Elesclomol (STA-4783) is a first-in-class investigational compound currently undergoing clinical evaluation as a novel cancer therapeutic. Elesclomol significantly inhibits the cell viability of SK-MEL-5, MCF-7 and HL-60 with IC50 of 110 nM, 24 nM and 9 nM, respectively. Elesclomol induces oxidative stress by provoking a buildup of reactive oxygen species within cancer cells. Elesclomol interacts with the electron transport chain (ETC) to generate high levels of ROS within the organelle and consequently cell death. Elesclomol induces apoptosis in cancer cells through the induction of oxidative stress. Treatment of cancer cells in vitro with elesclomol resulted in the rapid generation of reactive oxygen species (ROS) and the induction of a transcriptional gene profile characteristic of an oxidative stress response. In addition, N-acetylcysteine blocked drug-induced apoptosis, indicating that ROS generation is the primary mechanism responsible for the proapoptotic activity of elesclomol.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO 80 mg/mL|
Mitochondrial electron transport is the cellular target of the oncology drug elesclomol.
Blackman RK, et al. PLoS One. 2012;7(1):e29798. PMID: 22253786.
Elesclomol, counteracted by Akt survival signaling, enhances the apoptotic effect of chemotherapy drugs in breast cancer cells.
Qu Y, et al. Breast Cancer Res Treat. 2010 Jun;121(2):311-21. PMID: 19609669.
Elesclomol induces cancer cell apoptosis through oxidative stress.
Kirshner JR, et al. Mol Cancer Ther. 2008 Aug;7(8):2319-27. PMID: 18723479.
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