Efaproxiral Sodium

SKU: orb1300730

Description

Efaproxiral Sodium (RSR13 sodium) is a synthetic small molecule allosteric effector of hemoglobin. It has been investigated in preclinical and clinical research for its potential to sensitize hypoxic tumors, such as breast cancer-derived brain metastases, to radiation therapy.

Research Area

Immunology & Inflammation, Metabolism Research, Signal Transduction

Key Properties

• CAS Number: 170787-99-2
• MW: 363.38
• Purity: 99.41% (May vary between batches)
• Formula: C₂₀H₂₃NO₄·Na
• SMILES: [Na+].Cc1cc(C)cc(NC(=O)Cc2ccc(OC(C)(C)C([O-])=O)cc2)c1
• Target: ROS,Reactive Oxygen Species
• Solubility: H2O:67 mg/mL (184.38 mM);DMSO:68 mg/mL (187.13 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.5 mM);Ethanol:68 mg/mL (187.13 mM)

Bioactivity

• In Vivo:
  Efaproxiral 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. Efaproxiral 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. Efaproxiral 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. Efaproxiral 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. Efaproxiral 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.
• In Vitro:
  Efaproxiral, 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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Efaproxiral, Efaproxiral Sodium, hemoglobin, Inhibitor, inhibit, ReactiveOxygenSpecies, Reactive Oxygen Species, RSR-13, RSR13, RSR13 sodium, RSR 13

Compound Identifiers

PubChem CID

2725048