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KI1001Thiotepa1 g$300

Chemical Characteristic

Product NameThiotepa
SynonymsThioplex
CAS No.52-24-4
Molecular Weight 189.22
FormulaC6H12N3PS
Chemical NameTris(1-aziridinyl)phosphine sulfide
SmilesS=P(N1CC1)(N1CC1)N1CC1
Chemical Structure

Biological activities

Thiotepa is an alkylating agent used to treat cancer. Thiotepa has been used in the palliation of a wide variety of neoplastic diseases and used as intravesical chemotherapy in bladder cancer. Thiotepa is metabolized in human liver microsomes by CYP3A4 (major) and CYP2B6 (minor).[1] In vitro chemosensitivity studies, plasma levels of the thiotepa 's primary metabolite, TEPA, is sufficient to induce significant cell kills in all three tumour lines derived from three histologically different murine colon tumours (MAC).[2] With human bladder cancer cells in culture, cytotoxicity of thiotepa is increased up to 10-fold by posttreatment with pentoxifylline. Furthermore, with human bladder or breast cancer xenografts in a modified subrenal capsule assay, enhancement of thiotepa is also observed by in vivo posttreatment with pentoxifylline.[3]

Protocols

In vivo: Thiotepa is dissolved in 0.9% NaCl solution.[3]

References

[1] Jacobson PA, et al. Cytochrome P450 isozymes 3A4 and 2B6 are involved in the in vitro human metabolism of thiotepa to TEPA. Cancer Chemother Pharmacol. 2002, (6): 461-467.
[2] Phillips RM, et al. Experimental correlations of in vitro drug sensitivity with in vivo responses to ThioTEPA in a panel of murine colon tumours. Cancer Chemother Pharmacol. 1988, 21(2): 168-172.
[3] Fingert HJ, et al. In vivo and in vitro enhanced antitumor effects by pentoxifylline in human cancer cells treated with thiotepa. Cancer Res. 1988, 48(15): 4375-4381.

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