Effective Hsp90 Inhibitor From MedChemExpress

Frequent activation of endogenous retrotransposons in cancer cells leads to tumour genomic instability. To examine the potential anticancer effects of inhibiting retrotransposition, we treated the MMTV-HER2/Neu mouse cancer model that naturally develops breast cancer with stavudine, a nucleoside reverse transcriptase inhibitor (NRTI). To establish a model of acquired treatment resistance, we were interested in selecting a drug that would be initially effective against primary tumours and relatively safe, thus enabling long-term application but allowing tumours to relapse regardless of continuous treatment. The drug that satisfied our criteria was a small molecule 17-DMAG (Alvespimycin), a clinical-stage semi-synthetic derivative of the Hsp90 inhibitor geldanamycin. Treatment with 17-DMAG of mice with established tumours resulted in complete responses in most of the animals.