替莫唑胺 T1178

Product Introduction
Bioactivity


英文名: Temozolomide

描述: 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。

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].

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]

存储条件: keep away from direct sunlightPowder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: PBS : 5 mg/mL (25.75 mM)
DMSO : 28.83mg/ml (200 mM)


关键字: DNA Alkylator/Crosslinker | Inhibitor | Apoptosis | Temozolomide | inhibit | CCRG-81045 | NSC362856 | NSC-362856 | Autophagy | CCRG81045

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相关库: Drug Repurposing Compound Library | Anti-Cancer Compound Library | Anti-Cancer Drug Library | Anti-Cancer Clinical Compound Library | Pediatric Drug Library | Anti-Cancer Approved Drug Library | Anti-Cancer Active Compound Library | Traditional Chinese Medicine Monomer Library | Tyrosine Kinase Inhibitor Library | EMA Approved Drug Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途