[CAS NO. 925206-65-1] RRx-001

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PRODUCTS SPECIFICATIONS [925206-65-1]

Catalog

HY-16438

Brand

MCE

CAS

925206-65-1

DESCRIPTION [925206-65-1]

Overview

MDL	MFCD25976849
Molecular Weight	268.02
Molecular Formula	C5H6BrN3O5
SMILES	BrCC(N1CC([N+]([O-])=O)([N+]([O-])=O)C1)=O

For research use only. We do not sell to patients.

4 Publications Citing Use of MCE

Summary

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 ^[1] . RRx-001 is a dual small molecule checkpoint inhibitor by downregulating CD47 and SIRP-α ^[2] . RRx-001 is a potent inhibitor of G6PD and shows potent antimalarial activity ^[3] .

In Vitro

RRx-001 (0-5 μM, 24 hours) inhibits MM cells growth and overcomes resistance to novel and conventional therapies ^[1] .
RRx-001 blocks migration of MM cells and associated angiogenesis ^[1] .
RRx-001 induces significant G1 phase growth arrest, with concomitant decrease in S phase. RRx-001 triggers significant apoptosis in MM cells ^[1] .
RRx-001 inhibits DNA methylation by downregulating DNA methytransferases ^[1] .
RRx-001 and the supernatant of RRx-001-treated macrophages downregulates CD47 on tumor cells and SIRPα on macrophages ^[2] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay ^[1]

Cell Line:	Human MM-cell lines (MM.1S, RPMI-8226, H929, ARP1, KMS-11, OPM2, LR5, ANBL6.WT), along with drug resistant cell lines such as (MM.1R, Dox40, LR5, ANBL6.BR, RPMI-8226).
Concentration:	0-5 μM.
Incubation Time:	24 hours.
Result:	Induced a dose-dependent significant (p < 0.05) decrease in viability of all cell lines.

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 ^[1] .
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 ^[2] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	CB-17 SCID-mice were subcutaneously inoculated with 5.0 × 10 ⁶ MM.1S cells in 100 µL of serum-free RPMI 1640 medium ^[1] .
Dosage:	5 mg/kg or 10 mg/kg.
Administration:	I.V., thrice-weekly for 24 days.
Result:	Blocked MM tumor growth and enhances survival. Treatment was well tolerated, suggested by no apparent weight loss.

Animal Model:	Female BALB/c nude mice (19.2 ± 1.7 g) based on A549 lung cancer model ^[2] .
Dosage:	10 mg/kg.
Administration:	IP, twice a week and once a day.
Result:	Resulted in the most significant tumor growth retardation. Reduction of resident macrophages in tumor-bearing mice attenuates the antitumor activity of RRx-001.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT04525014	EpicentRx, Inc.\|Texas Children´s Cancer Center	Brain Tumor, Recurrent\|Brain Tumor, Pediatric\|Central Nervous System Neoplasms\|Unspecified Childhood Solid Tumor, Protocol Specific	December 1, 2022	Phase 1
NCT02801097	EpicentRx, Inc.	Malignant Solid Tumor\|Metastatic Cancer\|Advanced Cancer	August 30, 2016	Phase 1
NCT03699956	EpicentRx, Inc.	Carcinoma, Small Cell Lung	December 24, 2018	Phase 3
NCT02215512	EpicentRx, Inc.	Brain Metastases	February 6, 2015	Phase 1
NCT02489903	EpicentRx, Inc.	Small Cell Carcinoma\|Carcinoma, Non-Small-Cell Lung\|Neuroendocrine Tumors\|Ovarian Epithelial Cancer	June 2015	Phase 2
NCT02871843	EpicentRx, Inc.	Glioblastoma\|Oligodendroglioma\|Anaplastic Oligodendroglioma	February 14, 2017	Phase 1
NCT02096354	EpicentRx, Inc.	Colorectal Neoplasms	May 2014	Phase 2
NCT02452970	EpicentRx, Inc.	Cholangiocarcinoma	July 16, 2015	Phase 2
NCT02096341	EpicentRx, Inc.	Malignant Solid Tumor\|Lymphomas	April 2014	Phase 1
NCT03515538	EpicentRx, Inc.\|Prothex Pharma, Inc.	Oral Mucositis	July 12, 2018	Phase 2
NCT01359982	EpicentRx, Inc.	Malignant Solid Tumor\|Lymphomas	September 2011	Phase 1
NCT05566041	EpicentRx, Inc.\|Sciclone Pharmaceuticals (China) Co., Ltd.	Carcinoma, Small Cell Lung	August 1, 2022	Phase 3
NCT02518958	EpicentRx, Inc.	Malignant Solid Tumor\|Lymphoma	July 21, 2015	Phase 1

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : ≥ 100 mg/mL ( 373.11 mM )

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.7311 mL	18.6553 mL	37.3107 mL
5 mM	0.7462 mL	3.7311 mL	7.4621 mL
10 mM	0.3731 mL	1.8655 mL	3.7311 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.5 mg/mL (9.33 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (9.33 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.5 mg/mL (9.33 mM); Clear solution

* All of the co-solvents are available by MCE.