RRx-001

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Chemical Structure| 925206-65-1 同义名 : ABDNAZ
CAS号 : 925206-65-1
货号 : A400874
分子式 : C5H6BrN3O5
纯度 : 95%
分子量 : 268.02
MDL号 : MFCD25976849
存储条件：

Pure form Inert atmosphere, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：
生物活性
靶点

  • Dehydrogenase
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.73mL

0.75mL

0.37mL

18.66mL

3.73mL

1.87mL

37.31mL

7.46mL

3.73mL
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