|2-溴-1-(3,3-二硝基氮杂环丁烷-1-基)乙烷-1-酮|CsnPharm

CAS No.: 925206-65-1

RRx-001/2-溴-1-(3,3-二硝基-1-氮杂环丁基)乙酮 Catalog No. CSN22557

Synonyms: ABDNAZ

RRx-001 is a potent inhibitor of glucose 6-phosphate dehydrogenase (G6PD).

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技术信息

生物活性

描述RRx-001 is a pleiotropic anticancer agent in phase III clinical trials, which polarizes tumor-associated macrophages from a low phagocytic M2 phenotype to a high phagocytic M1 phenotype. In vitro, RRx-001 was found to decrease the expression levels of CD47 and SIRPα on tumor cells and monocytes/macrophages, respectively, reducing the phagocytosis inhibitory function of the CD47/SIRPα interaction^[1]. RRx-001 has nephro-, geno- and myeloprotective effects in vivo. Importantly, RRx-001 did not protect sarcoma-180 solid tumor xenografts against cisplatin-induced cytotoxicity^[2]. RRx-001 is demonstrated to induce Nrf2 in normal tissues, mediating protection, and to downregulate the Nrf2-controlled antiapoptotic target gene, B-cell lymphoma 2 (Bcl-2) in tumors, mediating cytotoxicity^[3]. Higher doses of RRx-001 (100, 1000 micro molar) significantly decreased erythrocyte deformability under hypoxia. Co-administration of RRx-001 and nitrite under hypoxic conditions results in a significant increase in erythrocyte deformability that is related to increased NO production^[4].
参考文献

[1] Cabrales P. RRx-001 Acts as a Dual Small Molecule Checkpoint Inhibitor by Downregulating CD47 on Cancer Cells and SIRP-α on Monocytes/Macrophages. Transl Oncol. 2019 Apr;12(4):626-632
[2] Oronsky B, Reid TR, Larson C, Carter CA, Brzezniak CE, Oronsky A, Cabrales P. RRx-001 protects against cisplatin-induced toxicities. J Cancer Res Clin Oncol. 2017 Sep;143(9):1671-1677
[3] Oronsky B, Scribner C, Aggarwal R, Cabrales P. RRx-001 protects normal tissues but not tumors via Nrf2 induction and Bcl-2 inhibition. J Cancer Res Clin Oncol. 2019 Aug;145(8):2045-2050
[4] Cirrik S, Ugurel E, Aksu AC, Oronsky B, Cabrales P, Yalcin O. Nitrite may serve as a combination partner and a biomarker for the anti-cancer activity of RRx-001. Biorheology. 2019;56(4):221-235

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.7311 mL
- 18.6553 mL
- 37.3106 mL
- 5 mM
- 0.7462 mL
- 3.7311 mL
- 7.4621 mL
- 10 mM
- 0.3731 mL
- 1.8655 mL
- 3.7311 mL

技术信息

CAS号

925206-65-1

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C5H6BrN3O5

运输

蓝冰

分子量

268.02

别名

ABDNAZ

溶解度

DMSO	240.0 mg/mL (895.5 mM)
Water	insoluble

动物实验配方

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RRx-001/2-溴-1-(3,3-二硝基-1-氮杂环丁基)乙酮 Catalog No. CSN22557

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