RRx-001
目录号: PL08875 纯度: ≥99%
CAS No. :925206-65-1
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中文名称
RRx-001
中文别名
RRX-001;2-溴-1-(3,3-二硝基-1-氮杂环丁基)乙酮
英文名称
RRx-001
英文别名
RRx-001;2-bromo-1-(3,3-dinitroazetidin-1-yl)ethanone;RRx001;2-BROMO-1-(3,3-DINITROAZETIDIN-1-YL)ETHAN-1-ONE;7RPW6SU9SC;Ethanone, 2-bromo-1-(3,3-dinitro-1-azetidinyl)-;1-bromoacetyl-3,3-dinitroazetidine;BCP19228;s8405;DB12060;AK00777061;Q27268765
Cas No.
925206-65-1
分子式
C5H6BrN3O5
分子量
268.02
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
RRx-001 是一种低氧选择性的表观遗传因子,被用作放射或化疗敏感剂,能诱发凋亡,克服骨髓瘤的耐药性。RRx-001 具有有效的抗癌活性且毒性极低。RRx-001是一个免疫检查点的抑制剂,可下调 CD47 和SIRP-α。RRx-001是G6PD的有效抑制剂,具有较强的抗疟活性。
生物活性
RRx-001, a hypoxia-selective epigenetic agent and studied as a radio- and chem-sensitizer, triggers apoptosis and overcomes drug resistance in myeloma. RRx-001 exhibits potent anti-tumor activity with minimal toxicity. RRx-001 is a dual small molecule checkpoint inhibitor by downregulating CD47 and SIRP-α. RRx-001 is a potent inhibitor of G6PD and shows potent antimalarial activity.
性状
Solid
体外研究(In Vitro)
RRx-001 (0-5 μM, 24 hours) inhibits MM cells growth and overcomes resistance to novel and conventional therapies.
RRx-001 blocks migration of MM cells and associated angiogenesis.
RRx-001 induces significant G1 phase growth arrest, with concomitant decrease in S phase. RRx-001 triggers significant apoptosis in MM cells.
RRx-001 inhibits DNA methylation by downregulating DNA methytransferases.
RRx-001 and the supernatant of RRx-001-treated macrophages downregulates CD47 on tumor cells and SIRPα on macrophages.
has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
RRx-001 (5 mg/kg or 10 mg/kg, I.V., thrice-weekly for 24 days) inhibits tumor growth and prolongs survival in a xenograft mouse model.
RRx-001 (10?mg/kg, IP, twice a week and once a day) exhibits potent anti-cancer activity on the A549 lung cancer model dependent on the presence of tumor-associated macrophages (TAMs) in tumor tissue. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
ClinicalTrial
参考文献
[1]. Das DS, et al. A novel hypoxia-selective epigenetic agent RRx-001 triggers apoptosis and overcomes drug resistance in multiple myeloma cells. Leukemia. 2016 Nov;30(11):2187-2197.
[2]. Yalcin O, et al. From METS to malaria: RRx-001, a multi-faceted anticancer agent with activity in cerebral malaria. Malar J. 2015 May 28;14:218.
溶解度数据
In Vitro: DMSO : ≥ 100 mg/mL (373.11 mM)配制储备液
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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