IPI-504 (Retaspimycin hydrochloride)

Catalog #

27753-1

$425 *

Size: 10 mg

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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.

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Synonyms

IPI-504; Retaspimycin hydrochloride;

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Product Data Gallery

Product Info

Storage and Usage

Citations

Target(s)

HSP90

Formula

C₃₁H_{46C_lN₃O₈}

624.2 Da

Solubility

Soluble in DMSO

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 Registry #

857402-63-2

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.

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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IPI-504 (Retaspimycin hydrochloride)

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