替莫唑胺-d3 (NSC 362856-d3) 是氘标记的替莫唑胺。替莫唑胺 (NSC 362856) 是一种口服活性 DNA 烷化剂，可穿过血脑屏障。替莫唑胺也是一种促自噬和促凋亡剂。替莫唑胺可有效对抗以低水平的 O6-烷基鸟嘌呤 DNA 烷基转移酶 (OGAT) 和功能性错配修复系统为特征的肿瘤细胞。替莫唑胺具有抗肿瘤和抗血管生成作用。
货号:ajcx23574
CAS:208107-14-6
分子式:C6H3D3N6O2
分子量：197.2
溶解度:DMF: 5 mg/ml,DMSO: 5 mg/ml,PBS (pH 7.2): 0.33 mg/ml
纯度：98%
存储：Store at -20°C
库存：现货

Background:

Temozolomide-d₃(TMZ-d₃) contains three deuterium atoms located on the methyl group. It is intended for use as an internal standard for the quantification of temozolomide by GC- or LC-MS. TMZ is an imidazotetrazine that is converted to a compound capable of alkylating DNA, thus interfering with DNA replication and leading to cytotoxicity in proliferating cells.¹TMZ is rapidly and completely absorbed from the gastrointestinal tract after oral administration and readily crosses the blood-brain barrier.¹Formulations containing TMZ are effective in a variety of types of cancer, including aggressive brain cancers.^1,2,3

1.Marchesi, F., Turriziani, M., Tortorelli, G., et al.Triazene compounds: Mechanism of action and related DNA repair systemsPharmacol. Res.56(4)275-287(2007) 2.Khan, O.A., Ranson, M., Michael, M., et al.A phase II trial of lomeguatrib and temozolomide in metastatic colorectal cancerBr. J. Cancer98(10)1614-1618(2008) 3.Daniel, R.A., Rozanska, A.L., Mulligan, E.A., et al.Central nervous system penetration and enhancement of temozolomide activity in childhood medulloblastoma models by poly(ADP-ribose) polymerase inhibitor AG-014699Br. J. Cancer103(10)1588-1596(2010)