For research use only. Not for therapeutic Use.
Efaproxiral is a haemoglobin (Hb) synthetic allosteric modifier, decreases Hb-oxygen (O2) binding affinity and enhances oxygenation of hypoxic tumours during radiation therapy [1].
Efaproxiral binds to only one pair of symmetry-related sites in the Hb central water cavity[2].
Efaproxiral readily crosses the red cell membrane in the presence of serum albumin solutions[2].
Efaproxiral is not inhibited from entering erythrocytes in the presence of an anion-channel blocking agent (DIDS)[2].
Efaproxiral (150 mg/kg, i.p.) increase tumor oxygenation，and increase the tumor growth inhibition of radiotherapy over 5 days of treatment[3].
Efaproxiral reduces hemoglobin-oxygen binding affinity, which facilitates oxygen release from hemoglobin into surrounding tissues and potentially increases the pO(2) of the tumors[4]
| Catalog Number | I001195 |
| CAS Number | 131179-95-8 |
| Synonyms | 2-[4-[2-(3,5-dimethylanilino)-2-oxoethyl]phenoxy]-2-methylpropanoic acid |
| Molecular Formula | C20H23NO4 |
| Purity | ≥95% |
| InChI | InChI=1S/C20H23NO4/c1-13-9-14(2)11-16(10-13)21-18(22)12-15-5-7-17(8-6-15)25-20(3,4)19(23)24/h5-11H,12H2,1-4H3,(H,21,22)(H,23,24) |
| InChIKey | BNFRJXLZYUTIII-UHFFFAOYSA-N |
| SMILES | CC1=CC(=CC(=C1)NC(=O)CC2=CC=C(C=C2)OC(C)(C)C(=O)O)C |
| Reference | [1]. Stea B, et al. Efaproxiral red blood cell concentration predicts efficacy in patients with brain metastases. Br J Cancer. 2006 Jun 19;94(12):1777-1784. [2]. Abraham DJ, et al. Allosteric modifiers of hemoglobin: 2-[4-[[(3,5-disubstituted anilino)carbonyl]methyl]phenoxy]-2-methylpropionic acid derivatives that lower the oxygen affinity of hemoglobin in red cell suspensions, in whole blood, and in vivo in rats. [3]. Hou H, et al. The effects of Efaproxyn (efaproxiral) on subcutaneous RIF-1 tumor oxygenation and enhancement of radiotherapy-mediated inhibition of tumor growth in mice. Radiat Res. 2007 Aug;168(2):218-25. [4]. Hou H, et al. Increased oxygenation of intracranial tumors by efaproxyn (efaproxiral), an allosteric hemoglobin modifier: In vivo EPR oximetry study. Int J Radiat Oncol Biol Phys. 2005 Apr 1;61(5):1503-9. |
