Retaspimycin Hydrochloride

• CAT Number: I005152
• CAS Number: 857402-63-2
• Molecular Formula: C31H46ClN3O8
• Molecular Weight: 624.2
• Purity: ≥95%
• Synonyms: [(3R,5S,6R,7S,8E,10S,11S,12Z,14E)-6,20,22-trihydroxy-5,11-dimethoxy-3,7,9,15-tetramethyl-16-oxo-21-(prop-2-enylamino)-17-azabicyclo[16.3.1]docosa-1(22),8,12,14,18,20-hexaen-10-yl] carbamate;hydrochloride
• Target: Metabolic Enzyme/Protease
• Solubility: 100 mM in H2O
• Storage: Store at -20°C

Retaspimycin Hcl(IPI504 Hcl) is the hydrochloride salt of a small-molecule inhibitor of heat shock protein 90 (HSP90) with antiproliferative and antineoplastic activities.IC50 Value:Target: HSP90Retaspimycin 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 may result in the induction of apoptosis.

Reference

[1]. A phase 1 study of IPI-504 (retaspimycin hydrochloride) in patients with relapsed or relapsed and refractory multiple myeloma By Siegel, David; Jagannath, Sundar; Vesole, David H.; Borello, Ivan; Mazumder, Amitabha; Mitsiades, Constantine; Goddard, Jill; Dunbar, Joi; Normant, Emmanuel; Adams, Julian; et al From Leukemia & Lymphoma (2011), 52(12), 2308-2315
[2]. The Heat Shock Protein 90 Inhibitor IPI-504 Induces KIT Degradation, Tumor Shrinkage, and Cell Proliferation Arrest in Xenograft Models of Gastrointestinal Stromal Tumors By Floris, Giuseppe; Debiec-Rychter, Maria; Wozniak, Agnieszka; Stefan, Cristiana; Normant, Emmanuel; Faa, Gavino; Machiels, Kathleen; Vanleeuw, Ulla; Sciot, Raf; Schoeffski, Patrick From Molecular Cancer Therapeutics (2011), 10(10), 1897-1908.
[3]. Antitumor Activity of the Hsp90 Inhibitor IPI-504 in HER2-Positive Trastuzumab-Resistant Breast Cancer By Scaltriti, Maurizio; Serra, Violeta; Normant, Emmanuel; Guzman, Marta; Rodriguez, Olga; Lim, Alice R.; Slocum, Kelly L.; West, Kip A.; Rodriguez, Varenka; Prudkin, Ludmila; et al From Molecular Cancer Therapeutics (2011), 10(5), 817-824.
[4]. Oh WK, Galsky MD, Stadler WM, Srinivas S, Chu F, Bubley G, Goddard J, Dunbar J, Ross RW.Multicenter phase II trial of the heat shock protein 90 inhibitor, retaspimycin hydrochloride (IPI-504), in patients with castration-resistant prostate cancer. Urology. 2011 Sep;78(3):626-30.
[5]. Hanson BE, Vesole DH. Retaspimycin hydrochloride (IPI-504): a novel heat shock protein inhibitor as an anticancer agent. Expert Opin Investig Drugs. 2009 Sep;18(9):1375-83.