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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+
Chemical Structure| 925206-65-1 Chemical Structure| 925206-65-1

Structure of RRx-001
CAS No.: 925206-65-1

Chemical Structure| 925206-65-1

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

Synonyms: ABDNAZ

4.5 *For Research Use Only !

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Product Details of RRx-001

CAS No. :925206-65-1
Formula : C5H6BrN3O5
M.W : 268.02
SMILES Code : O=C(N1CC([N+]([O-])=O)([N+]([O-])=O)C1)CBr
Synonyms :
ABDNAZ
MDL No. :MFCD25976849
InChI Key :JODKFOVZURLVTG-UHFFFAOYSA-N
Pubchem ID :15950826

Safety of RRx-001

GHS Pictogram:
Signal Word:Danger
Hazard Statements:H301-H228-H341
Precautionary Statements:P501-P270-P240-P210-P241-P264-P280-P370+P378-P301+P310+P330-P405
Class:4.1(6.1)
UN#:2926
Packing Group:

Isoform Comparison

Biological Activity

Target
  • Dehydrogenase

In Vitro:

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.

In Vivo:

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

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT02096341 Malignant Solid Tumor|Lymphoma... More >>s Less << PHASE1 TERMINATED 2025-01-16 Sarah Cannon Research Institut... More >>e, Nashville, Tennessee, 37203, United States Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 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

References

 

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