Elesclomol (STA-4783) binds the FDX1 α2/α3 helices and β5 strand, but does not bind the paralog protein FDX2. Elesclomol-Cu(II) is an FDX1 neo-substrate. FDX1 protein binds and reduces the elesclomol-Cu(II) complex^[1].
Elesclomol-Cu (1:1 ratio) (40 nM) for only 2 hours results in a 15- to 60-fold increase in intracellular copper levels that triggered cell death more than 24 hours later in ABC1 cells^[1].
The addition of copper to elesclomol at a 1:1 molar ratio prior to treatment significantly reduces cell viability when cells are grown in glycolytic (glucose media) conditions^[2].
Elesclomol (200 nM; 18 hours) treatment increases the number of early and late apoptotic cells in HSB2 cells. Elesclomol induces apoptosis in cancer cells through the induction of oxidative stress^[3].
Elesclomol significantly inhibits the cell viability of SK-MEL-5, MCF-7, and HL-60 cells with IC₅₀ values of 110 nM, 24 nM and 9 nM, respectively^[5].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Apoptosis Analysis^[3]

Cell Line:HSB2 cellsConcentration:200 nMIncubation Time:18 hoursResult:Increased the number of early and late apoptotic cells.

Elesclomol (10 mg/kg; subcutaneous injection; every three days from post-natal day 5 to 26 and once weekly until post-natal day 54) treatment ameliorates severe cardiac pathology with a partial reduction in hypertrophy. Cardiac [Cu] increased with Elesclomol treatment from a vehicle knockout level of 34 to 55%^[4].
Elesclomol escorted copper to the mitochondria and increased cytochrome c oxidase levels in the brain. Elesclomol prevents detrimental neurodegenerative changes and improved the survival of the mottled-brindled mouse^[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:Cardiac Ctr1 knockout mice[4]Dosage:10 mg/kgAdministration:Subcutaneous injection; every three days from post-natal day 5 to 26 and once weekly until post-natal day 54Result:Ameliorated severe cardiac pathology with a partial reduction in hypertrophy.

NCT NumberSponsorConditionStart DatePhaseNCT00522834Synta Pharmaceuticals Corp.MelanomaAugust 2007Phase 3NCT00888615GOG Foundation|National Cancer Institute (NCI)Fallopian Tube Clear Cell Adenocarcinoma|Fallopian Tube Endometrioid Adenocarcinoma|Fallopian Tube Mucinous Adenocarcinoma|Fallopian Tube Serous Adenocarcinoma|Fallopian Tube Transitional Cell Carcinoma|Fallopian Tube Undifferentiated Carcinoma|Ovarian Brenner Tumor|Ovarian Clear Cell Adenocarcinoma|Ovarian Endometrioid Adenocarcinoma|Ovarian Mucinous Adenocarcinoma|Ovarian Seromucinous Carcinoma|Ovarian Serous Adenocarcinoma|Ovarian Transitional Cell Tumor|Ovarian Undifferentiated Carcinoma|Primary Peritoneal Serous Adenocarcinoma|Recurrent Fallopian Tube Carcinoma|Recurrent Ovarian Carcinoma|Recurrent Primary Peritoneal CarcinomaDecember 13, 2010Phase 2NCT00808418Synta Pharmaceuticals Corp.Prostate CancerNovember 2008Phase 1

400.52

Solid

C₁₉H₂₀N₄O₂S₂

488832-69-5

伊利司莫

Powder-20°C3 years4°C2 yearsIn solvent-80°C6 months-20°C1 month

In Vitro: 

DMSO : 100 mg/mL (249.68 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量1 mg5 mg10 mg1 mM2.4968 mL12.4838 mL24.9675 mL5 mM0.4994 mL2.4968 mL4.9935 mL10 mM0.2497 mL1.2484 mL2.4968 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

• 请依序添加每种溶剂： 50% PEG300    50% saline

  Solubility: 5 mg/mL (12.48 mM); Suspended solution; Need ultrasonic

• 2.

• 请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

  Solubility: ≥ 2.5 mg/mL (6.24 mM); Clear solution

• 3.

• 请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

  Solubility: ≥ 2.5 mg/mL (6.24 mM); Clear solution