OA-Br-1 is an orally active, selective inhibitor of PTP1B with an IC50 value of 7.08 μM. It induces apoptosis and exhibits broad-spectrum anti-cancer cell proliferation activity. OA-Br-1 exerts anti-breast cancer effects both in vitro and in vivo through the PTP1B/PI3K/AKT signaling pathway.

OA-Br-1 exhibits strong inhibitory activity against PTP1B with an IC50 value of 7.08 μM, while its inhibitory effect on TCPTP is weaker, with an IC50 of 222.28 μM [1]. It inhibits the proliferation of breast cancer cells (MCF-7, MDA-MB-231, MDA-MB-453) in a concentration- and time-dependent manner, with IC50 values of 8.76, 18.13, and 22.34 μM at 72 hours, respectively [1]. OA-Br-1 (5-30 μM; 48 h) induces apoptosis in MCF-7 and MDA-MB-231 cells [1] and increases the thermal stability of PTP1B [1]. Additionally, OA-Br-1 reduces colony formation in these cells dose-dependently [1] and decreases protein levels of p-PI3K and p-AKT, indicating its antitumor activity through the PTP1B/PI3K/AKT pathway in breast cancer cells [1].

OA-Br-1 (30-60 mg/kg; oral administration; daily) exhibits antitumor effects in a BALB/c female nude mouse model with subcutaneously implanted MCF-7 cells by inhibiting the PTP1B/PI3K/AKT signaling pathway [1].