Elesclomol (STA-4783)

Catalog #

27748-1

$180 *

Size: 5 mg

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Description

Elesclomol is a HSP-90 Inhibitor with pro-apoptotic and potential antineoplastic activities. Elesclomol induces oxidative stress and triggers mitochondrial-induced apoptosis in cancer cells.

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Synonyms

Elesclomol; STA-4783; STA4783

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Product Info

Storage and Usage

Citations

Target(s)

HSP90

Formula

C₁₉H₂₀N₄O₂S₂

400.5 Da

Solubility

Soluble in DMSO

CAS Registry #

488832-69-5

Background

Elesclomol (also known as STA-4783), originally identified in a cell-based phenotypic screen for proapoptotic activity, is a novel small-molecule that potently induces apoptosis of cancer cells through the rapid generation of reactive oxygen species (ROS) and the induction of unmanageable levels of oxidative stress. Elesclomol exhibits autitumor activity against a broad spectrum of types of cancer cell in human tumor xengograft models due to its excessive ROS production and elevated levels of oxidative stress leading to the death of cancer cells. Elesclomol is currently being studies as a novel cancer therapeutic, in which it has demonstrated ability to prolong progression-free survival in study subjects. Elesclomol induces oxidative stress by provoking a buildup of reactive oxygen species within cancer cells. Elesclomol requires a redox active metal ion to function; the Cu(II) complex is 34 times more potent than the Ni(II) complex and 1040-fold more potent than the Pt(II) complex.

References

1. Blackman, RK, et al. PLoS ONE 2012; 7(1): e29798
2. Kirshner, JR., et al. Mol Cancer Ther 2008; 7:2319-2327

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Elesclomol (STA-4783)

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