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Efaproxiral Sodium ROS modulator

Cat.No.S4263

Efaproxiral Sodium(RSR13 Sodium) is a synthetic allosteric modifier of hemoglobin, decreases Hb-oxygen (O2) binding affinity and enhances oxygenation of hypoxic tumours during radiation therapy. This compound is used for brain metastases originating from breast cancer.
Efaproxiral Sodium ROS modulator Chemical Structure

Chemical Structure

Molecular Weight: 363.38

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Chemical Information, Storage & Stability

Molecular Weight 363.38 Formula

C20H23NO4.Na

 Storage (From the date of receipt)
CAS No. 170787-99-2 Download SDF Storage of Stock Solutions

Synonyms RSR13 Sodium Smiles CC1=CC(=CC(=C1)NC(=O)CC2=CC=C(C=C2)OC(C)(C)C(=O)[O-])C.[Na+]

Solubility

In vitro
Batch:

DMSO : 73 mg/mL (200.89 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 73 mg/mL

Ethanol : 73 mg/mL

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In vivo
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Mechanism of Action

In vitro

Efaproxiral Sodium, a synthetic allosteric modifier of hemoglobinoxygen binding affinity, has been shown to bind reversibly to hemoglobin, stabilizing the deoxyhemoglobin tetramer conformation to reduce its affinity for oxygen. [1]
In vivo

Efaproxiral Sodium plus oxygen breathing reduces the radiobiological hypoxic fraction of EMT6 tumors from the value of 24% found in both air-breathing and oxygen-breathing mice to 9% and improves the response of the tumors to radiation. Carboplatin (100 mg/kg) slowes tumor growth in air-breathing mice, producing a growth delay of 3.3 days. This compound plus oxygen increases the growth delay to 5.7 days; this is 2.4 days (71%) greater than that for carboplatin alone and 2.1 days (57%) greater than that for carboplatin plus oxygen breathing. This chemical plus oxygen breathing, therefore, improves the tumor growth delay obtained with 100 mg/kg carboplatin to or beyond that obtained with the highly toxic dose of 150 mg/kg carboplatin, but does so without increasing the toxicity beyond that seen with 100 mg/kg carboplatin in air-breathing mice.[1] It significantly increases tumor oxygenation by 8.4 to 43.4 mmHg within 5 days in C3H mice with RIF-1 tumors, with maximum increases at 22-31 min after treatment. This compound plus oxygen plus Radiation produces tumor growth inhibition throughout the treatment duration in C3H mice with RIF-1 tumors, and inhibition is significantly different from radiation plus oxygen from day 3 to day 5. [2]
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00433472 Withdrawn
Brain and Central Nervous System Tumors
Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins|National Cancer Institute (NCI)
 Not Applicable

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