Cladribine CAS Registry Number: 4291-63-8 克拉利宾
CAS Name: 2-Chloro-2'-deoxyadenosine
Additional Names: 2-chloro-6-amino-9-(2-deoxy-b-D-erythro-pentofuranosyl)purine; 2-chlorodeoxyadenosine; 2-CdA; CldAdoTrademarks: Leustatin (Ortho Biotech)
Percent Composition: C 42.04%, H 4.23%, Cl 12.41%, N 24.51%, O 16.80%
📌 参考资料/链接：
Literature References: Substituted purine nucleoside with antileukemic activity. Prepn as intermediate in synthesis of 2-deoxynucleosides: H. Venner, Ber. 93, 140 (1960); M. Ikehara, H. Tada, J. Am. Chem. Soc. 85, 2344 (1963); eidem, ibid. 87, 606 (1965). Synthesis and biological activity: L. F. Christensen et al., J. Med. Chem. 15, 735 (1972). Stereospecific synthesis: Z. Kazimierczuk et al., J. Am. Chem. Soc. 106, 6379 (1984); R. K. Robins, G. R. Revankar, EP 173059; eidem, US 4760137 (1986, 1988 both to Brigham Young Univ.). Specific toxicity to lymphocytes: D. A. Carson et al., Proc. Natl. Acad. Sci. USA 77, 6865 (1980); eidem, Blood 62, 737 (1983). Mechanism of action: S. Seto et al., J. Clin. Invest. 75, 377 (1985). Clinical evaluation in chronic lymphocytic leukemia: L. D. Piro et al., Blood 72, 1069 (1988); in hairy cell leukemia: eidem, N. Engl. J. Med. 322, 1117 (1990).
📄 详细内容
Properties: Crystals from water, softens at 210-215°, solidifies and turns brown (Christensen). Also reported as crystals from ethanol, mp 220° (softens), resolidifies, turns brown and does not melt below 300° (Kazimierczuk). [a]D25 -18.8° (c = 1 in DMF). uv max in 0.1N NaOH: 265 nm; in 0.1N HCl: 265 nm.
Melting point: mp 220° (softens), resolidifies, turns brown and does not melt below 300°
Optical Rotation: [a]D25 -18.8° (c = 1 in DMF)
Absorption maximum: uv max in 0.1N NaOH: 265 nm; in 0.1N HCl: 265 nm
Therap-Cat: Antineoplastic.
Keywords: Antineoplastic; Antimetabolites; Purine Analogs.
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