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My Cart> Small Molecule Compounds > Inhibitors & Antagonists & Agonists > DNA Damage & DNA Repai > LomustineCAS：13010-47-4
Molecular Formula：C9H16ClN3O2
Molecular Weight：233.7
Storage：Powder:-20℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：Light yellow to yellow Solid
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| CAS | 13010-47-4 |
| Name | Lomustine |
| Molecular Formula | C9H16ClN3O2 |
| Molecular Weight | 233.7 |
| Solubility | Soluble in DMSO |
| Purity | ≥98% |
| Appearance | Light yellow to yellow Solid |
| Storage | Powder:-20℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| EC | EINECS 235-859-2 |
| MDL | MFCD00012392 |
| SMILES | O=C(NC1CCCCC1)N(CCCl)N=O |
| InChIKey | GQYIWUVLTXOXAJ-UHFFFAOYSA-N |
| InChI | InChI=1S/C9H16ClN3O2/c10-6-7-13(12-15)9(14)11-8-4-2-1-3-5-8/h8H,1-7H2,(H,11,14) |
| PubChem CID | 3950 |
| Target Point | DNA Alkylator |
| Passage | DNA Damage/DNA Repair |
| Background | It is a DNA alkylator with antitumor activity. Suppresses cancer cells by damaging DNA and preventing cell division. |
| Biological Activity | Lomustine 是一种 DNA 烷化剂 (DNA alkylator)，具有抗肿瘤活性。[1-3] |
| In Vitro | 洛莫司汀是一种DNA烷化剂。洛莫司汀(CCNU，0-250μM)对表达肿瘤来源的突变体IDH1的U87-MG细胞具有细胞毒性，对野生型IDH1的表达几乎没有影响。洛莫司汀和丙卡巴肼或长春新碱的组合对表达突变型或野生型IDH1的细胞的杀伤没有累加效应。此外，过量表达ALKBH2或ALKBH3可部分减少暴露于洛莫司汀的死亡HT1080细胞[1]。 Lomustine抑制U87-MG生长，ED50为68.1μM。洛莫司汀(30，40μM)与二十二碳六烯酸(DHA)组合，可以抑制另外2种人源胶质母细胞瘤细胞系，并诱导U87-MG凋亡和坏死。洛莫司汀(30μM)导致G2/M停滞[2]。洛莫司汀降低F98大鼠原位胶质瘤细胞和Tu-2449小鼠胶质瘤细胞系的活力，IC50分别为20.8μM和18.6μM[3]。 |
| In Vivo | 洛莫司汀(30mg/kg)与Toca 511 + 5-FC组合可延长携带F98肿瘤细胞的大鼠的存活。 Lomustine(30 mg/kg)联合Toca-511 + 5-FC在携带Tu-2449胶质瘤细胞的B6C3F1小鼠中也具有抗肿瘤活性[3]。 |
| Cell Experiment | 最初，将细胞(5000个细胞/孔)在96孔平底板中在完全培养基中培养过夜以建立线性生长速率。用补充有2％FBS和不同处理(100μL总体积/孔)的新培养基替换用过的培养基。补充乙醇的细胞(<0.5％)用作载体对照。在用WST-1测定试剂评估细胞生长之前，将细胞在潮湿气氛中在37℃，5％CO 2中维持24小时。单独的培养基与WST-1测定试剂组合建立非特异性值，其从实验光密度(OD)读数(450nm处的OD)中减去。载体对照OD读数用作标准化至100％的标准增殖潜力。通过将平均OD治疗读数除以平均OD载体读数并乘以100来计算增殖指数[2]。 |
| Animal Experiment | 小鼠[3]在研究期间，B6C3F1小鼠组仅接受PBS或5-FC作为对照(每组n = 8)。一组小鼠(洛莫司汀第1天+ PBS)在第1天接受一剂洛莫司汀(30mg/kg)和总共六个周期的PBS(800μL/天，BID，每10天连续4天)。其余小鼠连续4天接受5-FC(500 mg/kg /剂量，IP，BID)，在第1天加入洛莫司汀(洛莫司汀第1天+ 5-FC)或第43天(洛莫司汀第43天+5天)FC)。将5-FC或PBS停止4天，10天的循环重复总共6次。每次实验在最后的5-FC处理结束时终止。收集所有组织并保存用于组织病理学。将接受洛莫司汀的组中的毒性与单独接受PBS或5-FC或在指定时间点与5-FC组合的组进行比较[3]。大鼠[3]大鼠组在研究期间仅接受PBS或5-FC作为对照(每组n = 8)。一组大鼠(洛莫司汀第1天+ PBS)在第1天接受一剂洛莫司汀(30mg/kg)和总共6个循环的PBS(8mL /天，BID)。其余大鼠连续5天接受5-FC(500mg/kg /剂量，IP，BID)，然后在第1天(洛莫司汀第1天+ 5-FC)或第22天接受药物停药2天，加用洛莫司汀(Lomustine Day 22 + 5-FC)。 5天开放，5天FC或PBS关闭2天的循环共重复6次[3]。 |
| Kinase Experiment | 简而言之，寡核苷酸底物(5'-FAM-TAGACATTGCCATTCTCGATAGGXTCCGGTCAAATCTAGACGAATTCCG，X = 1-MedA)用于测定。在50mM Hepes K(pH 8.0)，50μM(NH 4)2 Fe(SO 4)2，50μMα-KG，2mM抗坏血酸，10μM寡聚底物，3μM酶，50μg/ mL中测定ALKBH2和ALKBH3。 BSA和10mM MgCl 2。反应在37℃下进行，并通过在95℃加热至少5分钟来终止反应。将寡核苷酸底物退火至反向互补寡核苷酸，并进行广泛的DpnII消化。将消化的DNA在15％TBE-Urea-PAGE凝胶上分离，并使用Typhoon Scanner进行成像[1]。 |
| Data Literature Source | [1]. 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. [2]. 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. [3]. 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 |
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是一种 DNA 烷化剂 (DNA alkylator)，具有抗肿瘤活性。通过损坏DNA和阻止细胞分裂来抑制癌细胞。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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