keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
规格 | 价格/CNY | 货期 | 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 * 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. |
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。 结果:p53 状态和 MGMT 的表达水平与 Temozolomide 的敏感性相关。MM200 和 IgR3 (express wild-type p53 and low MGMT levels) 对 Temozolomide 显示出相当的敏感性,IC50 值分别为 23 和 22 μM,而 SK-mel-28 和 Mel-FH (mutant-type p53 and high MGMT level) 具有耐药性,IC50 值 >256 和 >247 μM。[1] 方法:黑色素瘤细胞 MM200 和 IgR3 用 Temozolomide (100 μM) 处理 24-72 h,使用 Flow Cytometry 方法检测细胞周期情况。 结果:Temozolomide 诱导 MM200 和 IgR3 细胞 的 G2/M 细胞周期停滞。[1] 方法:人胶质瘤细胞 U118 用 Temozolomide (250-500 μM) 处理 3-48 h,检测 DNA 中 m5C 水平。 结果:U118 细胞对 Temozolomide 的反应取决于反应的浓度和时间。在 Temozolomide 处理的短时间内,DNA 中 m5C 的量显著增加。m5C (R) 的量在 500 μM Temozolomide 处理 24 h 后达到最高水平。[2] |
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。 结果:AG-014699 在髓母细胞瘤体内模型中增强 Temozolomide 疗效。[3] 方法:为检测体内抗肿瘤活性,将 Temozolomide (0.9 mg/kg,口服,每天一次) 和 Aldox (16 mg/kg,静脉注射,每周一次) 给药给携带人胶质母细胞瘤 U87MG 的 Foxn1 裸鼠,每天一次,持续五周。 结果:Temozolomide 和 AldoxAldo 联合治疗诱导了显著的肿瘤体积抑制和存活率增加。[4] |
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, 替莫唑胺, TZM, CCRG 81045, TMZ |
分子量 | 194.15 |
分子式 | C6H6N6O2 |
CAS No. | 85622-93-1 |
keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 28.83mg/ml (200 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 5.1507 mL | 25.7533 mL | 51.5066 mL | 128.7664 mL |
5 mM | 1.0301 mL | 5.1507 mL | 10.3013 mL | 25.7533 mL | |
10 mM | 0.5151 mL | 2.5753 mL | 5.1507 mL | 12.8766 mL | |
20 mM | 0.2575 mL | 1.2877 mL | 2.5753 mL | 6.4383 mL | |
50 mM | 0.103 mL | 0.5151 mL | 1.0301 mL | 2.5753 mL | |
100 mM | 0.0515 mL | 0.2575 mL | 0.5151 mL | 1.2877 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Temozolomide 85622-93-1 Apoptosis Autophagy Cell Cycle/Checkpoint DNA Damage/DNA Repair DNA Alkylator/Crosslinker DNA/RNA Synthesis NSC 362856 Inhibitor inhibit CCRG-81045 NSC362856 替莫唑胺 NSC-362856 TZM CCRG81045 CCRG 81045 TMZ inhibitor