Title: Vorinostat
CAS Registry Number: 149647-78-9
CAS Name: N-Hydroxy-
N¢-phenyloctanediamide
Synonyms: suberoylanilide hydroxamic acid; SAHA
Molecular Formula: C14H20N2O3
Molecular Weight: 264.32
Percent Composition: C 63.62%, H 7.63%, N 10.60%, O 18.16%
Literature References: Second generation hybrid polar compound; histone deacetylase (HDAC) inhibitor that induces cell cycle arrest, differentiation and apoptosis in tumor cells. Prepn: R. Breslow
et al., WO 9307148;
eidem, US 5369108 (1993, 1994 both to Sloan-Kettering Inst.; Columbia Univ.); J. C. Stowell
et al., J. Med. Chem. 38, 1411 (1995). Synthesis: A. Mai
et al., Org. Prep. Proceed. Int. 33, 391 (2001). HTLC determn in serum: L. Du
et al., Rapid Commun. Mass Spectrom. 19, 1779 (2005).
In vitro antiproliferative activity: P. N. Munster
et al., Cancer Res. 61, 8492 (2001).
In vivo antineoplastic activity: L. A. Cohen
et al., Anticancer Res. 22, 1497 (2002). Clinical pharmacokinetics and activity in cancer patients: W. K. Kelly
et al., J. Clin. Oncol. 23, 3923 (2005). Review of mechanism of action: V. M. Richon
et al., Blood Cells Mol. Dis. 27, 260-264 (2001); of development and therapeutic potential: R. W. Johnstone,
IDrugs 7, 674-682 (2004).
Properties: White solid, mp 159-160.5°.
Melting point: mp 159-160.5°
Therap-Cat: Antineoplastic.
Keywords: Antineoplastic.