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Lomustine

Lomustine

产品编号 T1601   CAS 13010-47-4
别名: CCNU, NSC 79037, 洛莫司汀

Lomustine (NSC-79037) 是一种具有抗肿瘤活性的 DNA 烷化剂。

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Lomustine Chemical Structure
Lomustine, CAS 13010-47-4
规格 价格/CNY 货期 数量
25 mg ¥ 148 现货
50 mg ¥ 275 现货
100 mg ¥ 488 现货
200 mg ¥ 795 现货
500 mg ¥ 1,370 现货
1 mL * 10 mM (in DMSO) ¥ 271 现货
产品目录号及名称: Lomustine (T1601)
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纯度: 99.86%
纯度: 98.36%
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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 Lomustine (NSC-79037) is an alkylating agent of value against both hematologic malignancies and solid tumors.
体外活性 Lomustine inhibits the growth of ZR-75-1 and U373 with IC50 of 12 μM and 15 μM, respectively. Lomustine reduces the level of expression of the DNA repair protein O6-alkylguanine-DNA alkyltransferase. [1] Lomustine (420 μM) triggers apoptosis through the mitochondrial pathway via decrease in the level of the anti-apoptosis proteins Bcl-2 and Bcl-xl, respectively, in both medulloblastoma and normal human epithelial and fibroblast cells. Lomustine induces cell cycle delay in G2/M phase in medulloblastoma cells and up-regulates p21 protein level in a p53-independent manner in HFSN1 cells. [2]
体内活性 Lomustine can cause delayed, cumulative dose-related, chronic hepatotoxicity that is irreversible and can be fatal. [4] Lomustine could result in infrequent severe hematological toxicity in cats with spontaneously arising tumors, and the incidence of either grade III or IV neutropenia and thrombocytopenia is 4.1% and 1.0%, respectively. Lomustine trends toward a greater likelihood for progressive neutropenia and statistically significant higher response rates in cats with spontaneously arising tumors. [5]
细胞实验 Cell lines are routinely grown as monolayers in DMEM supplemented with 10% foetal calf serum, 25 mm HEPES, glutamine and penicillin/streptomycin. Cytotoxicity studies are carried out in HEPES-free medium in a 5% CO2 atmosphere. 750-1000 cells/well are plated in 96 well plates and after overnight incubation are treated for 2 hours with or without 33 μM BG. Temozolomide or CCNU is then added for 1 hour in the same medium, the final DMSO concentration not exceeding 1%. The cells are grown for a further 7 days in fresh medium and assayed for protein content by the NCI sulphorhodamine assay; growth studies show that cells are in log phase growth during the assay period. For the repeat temozolomide dosing schedule cells are given consecutive 24 hours treatments, with fresh medium each day. Assays are carried out at least in duplicate.(Only for Reference)
别名 CCNU, NSC 79037, 洛莫司汀
分子量 233.7
分子式 C9H16ClN3O2
CAS No. 13010-47-4

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 42 mg/mL(179.7 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 4.279 mL 21.395 mL 42.7899 mL 106.9748 mL
5 mM 0.8558 mL 4.279 mL 8.558 mL 21.395 mL
10 mM 0.4279 mL 2.1395 mL 4.279 mL 10.6975 mL
20 mM 0.2139 mL 1.0697 mL 2.1395 mL 5.3487 mL
50 mM 0.0856 mL 0.4279 mL 0.8558 mL 2.1395 mL
100 mM 0.0428 mL 0.2139 mL 0.4279 mL 1.0697 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. Baer JC, et al. Br J Cancer, 1993, 67(6), 1299-12302. 2. Shinwari Z, et al. J Neurooncol, 2008, 87(2), 123-132. 3. Rassnick KM, et al. J Vet Intern Med, 1999, 13(6), 601-605. 4. Kristal O, et al. J Vet Intern Med, 2004, 18(1), 75-80. 5. Fan TM, et al. J Am Anim Hosp Assoc, 2002, 38(4), 357-363. 6. Wang P, et al. Oncometabolite D-2-Hydroxyglutarate Inhibits ALKBH DNA Repair Enzymes and Sensitizes IDH Mutant Cells to Alkylating Agents. Cell Rep. 2015 Dec 22;13(11):2353-2361. 7. Harvey KA, et al. Enhanced anticancer properties of lomustine in conjunction with docosahexaenoic acid in glioblastoma cell lines. J Neurosurg. 2015 Mar;122(3):547-56. 8. Yagiz K, et al. Toca 511 plus 5-fluorocytosine in combination with lomustine shows chemotoxic and immunotherapeutic activity with no additive toxicity in rodent glioblastoma models. Neuro Oncol. 2016 Oct;18(10):1390-401.
Bendamustine hydrochloride Cyclophosphamide Pipobroman Procarbazine hydrochloride PK11000 RITA Streptozocin Illudin M

相关化合物库

该产品包含在如下化合物库中:
抗癌药物库 酪氨酸激酶分子库 抗癌活性化合物库 抗癌临床化合物库 抗癌上市药物库 抗衰老化合物库 造血毒性小分子库 儿童药物库 NO PAINS 化合物库 口服活性化合物库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

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
%
% Tween 80
% ddH2O
计算 重置

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

Lomustine 13010-47-4 Apoptosis Autophagy DNA Damage/DNA Repair Others DNA Alkylator/Crosslinker DNA Alkylation inhibit NSC79037 NSC-79037 Inhibitor CCNU NSC 79037 洛莫司汀 inhibitor

 

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