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/ Temozolomide

替莫唑胺 /Temozolomide {[allProObj[0].p_purity_real_show]}

货号：A137834 同义名： NSC 362856;CCRG 81045

Temozolomide is a DNA-methylating agent and an alkylating cytostatic drug used in the treatment of some brain cancers, astrocytoma and glioblastoma multiforme.

HazMat Fee +

There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Temozolomide 化学结构 CAS号：85622-93-1
Temozolomide 化学结构
CAS号：85622-93-1
Temozolomide 3D分子结构
CAS号：85622-93-1
Temozolomide 化学结构 CAS号：85622-93-1
Temozolomide 3D分子结构 CAS号：85622-93-1
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Temozolomide 纯度/质量文件 产品仅供科研

货号：A137834 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

全球学术期刊中引用的产品

• Nat. Biomed. Eng., 2024, 8, 1412-1424. Ambeed. [ A538667 , A631746 ]
• JMC, 2024. Ambeed. [ A833302 , A475501 , A341986 , A356070 ]
• BMC Cancer, 2024, 24(1): 1415. Ambeed. [ A809692 , A209020 ]
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产品名称 DNA synthesis ↓ helicase ↓ RdRp ↓ ribonucleotide reductase ↓ tRNA synthetase ↓ YB-1 ↓ 其他靶点 纯度
Fexinidazole ✔ 98%
Daptomycin ✔ 98%
Blasticidin S·HCl ✔ 98%
Metronidazole ✔ 98%
Daunorubicin HCl +++

DNA synthesis, Ki: 20 nM

 		98%
Triglycidyl isocyanurate ✔ p53 98+%
Nedaplatin ✔ 99%+
Bendamustine ✔ 98+%
Trifluridine ✔ 98%
Robinetin ✔ 99%+
Carboplatin ✔ 99%
Cidofovir ✔ 99%
Cisplatin ✔ 99%
Cytarabine ++++

DNA synthesis, IC50: 16 nM

 		98%
Acelarin ++++

DNA synthesis, EC50: 0.2 nM

 		99%+
Oxaliplatin ✔ 98%
YK-4-279 ✔ 99%+
ML216 +

BLMfull-length, IC50: 2.98 μM

BLM636-1298, IC50: 0.97 μM

 		99%+
RK-33 ✔ 98%
Brr2-IN-3 ✔ 99%+
Phen-DC3 Trifluoromethanesulfonate ✔ 98%
Favipiravir ✔ 97%
Suramin sodium salt ++

RdRp, IC50: 0.26 μM

 		99%+
Clofarabine ++

Ribonucleotide reductase, IC50: 65 nM

 		97%
Didox ✔ 98%
(E)-3-AP ✔ 97%
Halofuginone +++

prolyl-tRNA synthetase, Ki: 18.3nM

 		99%+
BC-LI-0186 +++

Leucyl-tRNA synthetase, Kd: 42.1 nM

Leucyl-tRNA synthetase, IC50: 46.11 nM

 		98%
SU056 +

YB-1, IC50: 1.73 μM

 		98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Temozolomide 生物活性

描述 DNA damage is an abnormal chemical structure in DNA, while a mutation is a change in the sequence of standard base pairs. DNA damages cause changes in the structure of the genetic material and prevent the replication mechanism from functioning and performing properly. Temozolomide is converted to the active metabolite 5-(3-methyltriazen-1-yl) imidazole-4-carboxamide (MTIC) by non-enzymatic chemical conversion that produces DNA damage[3]. In vitro, temozolomide exhibited anti-proliferation to human malignant glioma cell lines U373MG, U87MG, and T98G with IC50 values of 40, 30 and 350 μM, respectively. Temozolomide induced apoptosis in the MGMT expressing cells occurred through AKT-Glycogen-Synthase-Kinase-3β signaling and is mediated by myelocytomatosis oncoprotein[4]. Temozolomide treatment at concentration of 100 mM for 72h increased the population at the G2/M phase and decreased the population at the G1 phase in all malignant glioma cells. In addition, temozolomide induced autophagy in U373-MG cells[5]. In vivo, administration of 40 mg/kg temozolomide significantly increased survival times in a B16F10 mouse metastatic melanoma model[6]. Treatment with temozolomide at dose of 2.5 mg/kg daily for 4 weeks resulted in a 78.30% tumor suppression, and reduced microvessel density in the glioblastoma orthotopic xenograft model[7].

Temozolomide 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 数据源
A172 200 μM Function Assay 48 h increases BRCC3 mRNA expression 25337721
A172 200 μM Function Assay 48 h increases the expression of BRCA1, BRCA2, RAD51 and FANCD2 25337721
A172 200 μM Function Assay 24/72/120 h increases γH2AX foci formation time-dependently 25337721
A2058 Growth Inhibition Assay 48 h  IC50=12 μM 25524552

Temozolomide 动物研究

Dose Nude Mice: 0.9 mg/kg - 266 mg/kg[1] (p.o.) Mice: 50 mg/kg[2] (i.v.)
Administration p.o., i.v.
Pharmacokinetics
Animal Mice[2]
Dose 50 mg/kg
Administration i.v.
T1/2 0.689 ± 0.019 h (plasma)
AUC0→7h 36.81 ± 1.11 μg/g·h (brain)
65.40 ± 2.00 μg/ml·h (plasma)

Temozolomide 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00611247 Leukemia, Myeloid Phase 2 Completed - United States, California ... 展开 >> Stanford University School of Medicine Stanford, California, United States, 94305 收起 <<
NCT00611247 - Completed - -
NCT00869050 Neuroendocrine Tumors Phase 2 Completed - United States, New York ... 展开 >> Columbia University Medical Center New York, New York, United States, 10032 收起 <<

Temozolomide 参考文献

[1]Iorio AL, da Ros M, et al. Tumor response of temozolomide in combination with morphine in a xenograft model of human glioblastoma. Oncotarget. 2017 Aug 3;8(52):89595-89606.

[2]de Gooijer MC, de Vries NA, et al. Improved Brain Penetration and Antitumor Efficacy of Temozolomide by Inhibition of ABCB1 and ABCG2. Neoplasia. 2018 Jul;20(7):710-720.

[3]Thomas A, Tanaka M, Trepel J, Reinhold WC, Rajapakse VN, Pommier Y. Temozolomide in the Era of Precision Medicine. Cancer Res. 2017 Feb 15;77(4):823-826. doi: 10.1158/0008-5472.CAN-16-2983. Epub 2017 Feb 3. PMID: 28159862; PMCID: PMC5313339.

[4]De Salvo M, Maresca G, D'agnano I, Marchese R, Stigliano A, Gagliassi R, Brunetti E, Raza GH, De Paula U, Bucci B. Temozolomide induced c-Myc-mediated apoptosis via Akt signalling in MGMT expressing glioblastoma cells. Int J Radiat Biol. 2011 May;87(5):518-33. doi: 10.3109/09553002.2011.556173. Epub 2011 Mar 15. PMID: 21405945.

[5]Kanzawa T, Germano IM, Komata T, Ito H, Kondo Y, Kondo S. Role of autophagy in temozolomide-induced cytotoxicity for malignant glioma cells. Cell Death Differ. 2004 Apr;11(4):448-57. doi: 10.1038/sj.cdd.4401359. PMID: 14713959.

[6]Mathieu V, Le Mercier M, De Neve N, Sauvage S, Gras T, Roland I, Lefranc F, Kiss R. Galectin-1 knockdown increases sensitivity to temozolomide in a B16F10 mouse metastatic melanoma model. J Invest Dermatol. 2007 Oct;127(10):2399-410. doi: 10.1038/sj.jid.5700869. Epub 2007 May 10. PMID: 17495956.

[7]Jo MY, Kim YG, Kim Y, Lee SJ, Kim MH, Joo KM, Kim HH, Nam DH. Combined therapy of temozolomide and ZD6474 (vandetanib) effectively reduces glioblastoma tumor volume through anti-angiogenic and anti-proliferative mechanisms. Mol Med Rep. 2012 Jul;6(1):88-92. doi: 10.3892/mmr.2012.868. Epub 2012 Apr 11. PMID: 22505191.

Temozolomide 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

5.15mL

1.03mL

0.52mL

25.75mL

5.15mL

2.58mL

51.51mL

10.30mL

5.15mL

Temozolomide 技术信息

CAS号85622-93-1
分子式C6H6N6O2
分子量 194.151
别名 NSC 362856;CCRG 81045;Temodar. Foreign brand name: Temodal;TMZ. US brand names: Methazolastone;RP46161;SCH-52365;Temodal;Methazolastone;MB 39831;TMZ
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,2-8°C
溶解度

DMSO: 20 mg/mL(103.01 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 2.5 mg/mL(12.88 mM)，配合低频超声助溶
动物实验配方

5% DMSO+30% PEG 300+water 2 mg/mL

Tags: Temozolomide | NSC 362856;CCRG 81045;Temodar. TMZ. RP46161;SCH-52365;Temodal;Methazolastone;MB 39831;TMZ | DNA/RNA Synthesis | DNA Alkylator/Crosslinker | AmBeed-信号通路专用抑制剂 | Temozolomide 纯度/质量文件 | Temozolomide 亚型比较 | Temozolomide 生物活性 | Temozolomide 细胞研究 | Temozolomide 动物研究 | Temozolomide 临床数据 | Temozolomide 参考文献 | Temozolomide 实验方案 | Temozolomide 技术信息

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