aladdin 阿拉丁 E408561 Elesclomol (STA-4783) 488832-69-5 10mM in DMSO

中文名：Elesclomol (STA-4783)

英文名：Elesclomol (STA-4783)

英文别名：N1',N3'-dimethyl-N1',N3'-di(phenylcarbonothioyl)malonohydrazide

纯度：10mM in DMSO

货号：E408561

包装：1ml

Cas号：488832-69-5

存储温度：-80℃储存

产品介绍：

Information

Elesclomol (STA-4783) Elesclomol (STA-4783) is a novel potent oxidative stress inducer that elicits pro-apoptosis events among tumor cells. Phase 3.
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.
Cell Data

cell lines：

Concentrations：Dissolved in DMSO at a concentration of 10 mM, final concentrations ~500 nM

Incubation Time：18, or 24 hours

Powder Purity:≥99%

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