Temozolomide.|85622-93-1|(替莫唑胺; NSC 362856; CCRG 81045; TMZ)-陌孚医药/Medlife

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Temozolomide. (Synonyms: 替莫唑胺; NSC 362856; CCRG 81045; TMZ)

目录号: PC10338 纯度: ≥98%

CAS No. :85622-93-1

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PC10338-50mg	50mg	¥840.00	请登录
PC10338-10mM (in 1mL DMSO)	10mM (in 1mL DMSO)	¥600.00	请登录

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中文名称	Temozolomide.
中文别名	替莫唑胺;8-氨基甲酰基-3-甲基咪唑[5,1-d]并-1,2,3,5-四氮嗪-4-(3H)-酮;替目唑胺;Temozolomide 替莫唑胺;非洛地平;替莫唑胺 USP标准品;替莫唑胺Temozolomid;替莫唑胺重氮盐;3,4-二氢-3-甲基-4-氧代咪唑并[5,1-d]-1,2,3,5-四嗪-8-甲酰胺;3-甲基-4-氧代-8-咪唑并[5,1-d][1,2,3,5]四嗪甲酰胺;4-甲基-5-氧代-2,3,4,6,8-五氮杂双环[4.3.0]壬-2,7,9-三烯-9-甲酰胺;4-甲基-5-氧代-2,3,4,6,8-五氮杂双环[4.3.0]壬基-2,7,9-三烯-9-甲酰胺;8-氨基甲酰基-3-甲基-3-甲基咪唑[5,1-d]并-1,2,3,5-四氮嗪-4（3H）-酮;8-氨甲酰-3-甲基咪唑[5,1-d]-1,2,3,5-四嗪-4(3H)-酮
英文名称	Temozolomide
英文别名	3-Methyl-4-oxo-3,4-dihydroimidazo[5,1-d][1,2,3,5]tetrazine-8-carboxamide;4-Methyl-5-oxo-2,3,4,6,8-pentazabicyclo[4.3.0]nona-2,7,9-triene-9-carboxamide;Temozolomide;3-Methyl-4-oxo-3,4-dihydroimidazo-[5,1-d][1,2,3,5]tetrazine-8-carboxamide;Temozolamide;Temozolomid;CCRG 81045;NSC 362856;temodar;TEMODAR TEMOZOLOMIDE;temosolomide;TZM;3,4-Dihydro-3-methyl-4-oxoimidazo[5,1-d]-1,2,3,5-tetrazine-8-carboxamide;3,4-Dihydro-3-methyl-4-oxoimidazo[5,1-d][1,2,3,5]tetrazine-8-carboxamide;Methazolastone;Temodal;Temozolomidum [Latin];Temozolodida [Spanish];Temozolomidum;Sch 52365;MB 39831;M&B 39831;8-Carbamoyl-3-methylimidazo(5,1-d)-1,2,3,5-tetrazin-4(3H)-one;M & B 39831;3,4-Dihydro-3-methyl-4-oxoimidazo(5,1-d)-1,2,3,5-tetrazine-8-carboxamide;3-Methyl-
Cas No.	85622-93-1
分子式	C₆H₆N₆O₂
分子量	194.15
包装储存	-20°C, protect from light, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

生物活性

Temozolomide (NSC 362856) is an oral active DNA alkylating agent that crosses the blood-brain barrier. Temozolomide is also a proautophagic and proapoptotic agent. Temozolomide is effective against tumor cells that are characterized by low levels of O6-alkylguanine DNA alkyltransferase (OGAT) and a functional mismatch repair system. Temozolomide has antitumor and antiangiogenic effects.

性状

Solid

IC50 & Target[1][2]

DNA alkylator

体外研究(In Vitro)

Temozolomide (TZM) is a methylating agent that crosses the blood-brain barrier and is indicated for malignant gliomas and metastatic melanomas. Temozolomide is effective against tumor cells that are characterized by low levels of O-alkylguanine DNA alkyltransferase (OGAT) and a functional mismatch repair system (MR). Determination of the IC₅₀ for Temozolomide (TZM) in different cell lines gave values ranging from 14.1 to 234.6 μM that fell into two clearly differentiated groups: cell lines with low IC₅₀ values (<50 μM), which include A172 (14.1±1.1 μM) and LN229 cells (14.5±1.1 μM), and those with high IC₅₀ values (>100 μM), which include SF268 (147.2±2.1 μM) and SK-N-SH cells (234.6±2.3 μM).

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Temozolomide (TZM), as a single agent, does not significantly increase mdian survival time (MST) with respect to control. Noteworthy, intracranial injection of NU1025, immediately before the administration of 100 or 200 mg/kg Temozolomide, significantly increases lifespans with respect to controls or to groups treated with Temozolomide only. When Temozolomide is fractionated, the increase in lifespan (ILS) obtained with this schedule is higher than that observed when NU1025 is combined with a single injection of Temozolomide (statistical comparison of survival curves: NU1025 intracranially+Temozolomide 100 mg/kg×2 vs NU1025+Temozolomide 200 mg/kg; P=0.023).

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature or refrigerated transportation.

储存方式

-20°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

ClinicalTrial

参考文献

[1]. Tentori L, et al. Combined treatment with temozolomide and poly(ADP-ribose) polymerase inhibitor enhances survival of mice bearing hematologic malignancy at the central nervous system site. Blood. 2002 Mar 15;99(6):2241-4. [Information]

[2]. Mathieu V, et al. Combining Anti-Human VEGF with temozolomide increases the antitumor efficacy of temozolomide in a human glioblastoma orthotopic xenograft model. Neoplasia. 2008 Dec;10(12):1383-92. [Information]

[3]. Perazzoli G, et al. Temozolomide Resistance in Glioblastoma Cell Lines: Implication of MGMT, MMR, P-Glycoprotein and CD133 Expression. PLoS One. 2015 Oct 8;10(10):e0140131. [Information]

溶解度数据

体外研究:

DMSO : 20.83 mg/mL (107.29 mM; Need ultrasonic)

H₂O : 2.86 mg/mL (14.73 mM; Need ultrasonic)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	5.1507 mL	25.7533 mL	51.5066 mL
5 mM	1.0301 mL	5.1507 mL	10.3013 mL
10 mM	0.5151 mL	2.5753 mL	5.1507 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

建议依照次序添加每种溶剂： PBS
Solubility: 9.09 mg/mL (46.82 mM); Clear solution; Need ultrasonic and warming and heat to 60°C
2.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 1.25 mg/mL (6.44 mM); Clear solution

此方案可获得 ≥ 1.25 mg/mL (6.44 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 12.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
3.

建议依照次序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 1.25 mg/mL (6.44 mM); Clear solution

此方案可获得 ≥ 1.25 mg/mL (6.44 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 12.5 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
4.

建议依照次序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 1.25 mg/mL (6.44 mM); Clear solution

此方案可获得 ≥ 1.25 mg/mL (6.44 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 12.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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