货号：T2046

储存条件：粉末-20°C可保存3年；液体-80°C可保存12月。

产品描述

DNA damage is an abnormal chemical structure in DNA, while a mutation is a change in the sequence of standard base pairs. DNA damages cause changes in the structure of the genetic material and prevent the replication mechanism from functioning and performing properly. Temozolomide is converted to the active metabolite 5-(3-methyltriazen-1-yl) imidazole-4-carboxamide (MTIC) by non-enzymatic chemical conversion that produces DNA damage. In vitro, temozolomide exhibited anti-proliferation to human malignant glioma cell lines U373MG, U87MG, and T98G with IC₅₀ values of 40, 30 and 350 μM, respectively. Temozolomide induced apoptosis in the MGMT expressing cells occurred through AKT-Glycogen-Synthase-Kinase-3β signaling and is mediated by myelocytomatosis oncoprotein. Temozolomide treatment at concentration of 100 mM for 72h increased the population at the G2/M phase and decreased the population at the G1 phase in all malignant glioma cells. In addition, temozolomide induced autophagy in U373-MG cells. In vivo, administration of 40 mg/kg temozolomide significantly increased survival times in a B16F10 mouse metastatic melanoma model. Treatment with temozolomide at dose of 2.5 mg/kg daily for 4 weeks resulted in a 78.30% tumor suppression, and reduced microvessel density in the glioblastoma orthotopic xenograft model.

产品信息