Elesclomol (STA-4783)

Elesclomol (STA-4783)

Catalog Number:
FC01364937APE
Mfr. No.:
APE-A4386
Price:
$228
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      • Overview
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          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.

          Reference:
          Ronald K. Blackman, Kahlin Cheung-Ong, Marinella Gebbia, David A. Proia, Suqin He, Jane Kepros, Aurelie Jonneaux, Philippe Marchetti, Jerome Kluza, Patricia E. Rao, Yumiko Wada, Guri Giaever, Corey Nislow. Mitochondrial electron transport is the cellular target of the oncology drug elesclomol. PLoS ONE 2012; 7(1): e29798
          Jessica R. Kirshner, Suqin He, Vishwasenani Balasubramanyam, Jane Kepros, Chin-Yu Yang, Mei Zhang, Zhenjian Du, James Barsoum, and John Bertin. Elesclomol induces cancer cell apoptosis through oxidative stress. Mol Cancer Ther 2008; 7:2319-2327

      • Properties
        • Categories
          Oxidative stress/apoptosis inducer, potent and novel
          Alternative Name
          STA 4783, STA4783; 1-N',3-N'-bis(benzenecarbonothioyl)-1-N',3-N'-dimethylpropanedihydrazide
          CAS Number
          488832-69-5
          Molecular Formula
          C19H20N4O2S2
          Molecular Weight
          400.5
          Appearance
          A solid
          Purity
          98.00%
          Solubility
          insoluble in H2O; ≥20.15 mg/mL in DMSO; ≥5.68 mg/mL in EtOH with gentle warming and ultrasonic
          Storage
          Store at -20°C
          SMILES
          CN(C(=S)C1=CC=CC=C1)NC(=O)CC(=O)NN(C)C(=S)C2=CC=CC=C2

          * For Research Use Only

      • Reference
        • 1. Albayrak G, Korkmaz FD, et al. "The outcomes of an impaired powerhouse in KRAS mutant lung adenocarcinoma cells by Elesclomol." J Cell Biochem. 2019 Jan 10. PMID:30628735
          2. Li H, Guo S, et al."Lipopolysaccharide and heat stress impair the estradiol biosynthesis in granulosa cells via increase of HSP70 and inhibition of smad3 phosphorylation and nuclear translocation." Cell Signal. 2017 Jan;30:130-141. PMID:27940052
          3. Ali A. Alshamrani, James L. et al. "Inhibiting Lactate Dehydrogenase A Enhances the Cytotoxicity of the Mitochondria Accumulating Antioxidant, Mitoquinone, in Melanoma Cells." Human Skin Cancer, Potential Biomarkers and Therapeutic Targets.October 19th 2016.

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