Elesclomol
Elesclomol, also known as STA-4783, is a HSP-90 Inhibitor, and is a small-molecule bis(thio-hydrazide amide) with oxidative stress induction, pro-apoptotic, and potential antineoplastic activities. Elesclomol induces oxidative stress, creating high levels of reactive oxygen species (ROS), such as hydrogen peroxide, in both cancer cells and normal cells. Because tumor cells have elevated levels of ROS compared to normal cells, the increase in oxidative stress beyond baseline levels elevates ROS beyond sustainable levels, exhausting tumor cell antioxidant capacity, which may result in the induction of the mitochondrial apoptosis pathway.
1: Blackman RK, Cheung-Ong K, Gebbia M, Proia DA, He S, Kepros J, Jonneaux A, Marchetti P, Kluza J, Rao PE, Wada Y, Giaever G, Nislow C. Mitochondrial electron transport is the cellular target of the oncology drug elesclomol. PLoS One. 2012;7(1):e29798. Epub 2012 Jan 11. PubMed PMID: 22253786; PubMed Central PMCID: PMC3256171.
2: Wu L, Zhou L, Liu DQ, Vogt FG, Kord AS. LC-MS/MS and density functional theory study of copper(II) and nickel(II) chelating complexes of elesclomol (a novel anticancer agent). J Pharm Biomed Anal. 2011 Jan 25;54(2):331-6. Epub 2010 Sep 15. PubMed PMID: 20933353.
3: O'Day S, Gonzalez R, Lawson D, Weber R, Hutchins L, Anderson C, Haddad J, Kong S, Williams A, Jacobson E. Phase II, randomized, controlled, double-blinded trial of weekly elesclomol plus paclitaxel versus paclitaxel alone for stage IV metastatic melanoma. J Clin Oncol. 2009 Nov 10;27(32):5452-8. Epub 2009 Oct 13. PubMed PMID: 19826135.
4: Qu Y, Wang J, Sim MS, Liu B, Giuliano A, Barsoum J, Cui X. Elesclomol, counteracted by Akt survival signaling, enhances the apoptotic effect of chemotherapy drugs in breast cancer cells. Breast Cancer Res Treat. 2010 Jun;121(2):311-21. Epub 2009 Jul 16. PubMed PMID: 19609669.
5: Wangpaichitr M, Wu C, You M, Maher JC, Dinh V, Feun LG, Savaraj N. N',N'-Dimethyl-N',N'-bis(phenylcarbonothioyl) Propanedihydrazide (Elesclomol) Selectively Kills Cisplatin Resistant Lung Cancer Cells through Reactive Oxygen Species (ROS). Cancers (Basel). 2009;1(1):23-38. PubMed PMID: 20535236; PubMed Central PMCID: PMC2882109.
6: Kirshner JR, He S, Balasubramanyam V, Kepros J, Yang CY, Zhang M, Du Z, Barsoum J, Bertin J. Elesclomol induces cancer cell apoptosis through oxidative stress. Mol Cancer Ther. 2008 Aug;7(8):2319-27. PubMed PMID: 18723479.
7: Molecule of the month. Elesclomol and obatoclax mesylate. Drug News Perspect. 2008 Mar;21(2):123-4. PubMed PMID: 18389103.
2: Wu L, Zhou L, Liu DQ, Vogt FG, Kord AS. LC-MS/MS and density functional theory study of copper(II) and nickel(II) chelating complexes of elesclomol (a novel anticancer agent). J Pharm Biomed Anal. 2011 Jan 25;54(2):331-6. Epub 2010 Sep 15. PubMed PMID: 20933353.
3: O'Day S, Gonzalez R, Lawson D, Weber R, Hutchins L, Anderson C, Haddad J, Kong S, Williams A, Jacobson E. Phase II, randomized, controlled, double-blinded trial of weekly elesclomol plus paclitaxel versus paclitaxel alone for stage IV metastatic melanoma. J Clin Oncol. 2009 Nov 10;27(32):5452-8. Epub 2009 Oct 13. PubMed PMID: 19826135.
4: Qu Y, Wang J, Sim MS, Liu B, Giuliano A, Barsoum J, Cui X. Elesclomol, counteracted by Akt survival signaling, enhances the apoptotic effect of chemotherapy drugs in breast cancer cells. Breast Cancer Res Treat. 2010 Jun;121(2):311-21. Epub 2009 Jul 16. PubMed PMID: 19609669.
5: Wangpaichitr M, Wu C, You M, Maher JC, Dinh V, Feun LG, Savaraj N. N',N'-Dimethyl-N',N'-bis(phenylcarbonothioyl) Propanedihydrazide (Elesclomol) Selectively Kills Cisplatin Resistant Lung Cancer Cells through Reactive Oxygen Species (ROS). Cancers (Basel). 2009;1(1):23-38. PubMed PMID: 20535236; PubMed Central PMCID: PMC2882109.
6: Kirshner JR, He S, Balasubramanyam V, Kepros J, Yang CY, Zhang M, Du Z, Barsoum J, Bertin J. Elesclomol induces cancer cell apoptosis through oxidative stress. Mol Cancer Ther. 2008 Aug;7(8):2319-27. PubMed PMID: 18723479.
7: Molecule of the month. Elesclomol and obatoclax mesylate. Drug News Perspect. 2008 Mar;21(2):123-4. PubMed PMID: 18389103.
| Chemical | |
|---|---|
| CAS Num | 488832-69-5 |
| Chemical Formula | C19H20N4O2S2 |
| Molecular Weight | 400.52 |
| IUPAC Chemical Name | N'1,N'3-dimethyl-N'1,N'3-di(phenylcarbonothioyl)malonohydrazide |
| Exact Mass | 400.10277 |
| Elemental Analysis | C, 56.98; H, 5.03; N, 13.99; O, 7.99; S, 16.01 |
| Synonym | STA4783; STA-4783; STA 4783, Elesclomol. |
| Solubility | Soluble in DMSO, not in water |
| SMILES Code | O=C(NN(C)C(C1=CC=CC=C1)=S)CC(NN(C)C(C2=CC=CC=C2)=S)=O |
| Biological | |
| Targets and Effects | HSP-90 Inhibitor |
| Pathways | Apoptosis |
| Physical | |
| Appearance | Solid powder |
| Purity | >98% (or refer to the Certificate of Analysis) |
| Shipping Condition | Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. |
| Storage Condition | Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
| Shelf Life | >5 years if stored properly |
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