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Efaproxiral Sodium

Name: Efaproxiral Sodium
Brand: Selleck Chemicals
SKU: S4263

Synonyms: RSR13 Sodium

Catalog No.S4263 Purity: 99.99%

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. Efaproxiral Sodium is used for brain metastases originating from breast cancer.

Efaproxiral Sodium Chemical Structure

CAS: 170787-99-2

Purity & Quality Control

Batch: Purity: 99.99%

99.99

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Biological Activity

Description	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. Efaproxiral Sodium is used for brain metastases originating from breast cancer.

In vitro
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. ^[1]

In Vivo
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.^[1] 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. ^[2]

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
NCT00433472	Withdrawn	Brain and Central Nervous System Tumors	Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins\|National Cancer Institute (NCI)		Not Applicable

References

Chemical lnformation & Solubility

Molecular Weight	363.38	Formula	C₂₀H₂₃NO₄.Na
CAS No.	170787-99-2	SDF	Download Efaproxiral Sodium SDF
Smiles	CC1=CC(=CC(=C1)NC(=O)CC2=CC=C(C=C2)OC(C)(C)C(=O)[O-])C.[Na+]
Storage (From the date of receipt)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

DMSO : 73 mg/mL ( (200.89 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 73 mg/mL

Ethanol : 73 mg/mL

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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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