| 包装 | 价格(元) |
| 10mM (in 1mL DMSO) | 询价 |
| 5mg | 询价 |
| 10mg | 询价 |
| 50mg | 询价 |
| 100mg | 询价 |
RRx-001 is an aerospace-derived anticancer agent with reactive nitrogen species (RNS)-generating chemistry that leads to epigenetic alterations, such as DNA methylation and histone acetylation in cancer cells.
Cell lines | Human cancer cell lines HEP-G2, HT-29, CACO-2 |
Preparation Method | The MTT proliferation assay kit was used to detect cell growth and proliferation. 5 103 cells were seeded in each well of a 96-well plate, treated with (or without) compound (RRx-001) and cultured for up to 72 h. Then 10 μL was added to each well |
Reaction Conditions | 5, 50, 100 mM RRx-001 for 72h |
Applications | RRx-001 affects glucose and G6PD enzyme activity in three different cancer cell lines namely Hep G2, CACO-2, and HT-29. In all cancer cell lines tested, RRx-001 induced G6PD inhibition in a concentration dependent fashion. |
Animal models | Nude mice, male, 7-8 weeks old and 20-25 grams in body weight |
Preparation Method | Tumors were imaged for basal FLUC, RLUC, and mRFP signals 24 h before administration of RRx-001. Following injection with RRx-001, mice were imaged for RLUC signal by intravenous injection of 50 μg of coelenterazine at 8 and 24 h post-RRx-001 treatment. |
Dosage form | 10 mg/kg RRx-001( i.v.) |
Applications | Mice were imaged for ARE-FLUC expression 24 h before and after RRx-001 administration. Results showed that a single dose of 10 mg/kg RRx-001 inhibited tumor growth and produced a tumor volume quadrupling time of 5.7±1.3 days compared to 3.3±0.7 days of vehicle control group. |
| 产品描述 | RRx-001 is an aerospace-derived anticancer agent with reactive nitrogen species (RNS)-generating chemistry that leads to epigenetic alterations, such as DNA methylation and histone acetylation in cancer cells[4,7]. 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[5]. RRx-001 also triggers p53 and p21 activity in response to double-stranded DNA breaks as well as deregulates cancer cellular energetics and metabolism[6]. Rx-001 affects glucose and G6PD enzyme activity in three different cancer cell lines namely Hep G2, CACO-2, and HT-29. In all cancer cell lines tested, RRx-001 induced G6PD inhibition in a concentration dependent fashion[1]. RRx-001 mediated nuclear translocation of Nrf2 and the activation of expression of its downstream enzymes HO-1 and NQO1 in tumor cells. Inhibition of intrinsic Nrf2 expression by Nrf2-specific siRNA increased cell sensitivity to RRx-001[2]. The increase in the synthesis and release of cytokines and the up-regulation of pro-inflammatory factors in LPS-treated microglial cells were significantly reduced by RRx-001 pretreatment. As the most classical inflammatory pathways, NF-κB and MAPK signaling pathways were activated by LPS, but were inhibited by RRx-001[9]. Molecular imaging of tumor cells co-expressing pARE-Firefly luciferase and pCMV-Renilla luciferase-mRFP in vitro and in vivo in mice revealed that RRx-001 significantly increased ARE-FLUC signal in cells in a dose- and time-dependent manner, suggesting that RRx-001 is an effective activator of the Nrf2-ARE signaling pathway[2]. RRx-001 plays a role in short-term blood flow redistribution in tumors enriched in percutaneous cells and α-SMA vessels[3]. One hour following administration of 99mTc labeled RBCs treated with 10 mg/kg RRx-001, An approximate 2.0-fold and 1.5-fold increase in 99mTc-labeled RBCs compared to vehicle control in HEPG2 and HT-29 tumor models, respectively. An approximate 40% and 36% decrease in HEP-G2 and HT-29 tumor weight, respectively, following treatment with RRx-001[8]. References: |
| 维奥蛋白资源库 - 中文蛋白资源 CopyRight © 2010-2024 |