 21.9 nM (HT-1080), 5.2 nM (PC-3), 21.6 nM (NCI-H1975), respectively.
In Vivo: BT5528 (1, 2, 3 mg/kg; i.v.; once a week; 2-5 weeks) inhibits tumor growth in vivo in mice xenograft model. BT5528 (3 mg/kg; i.v.; once a week; 3 weeks) exhibits greate ability to penetrate solid tumours in Non-small-cell lung carcinoma (NSCLC) Patient-derived xenograft (PDX) xenograft model in mice.