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Efaproxiral Sodium

Name: Efaproxiral Sodium
Brand: Selleck Chemicals
SKU: S4263
Rating: 5 (1 reviews)

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 No. 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 2024-05-22)
NCT00433472	Withdrawn	Brain and Central Nervous System Tumors	Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins\|National Cancer Institute (NCI)		Not Applicable

References

Chemical Information & 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
Batch:

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In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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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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