Busulfan
Busulfan is an alkyl sulfonate that exhibits anticancer chemotherapeutic activity. Busulfan is an alkylating agent that attaches an alkyl group to the N7 position of guanine bases, inhibiting DNA replication; it is clinically used to treat chronic myelogenous leukemia (CML). In vitro, busulfan inhibits growth of promyelocytic leukemia cells. This compound may also induce senescence in normal cells through activation of ERK and p38 MAPK signaling.
References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18845326
| Cas No. |
55-98-1 |
|---|---|
| Purity |
≥98% |
| Formula |
C6H14O6S2 |
| Formula Wt. |
246.30 |
| Chemical Name |
1,4-Butanediol dimethanesulfonate esters |
| IUPAC Name |
4-methylsulfonyloxybutyl methanesulfonate |
| Synonym |
Busulphan |
| Melting Point |
287°C |
| Solubility |
Soluble in acetone (22 mg/mL), ethanol, or DMSO. Insoluble in water. |
| Appearance |
White crystalline powder |
Galaup A, Paci A. Pharmacology of dimethanesulfonate alkylating agents: busulfan and treosulfan. Expert Opin Drug Metab Toxicol. 2013 Mar;9(3):333-47. PMID: 23157726.
Probin V, Wang Y, Zhou D. Busulfan-induced senescence is dependent on ROS production upstream of the MAPK pathway. Free Radic Biol Med. 2007 Jun 15;42(12):1858-65. PMID: 17512465.
Frame D. Chronic myeloid leukemia: standard treatment options. Am J Health Syst Pharm. 2006 Dec 1;63(23 Suppl 8):S10-4; quiz S21-2. PMID: 17106015.
Iwamoto T, Hiraku Y, Oikawa S, et al. DNA intrastrand cross-link at the 5-GA-3 sequence formed by busulfan and its role in the cytotoxic effect. Cancer Sci. 2004 May;95(5):454-8. PMID: 15132775.
