General
Preferred name
EFAPROXIRAL
Synonyms
GSJ61 ()
RSR13 ()
GSJ 61 ()
RSR-13 ()
Efaproxyn ()
RSR13 sodium ()
Efaproxiral (sodium) ()
RSR13 (sodium) ()
EFAPROXIRAL SODIUM ()
RSR-13 SODIUM ()
P&D ID
PD004357
CAS
131179-95-8
170787-99-2
Tags
available
drug
drug candidate
Drug indication
Lung cancer
Neoplasm
Drug Status
approved
investigational
Max Phase
3.0
Structure
Probe scores
P&D probe-likeness score
[[ v.score ]]%
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION Efaproxiral is a haemoglobin (Hb) synthetic allosteric modifier, decreases Hb-oxygen (O2) binding affinity and enhances oxygenation of hypoxic tumours during radiation therapy [1].
PRICE 29
PRICE 29
DESCRIPTION Efaproxiral sodium (RSR13 sodium) is a synthetic allosteric modifier of haemoglobin (Hb), decreases Hb-oxygen (O2) binding affinity and enhances oxygenation of hypoxic tumours during radiation therapy.;in vitro: Efaproxiral increases oxygen levels in hypoxic tumor tissues by binding non-covalently to the hemoglobin tetramer and decreasing hemoglobin-oxygen binding affinity. Increasing tumor oxygenation reduces tumor radioresistance. Efaproxiral can enhance the oxygenation of hypoxic tumours and function as a radiation sensitiser, increasing the effectiveness of RT.
DESCRIPTION synthetic small molecule with radiosensitizing activity. Efaproxiral increases oxygen levels in hypoxic tumor tissues by binding non-covalently to the hemoglobin tetramer and decreasing hemoglobin-oxygen binding affinity. Increasing tumor oxygenation reduces tumor radioresistance. One use for efaproxiral is to increase the efficacy of certain chemotherapy drugs which have reduced efficacy against hypoxic tumours, and can thus be made more effective by increased offloading of oxygen into the tumour tissues. However, no benefit was seen for efaproxiral in phase III clinical trials. (BOC Sciences Bioactive Compounds)
DESCRIPTION Efaproxiral is a synthetic small molecule with radiosensitizing activity. It is a haemoglobin synthetic allosteric modifier, decreases Hb-oxygen (O2) binding affinity and enhances oxygenation of hypoxic tumours during radiation therapy. Efaproxiral is also an allosteric modulator of Free fatty acid receptor 1, EC50 = 14.2 nM. (Enamine Bioactive Compounds)
DESCRIPTION Efaproxiral (RSR13) is a hemoglobin allosteric modifier, a potential radiosensitizer and chemotherapy enhancer in cancer treatment, improving tumor oxygenation. (TargetMol Bioactive Compound Library)
DESCRIPTION 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. (BOC Sciences Bioactive Compounds)
DESCRIPTION Efaproxiral Sodium (RSR13 sodium), a synthetic allosteric modifier of hemoglobin, is utilized for brain metastases originating from breast cancer. (TargetMol Bioactive Compound Library)
Compound Sets
18
AdooQ Bioactive Compound Library
A12323
BOC Sciences Bioactive Compounds
efaproxiral-cas-131179-95-8-item-84-83062
efaproxiral-sodium-cas-170787-99-2-item-84-85639
Cayman Chemical Bioactives
28294
ChEMBL Drugs
CHEMBL18901
CHEMBL2107744
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugBank
DB08486
DrugCentral
4465
DrugCentral Approved Drugs
4465
DrugMAP
DMX7BM4
DrugMatrix
Enamine Bioactive Compounds
EBC-209030
JUMP-Target 1 Compound Set
122335
MedChem Express Bioactive Compound Library
HY-13619
HY-13619A
Other bioactive compounds
ReFrame library
Selleckchem Bioactive Compound Library
efaproxiral-sodium
TargetMol Bioactive Compound Library
T21318
T6482
External IDs
44
Properties
(calculated by RDKit )
Molecular Weight
341.16
Hydrogen Bond Acceptors
3
Hydrogen Bond Donors
2
Rotatable Bonds
6
Ring Count
2
Aromatic Ring Count
2
cLogP
3.73
TPSA
75.63
Fraction CSP3
0.3
Chiral centers
0.0
Largest ring
6.0
QED
0.84
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Pathway
NF-¦ÊB
Immunology/Inflammation
Metabolic Enzyme/Protease
NF-κB
Metabolism
Target
ROS
hemoglobin
Reactive Oxygen Species
HBA1, HBB
HBB
Reactive Oxygen Species (ROS)
MOA
hemoglobin oxygen release stimulant
Source data