mpc-3100

MPC-3100 is a fully synthetic, orally bioavailable small-molecule inhibitor of heat shock protein 90 (Hsp90), developed by Myriad Pharmaceuticals for the treatment of cancer. It selectively binds to the N-terminal ATP-binding site of Hsp90 and blocks its ATPase activity. By inhibiting Hsp90’s chaperone function, MPC-3100 promotes degradation of oncogenic signaling proteins involved in tumor cell proliferation and survival. This mechanism may inhibit growth and survival across a variety of cancer cell types. Preclinical studies have shown broad-spectrum antiproliferative activity against multiple cancer cell lines and efficacy in xenograft models. Phase I clinical trials demonstrated that MPC-3100 is safe and well-tolerated at doses below 600 mg per day[1][2][3][4][5]. MPC‑3100 has also been studied in combination with doxorubicin for synergistic cytotoxic effects in breast cancer cell lines[6]. The drug has not received regulatory approval for any indication.

Other names

(S)-1-(4-(2-(6-Amino-8-((6-bromobenzo[d][1,3]dioxol-5-yl)thio)-9H-purin-9-yl)ethyl)piperidin-1-yl)-2-hydroxypropan-1-one