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Elesclomol

Cat. No. M2083
Elesclomol Structure
Synonym:

STA-4783

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
2mg USD 40  USD40 In stock
5mg USD 56  USD56 In stock
10mg USD 90  USD90 In stock
50mg USD 185  USD185 In stock
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Quality Control & Documentation
Biological Activity

Elesclomol (STA-4783) is a novel oxidative stress inducer that acts on tumor cells and promotes their apoptosis, and is a strong copper ion-carrier that can be used for cuproptosis studies. By Affymetrix microarray analysis, Elesclomol significantly induced the expression of heat shock stress response genes and metallothionein genes in Hs294T cells treated at 100 nM for 6 h. Ramos Burkitt's lymphoma B cells were treated with Elesclomol (100 nM) for 1 h and 6 h, respectively, and the Hsp70 RNA level was rapidly increased by 4.8 times and 160 times, which was consistent with the intracellular ROS content. After 0.5 h and 6 h Elesclomol treatment, ROS content increased by 20% and 385%, respectively. Antioxidant N-acetylcysteine (NAC) and Tiron pretreatment could inhibit the induction of Hsp70. HSB2 cells treated with 200 nM Elesclomol for 18 h could induce oxidative stress and increase the apoptotic cells in early stage and late stage by 3.7 times and 11 times, respectively. The above effects could be completely inhibited by NAC, but had no effect on normal cells.

Chemical Information
Molecular Weight 400.52
Formula C19H20N4O2S2
CAS Number 488832-69-5
Solubility (25°C) DMSO 40 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

References

[1] Blackman RK, et al. PLoS One. Mitochondrial electron transport is the cellular target of the oncology drug elesclomol.

[2] Qu Y, et al. Breast Cancer Res Treat. Elesclomol, counteracted by Akt survival signaling, enhances the apoptotic effect of chemotherapy drugs in breast cancer cells.

[3] Kirshner JR, et al. Mol Cancer Ther. Elesclomol induces cancer cell apoptosis through oxidative stress.

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Keywords: Elesclomol, STA-4783 supplier, Cuproptosis, inhibitors, activators


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