Temozolomide（T127425 ≥98%, T408143 10mM in DMSO） is an alkylating chemotherapeutic agent widely used in the treatment of several cancers. Like other alkylating agents, it exerts its cytotoxic effect by transferring alkyl groups to DNA, primarily at the N7 and O6 positions of guanine and the N3 position of adenine. This DNA modification disrupts normal replication and repair. Because cancer cells divide more rapidly and often with reduced error-correction capacity compared to healthy cells, they are particularly vulnerable to temozolomide-induced DNA damage.
Temozolomide is well established as a standard therapy for several malignancies, including oligodendrocytoma, melanoma and Glioblastoma multiforme (GBM).
Recent research has highlighted improved outcomes when temozolomide is combined with MGMT Inhibitors:
• Temozolomide efficacy is limited by O6-methylguanine DNA methyltransferase (MGMT), an enzyme that repairs alkylated DNA lesions. Co-administration with MGMT inhibitors such as Lomeguatrib (L125047 ≥98%, L422355 10mM in DMSO) or O6-Benzylguanine (B101579 ≥98%, O422422 10mM in DMSO) enhances therapeutic effectiveness by preventing DNA repair.
• In glioblastoma models, the combination of temozolomide and Epigallocatechin Gallate (E107404 ≥98%, E107403 analytical standard, E409009 10mM in DMSO, EGCG-a polyphenol from green tea) has been shown to extend survival compared to temozolomide alone. EGCG enhances efficacy by inhibiting GRP78, an endoplasmic reticulum chaperone linked to tumor survival and therapy resistance.
References:
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