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5mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Purity: ≥98%
Elesclomol (STA4783; STA-4783; STA4783) is a bis(thio-hydrazide amide)-based heat shock protein 70/HSP70 inducer as well as an oxidative stress inducer with potential antitumor and pro-apoptotic activity. It activates natural killer (NK) cell-mediated tumor killing and elicits pro-apoptosis events among tumor cells. It was developed by GSK company as a chemotherapy adjuvant but the trial was suspended due to safety concerns.
ln Vitro |
FDX1's α2/α3 helix and β5 strand are bound by elisclomol (STA-4783), but not by the paralogous protein FDX2. A novel FDX1 substrate is elesclomol-Cu(II). Elesclomol-Cu(II) complex is bound by and reduced by the FDX1 protein [1]. After just two hours, electrolysomol-Cu (1:1 ratio) (40 nM) increases intracellular copper levels by 15–60 times, leading to the death of ABC1 cells within 24 hours [1]. Prior to treatment, adding copper to elesclomol at a 1:1 molar ratio dramatically lowers cell viability in cells grown in glycolytic (glucose media) culture [2]. HSB2 cells treated with esclomol (200 nM; 18 hours) have more early and late apoptotic cells. Elesclomol causes oxidative stress, which causes cancer cells to undergo apoptosis [3]. Elesclomol, with IC50 values of 110 nM, 24 nM, and 9 nM, respectively, dramatically reduces the viability of SK-MEL-5, MCF-7, and HL-60 cells [5].
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ln Vivo |
Elesclomol (10 mg/kg; subcutaneous; every three days from postpartum day 5 to 26 and weekly till postpartum day 54) treatment improved hypertrophic heart disease and partially decreased severe cardiac pathology. After receiving Elesclomol, heart [Cu] rose from 34% to 55% of vector knockout levels [4]. Elesclomol raises the amounts of cytochrome c oxidase in the brain and transports copper to the mitochondria. In spotted mice, eloxamol enhances survival and averts detrimental neurological alterations [4].
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Cell Assay |
Apoptosis Analysis[3]
Cell Types: HSB2 cells Tested Concentrations: 200 nM Incubation Duration: 18 hrs (hours) Experimental Results: Increased the number of early and late apoptotic cells. |
Animal Protocol |
Animal/Disease Models: Cardiac Ctr1 knockout mice[4]
Doses: 10 mg/kg Route of Administration: subcutaneous (sc) injection; every three days from post-natal day 5 to 26 and once weekly until post-natal day 54 Experimental Results: Ameliorated severe cardiac pathology with a partial reduction in hypertrophy. |
References |
[1]. Peter Tsvetkov, et al. Copper induces cell death by targeting lipoylated TCA cycle proteins. Science. 2022 Mar 18;375(6586):1254-1261.
[2]. Peter Tsvetkov, et al. Mitochondrial metabolism promotes adaptation to proteotoxic stress. Nat Chem Biol. 2019 Jul;15(7):681-689. [3]. Kirshner JR, et al. Elesclomol induces cancer cell apoptosis through oxidative stress. Mol Cancer Ther. 2008 Aug;7(8):2319-27. [4]. Liam M Guthrie, et al. Elesclomol alleviates Menkes pathology and mortality by escorting Cu to cuproenzymes in mice. Science. 2020 May 8;368(6491):620-625. [5]. Bair JS, et al. Chemistry and biology of deoxynyboquinone, a potent inducer of cancer cell death. J Am Chem Soc. 2010 Apr 21;132(15):5469-7 |
Molecular Formula |
C19H20N4O2S2
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Molecular Weight |
400.5
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CAS # |
488832-69-5
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SMILES |
O=C(NN(C)C(C1=CC=CC=C1)=S)CC(NN(C)C(C2=CC=CC=C2)=S)=O
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InChi Key |
BKJIXTWSNXCKJH-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C19H20N4O2S2/c1-22(18(26)14-9-5-3-6-10-14)20-16(24)13-17(25)21-23(2)19(27)15-11-7-4-8-12-15/h3-12H,13H2,1-2H3,(H,20,24)(H,21,25)
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Chemical Name |
N'1,N'3-dimethyl-N'1,N'3-di(phenylcarbonothioyl)malonohydrazide
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Synonyms |
STA 4783, Elesclomol; STA4783; STA-4783;
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.4969 mL | 12.4844 mL | 24.9688 mL | |
5 mM | 0.4994 mL | 2.4969 mL | 4.9938 mL | |
10 mM | 0.2497 mL | 1.2484 mL | 2.4969 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.