Edatrexate

Title: Edatrexate
CAS Registry Number: 80576-83-6
CAS Name: N-[4-[1-[(2,4-Diamino-6-pteridinyl)methyl]propyl]benzoyl]-L-glutamic acid
Additional Names: 10-ethyl-10-deazaaminopterin; 10-EdAM; 10-EDAAM
Manufacturers' Codes: CGP-30694
Molecular Formula: C22H25N7O5
Molecular Weight: 467.48
Percent Composition: C 56.52%, H 5.39%, N 20.97%, O 17.11%
Literature References: Dihydrofolate reductase inhibitor. Prepn: F. M. Sirotnak, J. I. DeGraw, FR 2464956 (1981 to SRI International); J. I. DeGraw, Jr., F. M. Sirotnak, US 4369319 (1983). Synthesis: J. I. DeGraw et al., J. Med. Chem. 25, 1227 (1982); and resolution of diastereomers: eidem, ibid. 29, 1056 (1986). HPLC determn: J. J. Kinahan et al., Anal. Biochem. 150, 203 (1985); O. Van Tellingen et al., J. Chromatogr. 529, 135 (1990). Pharmacology and toxicology: M. P. Fanucchi et al., Cancer Res. 47, 2334 (1987). Clinical evaluation in non-small cell lung cancer: J. S. Lee et al, Invest. New Drugs 8, 299 (1990). Review of pharmacology and antitumor activity: F. M. Sirotnak et al., NCI Monogr. 5, 127-131 (1987).
Properties: Prepd as 1.75 H2O, uv max (pH 13): 255, 370 nm (e 30731, 7582).
Absorption maximum: uv max (pH 13): 255, 370 nm (e 30731, 7582)
Therap-Cat: Antineoplastic.
Keywords: Antineoplastic; Antimetabolites; Folic Acid Analogs/Antagonists.
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