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别名 替莫唑胺, TZM, TMZ, NSC 362856, CCRG 81045
Temozolomide (TMZ) 是一种 DNA 烷基化剂,具有血脑屏障渗透性和口服活性。Temozolomide 具有抗肿瘤活性和抗血管生成活性,还可以诱导细胞凋亡和自噬。 Temozolomide 在酸性条件下稳定,在中性或微碱性条件下会发生水解。


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Temozolomide (TMZ) 是一种 DNA 烷基化剂,具有血脑屏障渗透性和口服活性。Temozolomide 具有抗肿瘤活性和抗血管生成活性,还可以诱导细胞凋亡和自噬。 Temozolomide 在酸性条件下稳定,在中性或微碱性条件下会发生水解。
| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 10 mg | ¥ 293 | 现货 | |
| 25 mg | ¥ 398 | 现货 | |
| 50 mg | ¥ 543 | 现货 | |
| 100 mg | ¥ 663 | 现货 | |
| 200 mg | ¥ 798 | 现货 | |
| 500 mg | ¥ 995 | 现货 | |
| 1 g | ¥ 1,260 | 现货 | |
| 1 mL x 10 mM (in DMSO) | ¥ 417 | 现货 |
| 产品描述 | Temozolomide (TMZ) is a DNA alkylating agent with blood-brain barrier permeability and oral activity. Temozolomide has antitumor activity and antiangiogenic activity, and also induces apoptosis and autophagy. Temozolomide is stable under acidic conditions and hydrolyzes under neutral or slightly alkaline conditions. |
| 靶点活性 | Astrocytes:> 1 mM, C6 cells:34 μM, A375 cells:> 75 μM, CTX TNA2 cells:430.6 μM, A2058 cells:35.5 μM, DBTRG-05MG cells:119.3 μM, A549 cells:> 250 μM, A431 cells:366 μM, Mel-FH cells:> 247 μM, SK-MEL-2 cells:> 256 μM, IgR3 cells:22 μM, A 172 cells:6.5 x 104 nM, B16 F10 cells:258 μM, MM200 cells:23 μM, DLD-1 cells:> 250 μM |
| 体外活性 | 方法:黑色素瘤细胞 SK-mel-28、MM200、IgR3、Mel-FH 用 Temozolomide (0-500 μM) 处理 72 h,使用 MTT 方法检测细胞活力。 |
| 体内活性 | 方法:为检测体内抗肿瘤活性,将 Temozolomide (68 mg/kg,灌胃) 和 AG-014699 (1 mg/kg,腹腔注射) 腹腔注射给携带髓母细胞瘤 D425Med、D283Med 或 D384Med 的 CD1 nu/nu 小鼠,每天一次,持续五天。 |
| 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 | 替莫唑胺, TZM, TMZ, NSC 362856, CCRG 81045 |
| 分子量 | 194.15 |
| 分子式 | C6H6N6O2 |
| CAS No. | 85622-93-1 |
| Smiles | CN1N=NC2=C(N=CN2C1=O)C(N)=O |
| 密度 | 1.97 g/cm3 |
| 存储 | store under nitrogen,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||||||||||||
| 溶解度信息 | DMSO: 30.6 mg/mL (157.61 mM), Sonication and heating are recommended. H2O: 5 mg/mL (25.75 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||||||||||||
| 体内实验配方 | PBS: 5 mg/mL (25.75 mM), Sonication is recommended. 10% DMSO+90% Saline: 2.88 mg/mL (14.83 mM), Solution. 请按顺序添加溶剂,在添加下一种溶剂之前,尽可能使溶液澄清。如有必要,可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考,体内配方并不是绝对的,请根据不同情况进行调整。 | ||||||||||||||||||||||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||||||||||||||||||||||
H2O/DMSO
DMSO
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对于不同动物的给药剂量换算,您也可以参考 更多