Temozolomide
作者：齐岳
发布时间：2023-09-05
08:51:43
点击数：
产品名称：Temozolomide
产品描述：
| 产品描述 | Temozolomide is a DNA alkylating agent interfering with DNA replication. | ||||||||||||||||
| 体外活性 | The cytotoxic/mutagenic effects of temozolomide are based on the presence of DNA O(6)-methylguanine adducts that generate base/base mismatches with cytosine and with thymine. These adducts lead to cell death, or if the cell survives, provoke somatic point mutations represented by C:G-->T:A transition in DNA helix [1]. The IC50 values for Temozolomide (TMZ) in different cell lines were ranging from 14.1 to 234.6 μM: cell lines with low IC50 values (< 50 μM), which included A172 (14.1 μM) and LN229 cells (14.5 μM), and those with high IC50 values (> 100 μM), which included SF268 (147.2 μM) and SK-N-SH cells (234.6 μM) [2]. TMZ sensitivity of both chemo-sensitive and resistant cells was enhanced significantly under hyperoxia. At the cell line-specific optimum oxygen concentration (D54-R, 80 %; U87-R, 40 %), resistant cells had the same response to TMZ as the parent chemosensitive cells under normoxia via the caspase-dependent pathway [3].
| ||||||||||||||||
| 体内活性 | No drug-related death occurred in mice treated with TZM (100 or 200 mg/kg) or with NU1025 ± TZM and that the maximal weight loss was 12%. Intracranial injection of NU1025, immediately before the administration of 100 or 200 mg/kg TZM, significantly increased lifespans with respect to controls or to groups treated with TZM only [4]. Co-administration of AG-014699 with temozolomide resulted in complete tumour regressions in all mice, of which three out of five were sustained throughout the experiment. The MMR-defective D283Med xenografts grew very rapidly (median time to RTV4=7 days) and showed very little response to temozolomide alone (TGD of only 2 days) with no regressions observed in any mice [5].
| ||||||||||||||||
| 细胞实验 | Cell lines exposed to TMZ (with or without 5-Aza or O6-BG pre-treatment) were grown in 24-well plates under standard culture conditions for 6 days. Cytotoxicity was determined using the sulphorhodamine-B (SRB) method. Briefly, the cells were fixed with 10% trichloroacetic acid for 20 min at 4°C then washed three times with water. After 24 hours, cells were stained for 30 min at room temperature with 0.4% SRB dissolved in 1% acetic acid and then washed three times with 1% acetic acid. The plates were air-dried and the dye solubilized with 300 ml/well of 10 mM Tris base (pH 10.5) for 10 min on a shaker. The optical density of each well was measured spectrophotometrically using a Titertek multiscan colorimeter at 492 nm [2]. | ||||||||||||||||
| 动物实验 | TZM was dissolved in dimethyl-sulfoxide (40 mg/mL), diluted in saline (5 mg/mL), and administered intraperitoneally on day 2 after tumor injection at 100 mg/kg or 200 mg/kg, doses commonly used for in vivo preclinical studies.15-17 Because cytotoxicity induced by TZM and PARP inhibitors can be improved by fractionated modality of treatment,9 in selected groups a total dose of 200 mg/kg TZM was divided in 2 doses of 100 mg/kg given on days 2 and 3. NU1025 was dissolved in polyethylene glycol-400 (40% in saline) and was injected intracranially at the maximal deliverable dose (1 mg/mouse, 0.03 mL) or, in selected groups, intraperitoneally (0.3 mL) on day 2 after tumor challenge, 1 hour before TZM administration. Control mice were injected with drug vehicles [4]. |
| 别名 | NSC 362856, TMZ, 替莫唑胺, TZM, CCRG 81045 |
| 分子量 | 194.15 |
| 分子式 | C6H6N6O2 |
| CAS No. | 85622-93-1 |
存储
| Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 9.7 mg/mL (50 mM)
( < 1 mg/mL refers to the product slightly soluble or insoluble )
联系我们：
邮箱：2519696869@qq.com
QQ: 2519696869
电话：18066853083
微信：18066853083
公司介绍：
西安齐岳生物科技有限公司是集化学科研和定制与一体的高科技化学公司。业务范围包括化学试剂和产品的研发、生产、销售等。涉及产品为通用试剂的分销、非通用试剂的定制与研发，涵盖生物科技、化学品、中间体和化工材料等领域。
主营产品：COF、MOF单体系列：三蝶烯衍生物、金刚烷衍生物、四苯甲烷衍生物、peg、上转换、石墨烯、光电材料、点击化学、凝集素、载玻片、蛋白质交联剂、脂质体、蛋白、多肽、氨基酸、糖化学等。
