CAS No. : 488832-69-5

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For research use only. Not Intended for Therapeutic Use!
Cat No:I000036
Molecular Formula:C19H20N4O2S2
Molecular Weight:400.5
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Appearance:Solid powder
Purity: > 98%
Cat No:I000036
Cas No:488832-69-5

Elesclomol (STA-4783,  cas 488832-69-5) is a novel potent oxidative stress inducer that elicits pro-apoptosis events among tumor cells.
in vitro: Elesclomol significantly induces the expression of heat shock stress response genes and metallothionein genes, a signature transcription profile indicative of oxidative stress in Hs294T cells. Elesclomol (100 nM) rapidly induces Hsp70 RNA levels with a 4.8-fold increase at 1 hour and a 160-fold increase at 6 hours in Ramos Burkitt/'s lymphoma B cells in consistent with the intracellular ROS content which increases by 20% as early as 0.5 hour and 385% at 6 hours, and the induction of Hsp70 can be blocked by antioxidants N-acetylcysteine (NAC) and Tiron pretreatment. Elesclomol increases the number of early and late apoptotic cells with 3.7- and 11-fold through the induction of oxidative stress, which can be completely blocked by NAC, while having little effect on normal cells. 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 copper-dependent ROS generation and cytoxicity in yeast. Instead of working through a specific cellular protein target, Elesclomol interacts with the electron transport chain (ETC), a biologically coherent set of processes occurring in the mitochondrion, to generate high levels of ROS within the organelle and consequently cell death.
in vivo: Although Elesclomol (25-100 mg/kg) as a single agent shows no antitumor activity in nude mouse xenograft models of human breast cancers (MDA435, MCF7 and ZR-75-1), lung cancer (RER) or lymphoma (U937), Elesclomol substantially enhances the efficacy of chemotherapeutic agents such as paclitaxel in these models, both in terms of tumor regression and extended survival of mice.

Originator: Synta Pharmaceuticals
Class: Antineoplastics; Hydrazines; Ketones; Small molecules; Thiones
Mechanism of Action: Apoptosis stimulants; Chelating agents; HSP70 heat shock protein stimulants; Reactive oxygen species stimulants
Orphan Drug Status: Yes - Malignant melanoma

1:Loss of ARID1A expression leads to sensitivity to ROS-inducing agent elesclomol in gynecologic cancer cells. Kwan SY, Cheng X, Tsang YT, Choi JS, Kwan SY, Izaguirre DI, Kwan HS, Gershenson DM, Wong KK.Oncotarget. 2016 Aug 30;7(35):56933-56943. doi: 10.18632/oncotarget.10921. PMID: 27486766 Free PMC Article
2:A phase I study of elesclomol sodium in patients with acute myeloid leukemia. Hedley D, Shamas-Din A, Chow S, Sanfelice D, Schuh AC, Brandwein JM, Seftel MD, Gupta V, Yee KW, Schimmer AD.Leuk Lymphoma. 2016 Oct;57(10):2437-40. doi: 10.3109/10428194.2016.1138293. Epub 2016 Feb 5. No abstract available. PMID: 26732437
3:Cellular mechanisms of the cytotoxicity of the anticancer drug elesclomol and its complex with Cu(II). Hasinoff BB, Wu X, Yadav AA, Patel D, Zhang H, Wang DS, Chen ZS, Yalowich JC.Biochem Pharmacol. 2015 Feb 1;93(3):266-76. doi: 10.1016/j.bcp.2014.12.008. Epub 2014 Dec 27. PMID: 25550273
4:An /enhanced PET/-based fluorescent probe with ultrasensitivity for imaging basal and elesclomol-induced HClO in cancer cells. Zhu H, Fan J, Wang J, Mu H, Peng X.J Am Chem Soc. 2014 Sep 17;136(37):12820-3. doi: 10.1021/ja505988g. Epub 2014 Sep 3. PMID: 25171114
5:The cytotoxicity of the anticancer drug elesclomol is due to oxidative stress indirectly mediated through its complex with Cu(II). Hasinoff BB, Yadav AA, Patel D, Wu X.J Inorg Biochem. 2014 Aug;137:22-30. doi: 10.1016/j.jinorgbio.2014.04.004. Epub 2014 Apr 16. PMID: 24798374
6:Synthesis, crystallographic characterization and electrochemical property of a copper(II) complex of the anticancer agent elesclomol. Vo NH, Xia Z, Hanko J, Yun T, Bloom S, Shen J, Koya K, Sun L, Chen S.J Inorg Biochem. 2014 Jan;130:69-73. doi: 10.1016/j.jinorgbio.2013.10.005. Epub 2013 Oct 12. PMID: 24176921
7:Syntheses and antitumor activities of N/'1,N/'3-dialkyl-N/'1,N/'3-di-(alkylcarbonothioyl) malonohydrazide: the discovery of elesclomol. Chen S, Sun L, Koya K, Tatsuta N, Xia Z, Korbut T, Du Z, Wu J, Liang G, Jiang J, Ono M, Zhou D, Sonderfan A.Bioorg Med Chem Lett. 2013 Sep 15;23(18):5070-6. doi: 10.1016/j.bmcl.2013.07.032. Epub 2013 Jul 25. PMID: 23937981
8:Molecular mechanisms of the biological activity of the anticancer drug elesclomol and its complexes with Cu(II), Ni(II) and Pt(II). Yadav AA, Patel D, Wu X, Hasinoff BB.J Inorg Biochem. 2013 Sep;126:1-6. doi: 10.1016/j.jinorgbio.2013.04.013. Epub 2013 Apr 28. PMID: 23707906
9:Final results of phase III SYMMETRY study: randomized, double-blind trial of elesclomol plus paclitaxel versus paclitaxel alone as treatment for chemotherapy-naive patients with advanced melanoma. O/'Day SJ, Eggermont AM, Chiarion-Sileni V, Kefford R, Grob JJ, Mortier L, Robert C, Schachter J, Testori A, Mackiewicz J, Friedlander P, Garbe C, Ugurel S, Collichio F, Guo W, Lufkin J, Bahcall S, Vukovic V, Hauschild A.J Clin Oncol. 2013 Mar 20;31(9):1211-8. doi: 10.1200/JCO.2012.44.5585. Epub 2013 Feb 11. PMID: 23401447
10:The oncology drug elesclomol selectively transports copper to the mitochondria to induce oxidative stress in cancer cells. Nagai M, Vo NH, Shin Ogawa L, Chimmanamada D, Inoue T, Chu J, Beaudette-Zlatanova BC, Lu R, Blackman RK, Barsoum J, Koya K, Wada Y.Free Radic Biol Med. 2012 May 15;52(10):2142-50. doi: 10.1016/j.freeradbiomed.2012.03.017. Epub 2012 Apr 17. PMID: 22542443
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