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Temozolomide

Temozolomide

产品编号 T1178   CAS 85622-93-1
别名: NSC 362856, 替莫唑胺, TZM, CCRG 81045, TMZ

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自噬

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Temozolomide Chemical Structure
Temozolomide, CAS 85622-93-1
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
产品目录号及名称: Temozolomide (T1178)
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纯度: 99.87%
纯度: 98.43%
纯度: 98%
纯度: 98%
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生物活性
化学信息
存储 & 溶解度
参考文献
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

存储

keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 28.83mg/ml (200 mM)

溶液配制表

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

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Mhaidat NM, et al. Temozolomide induces senescence but not apoptosis in human melanoma cells. Br J Cancer. 2007 Nov 5;97(9):1225-33. 2. Barciszewska AM, et al. A New Epigenetic Mechanism of Temozolomide Action in Glioma Cells. PLoS One. 2015 Aug 26;10(8):e0136669. 3. Daniel RA, et al. Central nervous system penetration and enhancement of temozolomide activity in childhood medulloblastoma models by poly(ADP-ribose) polymerase inhibitor AG-014699. Br J Cancer. 2010 Nov 9;103(10):1588-96. 4. Da Ros M, et al. Aldoxorubicin and Temozolomide combination in a xenograft mice model of human glioblastoma. Oncotarget. 2018 Oct 9;9(79):34935-34944. 5. Daniel RA, et al. Central nervous system penetration and enhancement of temozolomide activity in childhood medulloblastoma models by poly(ADP-ribose) polymerase inhibitor AG-014699. 6. Zhang B, Xu C, Liu J, et al. Nidogen-1 expression is associated with overall survival and temozolomide sensitivity in low-grade glioma patients[J]. Aging (Albany NY). 2021, 13(6): 9085. 7. Herbener V J, Burster T, Goreth A, et al. Considering the Experimental use of Temozolomide in Glioblastoma Research[J]. Biomedicines. 2020, 8(6): 151.

文献引用

1. Wang Y, Wang X, Wang K, et al.Chronic stress accelerates glioblastoma progression via DRD2/ERK/β-catenin axis and Dopamine/ERK/TH positive feedback loop.Journal of Experimental & Clinical Cancer Research.2023, 42(1): 1-17. 2. Liu X, Guo C, Leng T, et al.Differential regulation of H3K9/H3K14 acetylation by small molecules drives neuron-fate-induction of glioma cell.Cell Death & Disease.2023, 14(2): 142. 3. Liu X, Guo Q, Gao G, et al.Exosome-transmitted circCABIN1 promotes temozolomide resistance in glioblastoma via sustaining ErbB downstream signaling.Journal of Nanobiotechnology.2023, 21(1): 1-25. 4. Chen Y, Guo Y, Li S, et al.Remdesivir inhibits the progression of glioblastoma by enhancing endoplasmic reticulum stress.Biomedicine & Pharmacotherapy.2023, 157: 114037. 5. Dong J, Peng Y, Zhong M, et al.Implication of lncRNA ZBED3-AS1 downregulation in acquired resistance to Temozolomide and glycolysis in glioblastoma.European Journal of Pharmacology.2022: 175444. 6. Tong S, Hong Y, Xu Y, et al.TFR2 regulates ferroptosis and enhances temozolomide chemo-sensitization in gliomas.Experimental Cell Research.2023: 113474. 7. Jiao W, Zhu S, Shao J, et al. ZSTK474 Sensitizes Glioblastoma to Temozolomide by Blocking Homologous Recombination Repair. BioMed Research International. 2022 8. Li J, Sun Y, Sun X, et al. AEG-1 silencing attenuates M2-polarization of glioma-associated microglia/macrophages and sensitizes glioma cells to temozolomide. Scientific reports. 2021, 11(1): 1-12. 9. Wang Y, Wang X, Wang X, et al. Imipramine impedes glioma progression by inhibiting YAP as a Hippo pathway independent manner and synergizes with temozolomide. Journal of Cellular and Molecular Medicine. 2021 10. Zhang B, Xu C, Liu J, et al. Nidogen-1 expression is associated with overall survival and temozolomide sensitivity in low-grade glioma patients. Aging (Albany NY). 2021 Mar 18;13(6):9085-9107. doi: 10.18632/aging.202789. Epub 2021 Mar 18.
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相关化合物库

该产品包含在如下化合物库中:
抗癌临床化合物库 抗癌药物库 酪氨酸激酶分子库 抗癌活性化合物库 抗癌上市药物库 表型筛选靶点鉴定库 细胞周期化合物库 DNA 损伤和修复分子库 造血毒性小分子库 经典已知活性库

剂量换算

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体内实验配液计算器

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。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
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技术支持

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。

Keywords

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

 

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