PU-H71 is an effective selective HSP90 inhibitor with an IC50 of 51 nM.

HSP90:51 nM

PU-H71(1 μ M) potently inhibits the growth of triple negative breast cancer (TNBC) cell lines MDA-MB-468, MDA-MB-231, and HCC-1806, with IC50 values of 65, 140, and 87 nM, respectively. PU-H71(1 μ M) kills 80%, 65%, and 80% of MDA-MB-468, MDA-MB-231, and HCC-1806 cells, respectively[1].

MDA-MB-231 model treated with PU-H71 at a dose of 75 mg/kg was 100% fully effective. After 37 days of treatment, tumor was replaced by scar tissue, accompanied by a reduction in many proliferative and anti apoptotic molecules, such as EGFR, HER3, Raf-1, Akt, and p-Akt, which decreased by 80%, 95%, 99%, 80%, and 65%, respectively. PU-H71 (75 mg/kg, three times a week) inhibits tumor growth by 96%, reduces tumor cell proliferation by 60%, decreases activated Akt associated with survival and high invasive potential by 85%, and increases apoptosis by 6-fold[1].