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BIOLOGICAL INFO
Solubility:
50mg/1ml in 10% NaOH; clear light green solution
Form:
Free base
Research Area:
Cancer
REVIEW Thioguanine competes with hypoxanthine and guanine for the enzyme hypoxanthine-guanine phosphoribosyltransferase (HGPRTase) and is itself converted to 6-thioguanilyic acid (TGMP), which reaches high intracellular concentrations at therapeutic doses. TGMP interferes with the synthesis of guanine nucleotides by its inhibition of purine biosynthesis by pseudofeedback inhibition of glutamine-5-phosphoribosylpyrophosphate amidotransferase, the first enzyme unique to the de novo pathway of purine ribonucleotide synthesis. TGMP also inhibits the conversion of inosinic acid (IMP) to xanthylic acid (XMP) by competition for the enzyme IMP dehydrogenase. Thioguanine nucleotides are incorporated into both the DNA and the RNA by phosphodiester linkages, and some studies have shown that incorporation of such false bases contributes to the cytotoxicity of thioguanine. Its tumor inhibitory properties may be due to one or more of its effects on feedback inhibition of de novo purine synthesis; inhibition of purine nucleotide interconversions; or incorporation into the DNA and RNA. The overall result of its action is a sequential blockade of the utilization and synthesis of the purine nucleotides.
REFERENCES
[1]
Vora A, Mitchell CD, Lennard L, et al. (October 2006). Toxicity and efficacy of 6-thioguanine versus 6-mercaptopurine in childhood lymphoblastic leukaemia: a randomised trial. Lancet 368 (9544): 1339-48. doi:10.1016/S0140-6736(06)69558-5. PMID 17046466.
[2]
Evans WE. (2004). Pharmacogenetics of thiopurine S-methyltransferase and thiopurine therapy.. Ther Drug Monit. 26 (2): 186-91. PMID 12891528.
For research use only. Not for diagnostic or therapeutic use. Not for human use. AK Scientific, Inc. does not sell to individuals. If you are a first-time customer, please email for review at least two official business documents issued by your local jurisdiction, state/province, or country.
WARNING: Attention California residents: This product can expose you to chemicals including 6-Thioguanine, which is known to the State of California to cause birth defects or other reproductive harm. For more information, go to www.P65Warnings.ca.gov.