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Temozolomide 替莫唑胺; NSC 362856; CCRG 81045; TMZ

Temozolomide (NSC 362856) 是一种可透过血脑屏障的口服活性的 DNA 烷基化 (DNA alkylating) 剂。Temozolomide 也是一种促自噬 (autophagy) 和促凋亡剂 (apoptosis)。Temozolomide 对以低水平的 O6-烷基鸟嘌呤 DNA 烷基转移酶 (OGAT) 和功能失配修复系统为特征的肿瘤细胞有效。Temozolomide 具有抗肿瘤和抗血管生成作用。

  • 货号:
    TK0248
  • 规格:
    10mg
    50mg
    100mg
  • 价格:
    0.00

产品参数

CAS No.85622-93-1
生物活性Temozolomide (NSC 362856) is an oral active DNA alkylating agent that crosses the blood-brain barrier. Temozolomide is also a proautophagic and proapoptotic agent. Temozolomide is effective against tumor cells that are characterized by low levels of O6-alkylguanine DNA alkyltransferase (OGAT) and a functional mismatch repair system. Temozolomide has antitumor and antiangiogenic effects.
分子式C6H6N6O2
分子量194.15
运输条件Room temperature in continental US; may vary elsewhere.
储存条件-20°C, protect from light, stored under nitrogen
溶解性数据DMSO : 20.83 mg/mL (107.29 mM; Need ultrasonic) H2O : 2.86 mg/mL (14.73 mM; Need ultrasonic)
体内研究Temozolomide (TZM), as a single agent, does not significantly increase mdian survival time (MST) with respect to control. Noteworthy, intracranial injection of NU1025, immediately before the administration of 100 or 200 mg/kg Temozolomide, significantly increases lifespans with respect to controls or to groups treated with Temozolomide only. When Temozolomide is fractionated, the increase in lifespan (ILS) obtained with this schedule is higher than that observed when NU1025 is combined with a single injection of Temozolomide (statistical comparison of survival curves: NU1025 intracranially+Temozolomide 100 mg/kg×2 vs NU1025+Temozolomide 200 mg/kg; P=0.023).
体外研究Temozolomide (TZM) is a methylating agent that crosses the blood-brain barrier and is indicated for malignant gliomas and metastatic melanomas. Temozolomide is effective against tumor cells that are characterized by low levels of O-alkylguanine DNA alkyltransferase (OGAT) and a functional mismatch repair system (MR). Determination of the IC50 for Temozolomide (TZM) in different cell lines gave values ranging from 14.1 to 234.6 μM that fell into two clearly differentiated groups: cell lines with low IC50 values (<50 μM), which include A172 (14.1±1.1 μM) and LN229 cells (14.5±1.1 μM), and those with high IC50 values (>100 μM), which include SF268 (147.2±2.1 μM) and SK-N-SH cells (234.6±2.3 μM).
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纯度及产品资料98%