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RRx-001
RRx-001 is a novel epigenetic modulator with potential radiosensitizing activity. It inhibits glucose 6-phosphate dehydrogenase(G6PD) in human tumor cells, binds hemoglobin and drives RBC-mediated redox reactions under hypoxia. RRx-001 triggers apoptosis and exhibits anticancer activity.RRx-001 is also a downregulator of the CD47- SIRPα checkpoint pathway.
CAS No. 925206-65-1
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RRx-001関連製品
シグナル伝達経路
Dehydrogenase阻害剤の選択性比較
生物活性
| 製品説明 | RRx-001 is a novel epigenetic modulator with potential radiosensitizing activity. It inhibits glucose 6-phosphate dehydrogenase(G6PD) in human tumor cells, binds hemoglobin and drives RBC-mediated redox reactions under hypoxia. RRx-001 triggers apoptosis and exhibits anticancer activity.RRx-001 is also a downregulator of the CD47- SIRPα checkpoint pathway. | ||
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| Targets |
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| In Vitro | ||||
| In vitro | RRx-001 exerts its anti-proliferative effect, at least partially, through interference with glucose 6 phosphate dehydrogenase (G6PD), a key enzyme in the pentose phosphate pathway, responsible for maintaining adequate levels of the major cellular reductant, NADPH. RRx-001 affects glucose and G6PD enzyme activity in three different cancer cell lines namely Hep G2, CACO-2, and HT-29. RRx-001 induced G6PD inhibition and increased glucose consumption in a concentration dependent fashion. RRx-001 induces p53 and PARP-1 via generation of ROS/RNS. It exerts anticancer activity, at least in part, by interfering with 3 crucial metabolic demands of rapidly proliferating cells: bioenergetics, macromolecular biosynthesis, and manipulation of cellular cytosolic redox homeostasis[1]. RRx-001 mediates nuclear translocation of Nrf2 and the activation of expression of its downstream enzymes HO-1 and NQO1 in tumor cells. Apart from epigenetic alterations, RRx-001 acts via pleiotropic mechanisms including redox signaling and redox-induced dysregulation of many different signal pathways such as Nrf2, p53, PARP cleavage, HIF1 alpha, and G6PD activity. It also triggers p53 and p21 activity in response to double-stranded DNA breaks as well as deregulates cancer cellular energetics and metabolism. RRx-001 is a potent activator of the Nrf2-ARE signaling pathway via ROS/RNS generation[3]. | |||
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| 細胞実験 | 細胞株 | Human cell cancer lines HEP-G2, HT-29 and CACO-2 | ||
| 濃度 | 5, 50, and 100 μM | |||
| 反応時間 | up to 72 h | |||
| 実験の流れ | Cell growth and proliferation is assessed using the MTT proliferation assay kit. Briefly, 5×103 cells are seeded in each well of a 96-well plate and cells are treated with or without compounds. Cells are cultured for up to 72 h. MTT reagent (10 μL) is added to each well, and then incubate for 3 h. Post incubation, the culture medium is removed, 100 μL Crystal Dissolving Solution is added to each well, and the absorbance of the solution is measured at 570 nm. MTT assays for samples of the same conditions are performed in triplicate. Briefly, MTT solution (0.5 mg/mL) is added, cells are incubated at 37ºC for 4 h and absorption at 540 nm is measured using a microplate reader. | |||
| In Vivo | ||
| In Vivo | RRx-001 shows promise for short-term blood flow redistribution in tumors with a pericyte- and α-SMA-rich vasculature[2]. RRx-001 monotherapy is well tolerated, with no dose-limiting toxicities. It not only facilitates nuclear translocation of Nrf2, but also upregulates endogenous Nrf2 expression in SCC VII tumors in mice[3]. | |
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| 動物実験 | 動物モデル | C3H mice/SCID mice |
| 投与量 | 15 mg/kg | |
| 投与経路 | i.v. | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT02096341 | Terminated | Malignant Solid Tumor|Lymphomas |
EpicentRx Inc. |
April 2014 | Phase 1 |
化学情報
| 分子量 | 268.02 | 化学式 | C5H6BrN3O5 |
| CAS No. | 925206-65-1 | SDF | Download RRx-001 SDFをダウンロードする |
| Smiles | C1C(CN1C(=O)CBr)([N+](=O)[O-])[N+](=O)[O-] | ||
| 保管 | |||
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In vitro |
DMSO : 54 mg/mL ( (201.47 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。) Ethanol : 14 mg/mL Water : Insoluble |
モル濃度計算器 |
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in vivo Add solvents to the product individually and in order. |
投与溶液組成計算機 | ||||
実験計算
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）
mg/kg
g
μL
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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