Efaproxiral
Title: Efaproxiral
CAS Registry Number: 131179-95-8
CAS Name: 2-[4-[2-[(3,5-Dimethylphenyl)amino]-2-oxoethyl]phenoxy]-2-methylpropanoic acid
Additional Names: 2-4-[[(3,5-dimethylanilino)carbonyl]methyl]phenoxy-2-methylpropionic acid
Manufacturers' Codes: RSR-13
Molecular Formula: C20H23NO4
Molecular Weight: 341.40
Percent Composition: C 70.36%, H 6.79%, N 4.10%, O 18.75%
Literature References: Allosteric modifier of hemoglobin (Hb). Binds in the central water cavity of the Hb molecule causing a conformational change such that bound oxygen is released more readily. Prepd not claimed: D. J. Abraham et al., US 5049695 (1991 to Center Innovative Technol.); eidem., J. Med. Chem. 34, 752 (1991). Oxygen binding affinities and mechanism of action: D. J. Abraham et al., Biochemistry 31, 9141 (1992). Effect on myocardial oxygen concentration: P. S. Pagel et al., J. Pharmacol. Exp. Ther. 285, 1 (1998). Antimetastatic effects: B. A. Teicher et al., Cancer Chemother. Pharmacol. 42, 24 (1998). Clinical pharmacokinetics and pharmacodynamics: L. Kleinberg et al., J. Clin. Oncol. 17, 2593 (1999). Clinical evaluation in brain tumor therapy: eidem, ibid. 20, 3149 (2002).
Properties: mp 85°.
Melting point: mp 85°
Therap-Cat: Antineoplastic adjunct (radiosensitizer).
Keywords: Antineoplastic Adjunct; Radiosensitizer.

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