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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.
All products are stocked and shipped from San Francisco Bay Area, California, USA.
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All products are for research and development use only, not for any other uses, and must be handled by technically-qualified persons.
These products are explicitly not intended to be used in foods and/or cosmetics and/or drugs (human and veterinary) and/or consumer products and/or biocides and/or pesticides of any kind unless explicitly stated otherwise.
Products are not sold to individuals. We do not ship to residential addresses. Consumer orders will be cancelled without notice.
New customers undergo an internal onboarding process. As part of this process, new customers may be asked for more information. Additional restrictions may apply.
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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.
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