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Background: Cancer cells depend on the Hsp90 chaperone to maintain many proteins critical for cancer growth, proliferation and survival in a functional state. Retaspimycin binds to and inhibits the cytosolic chaperone functions of HSP90, which maintains the stability and functional shape of many oncogenic signaling proteins and may be overexpressed or overactive in tumor cells. Retaspimycin-mediated inhibition of HSP90 promotes the proteasomal degradation of oncogenic signaling proteins in susceptible tumor cell populations, which results in the induction of apoptosis.
Biological Activity: IPI-504 potently inhibits proliferation in several tumor cell lines with 50% inhibition concentration IC50 values ranging from 10-40 nM and has been used for the treatment of gastrointestinal stromal tumors, soft-tissue sarcomas and non-small cell lung cancer.
CAS Number: 857402-63-2
Description: Retaspimycin hydrochloride (also known as IPI-504), a hydroquinone hydrochloride salt derivative of 17-AAG, is a novel, potent and selective inhibitor of Hsp90 that binds at the N-terminal ATP/ADP-binding site of Hsp90. Once in the systemic circulation, IPI-504 is deprotonated and converted into the free base IPI-504 which is subsequently oxidized to 17-AAG.
Solubility: Soluble in DMSO
Storage Stability: Store at or below -20°C. Solid form is stable at least 12 months from date of receipt, when stored as directed. Do not store aqueous solutions for more than one day.
Target: HSP90
Biosafety Level: Not applicable (BSL-1)
References: 1. Siegel, D., et al. Leukemia & Lymphoma, 2011; 52(12): 2308-2315.
2. Leow, CC., et al. Mol Cancer Ther 2009; 8: 2131-2141.
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