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RRx-001 {[allProObj[0].p_purity_real_show]}

货号:A400874 同义名: ABDNAZ

RRx-001是一种新型的表观遗传调节剂,具有潜在的放射增敏活性,能抑制葡萄糖-6-磷酸脱氢酶 (G6PD),触发凋亡,具有抗肿瘤活性,并下调 CD47 和 SIRPα 检查点通路。

HazMat Fee +

There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
RRx-001 化学结构 CAS号:925206-65-1
RRx-001 化学结构
CAS号:925206-65-1
RRx-001 3D分子结构
CAS号:925206-65-1
RRx-001 化学结构 CAS号:925206-65-1
RRx-001 3D分子结构 CAS号:925206-65-1
规格 价格 会员价 库存 数量
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RRx-001 纯度/质量文件 产品仅供科研

货号:A400874 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 Dehydrogenase 其他靶点 纯度
Trilostane 99+%
AGI-6780 +++

IDH2 R140Q mutant, IC50: 23 nM

99%+
Gimeracil 98%
AGI-5198 ++

R132H-IDH1, IC50: 70 nM

R132C-IDH1, IC50: 0.16 μM

99%+
SW033291 ++++

15-PGDH, Ki: 0.1 nM

15-PGDH, IC50: 1.5 nM

99%+
Mycophenolic acid 99+%
Fomepizole 98%
Leflunomide 98%
3-Nitropropanoic acid 99%+
Isovaleramide 99%
Mycophenolate Mofetil +++

Inosine monophosphate dehydrogenase I, IC50: 39 nM

Inosine monophosphate dehydrogenase II, IC50: 27 nM

98%
MK-8245 ++++

SCD1 (rat), IC50: 3 nM

SCD1 (mouse), IC50: 1 nM

99%+
Vidofludimus ++

Human DHODH, IC50: 134 nM

99%+
Emodin 98%
Ivosidenib 98%
NCT-501 ++

ALDH1A1, IC50: 40 nM

98%
Gossypol 99%+
Devimistat 98%
Disulfiram 98%+
Enasidenib ++++

IDH2, IC50: 12 nM

98%
PluriSIn 1 99%+
ML390 +

DHODH, IC50: 0.56 μM

99%+
Teriflunomide 99%+
Daidzin +++

ALDH-Ⅰ, Ki: 20 nM

98+%
18β-Glycyrrhetinic acid 99%
RRx-001 95%
NCT-503 +

PHGDH, IC50: 2.5 μM

99%+
Vorasidenib 99%+
Ammonium Glycyrrhizinate(x:1) 98+%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

RRx-001 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].

RRx-001 细胞实验

Cell Line
Concentration Treated Time Description References
LLC cells 100 µg/mL 12 hours To evaluate the inhibitory effect of LRT nanomedicine on calcium influx in LLC cells, results showed that LRT significantly inhibited calcium ion uptake. Nat Commun. 2023 Nov 11;14(1):7306.
LLC cells 100 µg/mL 24 hours To observe the intracellular calcium levels in LLC cells treated with LRT by CLSM, results showed a significant reduction in intracellular calcium levels. Nat Commun. 2023 Nov 11;14(1):7306.
HCT 116 colon cancer cells 0.5 µM 24 hours Induced transcription of interferon-responsive genes, sustained for up to 4 weeks post-exposure Clin Epigenetics. 2017 Jan 19;9:4.
A549 cells 2 µM 24 hours RRx-001 decreased the protein levels of CD47 and SIRPα, indicating that it disrupted the CD47-SIRPα interaction and promoted phagocytosis. Transl Oncol. 2019 Apr;12(4):626-632.
M2 polarized bone marrow-derived macrophages (BMDM) 2 µM 24 hours RRx-001 significantly increased the mRNA expression levels of M1 markers CD80 and CD86, indicating that it polarized macrophages from the M2 phenotype to the M1 phenotype. Transl Oncol. 2019 Apr;12(4):626-632.
Bone marrow-derived macrophages (BMDMs) 100-300 nM 30 minutes RRx-001 dose-dependently inhibited IL-1β secretion, caspase-1 cleavage, and cell death, indicating its inhibitory effect on NLRP3 inflammasome activation. Cell Mol Immunol. 2021 Jun;18(6):1425-1436.
HUVEC 5 µM 30 minutes To assess the adhesion of RBCs to endothelial cells after RRx-001 treatment, results showed that RRx-001 significantly increased RBC adhesion under TNFα-induced inflammation and hypoxia Int J Mol Sci. 2021 Apr 29;22(9):4713.
J82 cells 0.5-5 µM 48 hours To evaluate the cytotoxic effect of RRx-001 on bladder cancer cells, results showed that RRx-001 exhibited cytotoxic effects at 48 hours. J Exp Clin Cancer Res. 2019 Feb 20;38(1):90.
T24 cells 0.5-5 µM 48 hours To evaluate the cytotoxic effect of RRx-001 on bladder cancer cells, results showed that RRx-001 exhibited cytotoxic effects at 48 hours. J Exp Clin Cancer Res. 2019 Feb 20;38(1):90.
5637 cells 0.5-5 µM 48 hours To evaluate the cytotoxic effect of RRx-001 on bladder cancer cells, results showed that RRx-001 exhibited cytotoxic effects at 48 hours. J Exp Clin Cancer Res. 2019 Feb 20;38(1):90.
KU-19-19 cells 0.5-5 µM 48 hours To evaluate the cytotoxic effect of RRx-001 on bladder cancer cells, results showed that RRx-001 exhibited cytotoxic effects at 48 hours. J Exp Clin Cancer Res. 2019 Feb 20;38(1):90.
AU-565, MCF-7, and MDA-MB-231 breast cancer cells 2 µM 8 hours RRx-001 significantly increased the phagocytosis of breast cancer cells. Transl Oncol. 2019 Apr;12(4):626-632.

RRx-001 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
BALB/c Nude mice A549 xenograft model Intraperitoneal injection 10 mg/kg Twice a week, continuous treatment RRx-001 significantly inhibited tumor growth, but its antitumor activity was attenuated when macrophages were depleted by clodronate. Transl Oncol. 2019 Apr;12(4):626-632.
Mice HDM-induced allergic asthma model Intraperitoneal injection 10 mg/kg Injected on days 7, 9, and 11, continued until day 14 RRx-001 significantly inhibited HDM-induced airway inflammation and mucus secretion, reduced the infiltration of eosinophils, neutrophils, and lymphocytes, and decreased the levels of total IgE and HDM-specific IgE in serum. Front Immunol. 2021 Aug 3;12:718779
Mice Heterotopic GCT model Intraperitoneal injection 10 mg/kg Every other day, for three weeks RRX-001 treatment significantly inhibited the in vivo growth of GCT cells, with both tumor size and weight significantly reduced Cell Death Differ. 2023 May;30(5):1235-1246
Mice LPS-induced systemic inflammation, DSS-induced colitis, and experimental autoimmune encephalomyelitis (EAE) models Intraperitoneal injection 10 mg/kg/day Once daily for 10 days (DSS-induced colitis); every 2 days for 22 days (EAE) RRx-001 significantly alleviated the symptoms of LPS-induced systemic inflammation, DSS-induced colitis, and EAE, demonstrating its therapeutic potential in NLRP3-driven disease models. Cell Mol Immunol. 2021 Jun;18(6):1425-1436.
Mice SCCVII and U87 tumor models Intravenous injection 15 mg/kg Single dose To examine the microregional effects of RRx-001 on tumor blood flow and oxygenation, results showed that RRx-001 caused a loss of perfusion in large regions of the tumor, but perfusion recovered after 12 hours. Clin Epigenetics. 2016 May 11;8:53
C57BL/6J mice Orthotopic lung cancer model Intravenous injection 40 mg/kg Every other day, for a total of three injections To evaluate the therapeutic efficacy of LRT nanomedicine in the orthotopic lung cancer model, results showed that LRT significantly inhibited tumor growth and prolonged the survival of mice. Nat Commun. 2023 Nov 11;14(1):7306.
Mice Nu/nu mice Intravenous injection 5 mg/kg and 10 mg/kg Every 72 hours for 2 weeks To assess the localization and tumor viability of RRx-001 treated RBCs, results showed that RRx-001 treated RBCs preferentially localized to tumors and significantly reduced tumor volume Int J Mol Sci. 2021 Apr 29;22(9):4713.
CB-17 SCID mice MM.1S xenograft model Intravenous injection 5 mg/kg or 10 mg/kg Three times weekly for 24 days RRx-001 significantly inhibited tumor growth and enhanced survival Leukemia. 2016 Nov;30(11):2187-2197

RRx-001 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

RRx-001 实验方案

计算器
存储液制备 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

RRx-001 技术信息

CAS号925206-65-1
分子式C5H6BrN3O5
分子量 268.02
SMILES Code O=C(N1CC([N+]([O-])=O)([N+]([O-])=O)C1)CBr
MDL No. MFCD25976849
别名 ABDNAZ
运输蓝冰
InChI Key JODKFOVZURLVTG-UHFFFAOYSA-N
Pubchem ID 15950826
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Inert atmosphere, 2-8°C

溶解方案

DMSO: 105 mg/mL(391.76 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案 一
方案 二
方案 三
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