Elesclomol (STA-4783)

製品コード：S1052 純度：99.60%

Elesclomol (STA-4783) is a novel potent oxidative stress inducer that elicits pro-apoptosis events among tumor cells. Phase 3.Elesclomol specifically binds ferredoxin 1 (FDX1) α2/α3 helices and β5 strand and inhibits FDX1-mediated Fe-S cluster biosynthesis.Elesclomol (STA-4783) is a potent copper ionophore and can be used in the research of copper-dependent cell death (cuproptosis).

CAS No. 488832-69-5

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 35500	国内在庫あり
5mg	JPY 22000	国内在庫あり
50mg	JPY 35500	国内在庫あり
200mg	JPY 85500	国内在庫あり
1g	JPY 265500	国内在庫なし(納期7~10日)

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製品安全説明書

現在のバッチを見る：純度： 99.60%

99.60

Elesclomol (STA-4783)と併用されることが多い化合物

Genipin

Elesclomol and Genipin significantly reduce mitochondrial membrane potential and induce apoptosis in A549 cells.

Lee JH, et al. Oncol Lett. 2020;20(6):374.

Elesclomol (STA-4783)関連製品

関連ターゲット	HSP40 HSP70 HSP90 HSP105 HSF1	もっと見る
関連製品	Tanespimycin (17-AAG) Luminespib (NVP-AUY922) Ganetespib (STA-9090) Alvespimycin (17-DMAG) HCl VER155008 BIIB021 Onalespib (AT13387) NVP-BEP800 KRIBB11 SNX-2112 HA15 Zelavespib (PU-H71) HSP990 (NVP-HSP990) NMS-E973 Apoptozole XL888 PF-04929113 (SNX-5422) KNK437 Teprenone TRC051384 VER-50589 Rocaglamide VER-49009 Pimitespib (TAS-116) JG98 DTHIB KW-2478	もっと見る
関連化合物ライブラリー	Kinase Inhibitor Library Angiogenesis Related compound Library TGF-beta/Smad compound library Cytoskeletal Signaling Pathway Compound Library Anti-Cardiovascular Disease Compound Library	もっと見る

シグナル伝達経路

HSP (HSP90)シグナル伝達経路

HSP (HSP90)阻害剤の選択性比較

阻害剤	Citation	LPA1	LPA2	LPA3	LAP1	その他
Ki16425	26	++	+	++
Ki16198	1	++		++
ACT-1016-0707	0	++++			++++
BMS-986278	0	++++			++++
AM966	0	+++
ONO-7300243	1	+++
BMS-986020	0	✔				BSEP,MRP4,MDR3
AM 095	1	✔

1. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation. 2. "✔" indicates inhibitory effect, but without specific value.

Cell Data

Cell Lines	Assay Type	Concentration	活性情報	PMID
MDA-MB-435	Antitumor assay	25 mg/kg	Antitumor activity against human MDA-MB-435 cells xenografted in CD-1 nu/nu mouse assessed as tumor regression at 25 mg/kg, iv qod administered 3 times a week for 2 consecutive weeks	23937981
SW756	Growth inhibition assay		Inhibition of human SW756 cell growth in a cell viability assay, IC50=0.004131μM.	SANGER
P12-ICHIKAWA	Growth inhibition assay		Inhibition of human P12-ICHIKAWA cell growth in a cell viability assay, IC50=0.004044μM.	SANGER
他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

生物活性

製品説明

Targets

HSP70 ^[1]
(Cell-free assay)

In Vitro
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 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. ^[1] 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. ^[2] 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. ^[3]
細胞実験	細胞株	Hs294T, HSB2, and Ramos
	濃度	Dissolved in DMSO at a concentration of 10 mM, final concentrations ~500 nM
	反応時間	18, or 24 hours
	実験の流れ	Cells are treated with various concentrations of Elesclomol for 18 or 24 hours. The level of intracellular ROS is monitored using the DCFDA probe, which emits a green fluorescence on oxidation. Cell death is determined by flow cytometry of cells double stained with Annexin V/FITC and propidium iodide (PI) using a Vybrant Apoptosis assay kit.

In Vivo
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 in these models, both in terms of tumor regression and extended survival of mice. ^[4]
動物実験	動物モデル	Female CD-1 nude mice bearing established MDA435 breast cancer xenograft tumors
	投与量	~100 mg/kg
	投与経路	Intravenous injection

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT00827203	Suspended	Metastatic Solid Tumors	Synta Pharmaceuticals Corp.	January 2009	Phase 1
NCT00808418	Completed	Prostate Cancer	Synta Pharmaceuticals Corp.	November 2008	Phase 1

参考
[1] Kirshner JR, et al. Mol Cancer Ther, 2008, 7(8), 2319-2327. [2] Bair JS, et al. J Am Chem Soc, 2010, 132(15, 5469-5478. [3] Blackman RK, et al. PLoS One, 2012, 7(1), e29798. [4] Gehrmann M. Curr Opin Investig Drugs, 2006, 7(6), 574-580. [5] Tsvetkov P, et al. Science. 2022 Mar 18;375(6586):1254-1261. + 展開

参考

+ 展開

化学情報

分子量	400.5	化学式	C₁₉H₂₀N₄O₂S₂
CAS No.	488832-69-5	SDF	Download Elesclomol (STA-4783) SDFをダウンロードする
Smiles	CN(C(=S)C1=CC=CC=C1)NC(=O)CC(=O)NN(C)C(=S)C2=CC=CC=C2
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	１ケ月-20°Cin solvent

In vitro
Batch:

DMSO : 80 mg/mL ( (199.75 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : Insoluble

Ethanol : Insoluble

モル濃度計算器

in vivo Batch: Add solvents to the product individually and in order.					投与溶液組成計算機
	Clear solution	5%DMSO 1 10%PEG300 Click to order 2 85%saline	0.6mg/ml (1.50mM)	Taking the 1 mL working solution as an example, add 50 μL of 12 mg/ml clarified DMSO stock solution to 100 μL of PEG300, mix evenly to clarify it; then continue to add 850 μL of saline to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
	Clear solution	5%DMSO 1 40%PEG300 Click to order 2 5%Tween 80 Click to order 3 50%ddH2O	10.0mg/ml (24.97mM)	Taking the 1 mL working solution as an example, add 50 μL of 200 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG300 Click to order 2 5%Tween 80 Click to order 3 50%ddH2O	7.5mg/ml (18.73mM)	Taking the 1 mL working solution as an example, add 50 μL of 150 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG300 Click to order 2 5%Tween 80 Click to order 3 50%ddH2O	10.0mg/ml (24.97mM)	Taking the 1 mL working solution as an example, add 50 μL of 200 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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よくある質問（FAQ）

質問1:
How can we use the compound for in vivo mouse studies?

回答
S1052 in 1% DMSO+30% polyethylene glycol+1% Tween 80 is a suspension, it is fine for oral administration. You can also dissolve S1052 in 0.5-1% CMC-Na solution and treat the mice by oral gavage.

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