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洛莫司汀

洛莫司汀用途

Lomustine 是一种 DNA 烷化剂 (DNA alkylator),具有抗肿瘤活性。
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洛莫司汀名称

[ CAS 号 ]:
13010-47-4

[ 中文名 ]:
洛莫司汀

[ 英文名 ]:
Lomustine

[中文别名 ]:

[英文别名 ]:

洛莫司汀生物活性

[ 描述 ]:

Lomustine 是一种 DNA 烷化剂 (DNA alkylator),具有抗肿瘤活性。

[ 相关类别 ]:

信号通路 >> 自噬 >> 自噬
信号通路 >> 细胞周期/DNA损伤 >> DNA烷基化剂/交联剂
研究领域 >> 癌症

[ 靶点 ]

DNA Alkylator[1]


[体外研究]

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]。

[体内研究]

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]。

[激酶实验]

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]。

[细胞实验]

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]。

[动物实验]

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]。

[参考文献]

[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.


[相关活性小分子]

卡利奇霉素 | 卡莫司汀 | RITA | SJG-136 | 福莫司汀 | 盐酸甲基苄肼 | 塞替派 | 1,2:5,6-二脱水半乳糖醇 | 米铂 | 2,4,6-三(二甲氨基)均三嗪 | 曲奥舒凡 | 乌拉莫司汀 | 赛特铂

洛莫司汀物理化学性质

[ 密度 ]:
1.4±0.1 g/cm3

[ 熔点 ]:
88-90

[ 分子式 ]:
C9H16ClN3O2

[ 分子量 ]:
233.695

[ 精确质量 ]:
233.093109

[ PSA ]:
61.77000

[ LogP ]:
2.76

[ 外观性状 ]:
黄色粉末

[ 蒸汽压 ]:
0.00142mmHg at 25°C

[ 折射率 ]:
1.583

[ 储存条件 ]:
库房低温通风干燥,与食品原料分开存放

洛莫司汀MSDS

详细MSDS(安全技术说明书)

洛莫司汀毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :
YS4900000
CHEMICAL NAME :
Urea, 1-(2-chloroethyl)-3-cyclohexyl-1-nitroso-
CAS REGISTRY NUMBER :
13010-47-4
LAST UPDATED :
199612
DATA ITEMS CITED :
69
MOLECULAR FORMULA :
C9-H16-Cl-N3-O2
MOLECULAR WEIGHT :
233.73
WISWESSER LINE NOTATION :
L6TJ AMVNNO&2G

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human
DOSE/DURATION :
30 mg/kg
TOXIC EFFECTS :
Behavioral - anorexia (human) Gastrointestinal - nausea or vomiting
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human
DOSE/DURATION :
3 mg/kg
TOXIC EFFECTS :
Gastrointestinal - nausea or vomiting Blood - leukopenia Blood - thrombocytopenia
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
70 mg/kg
TOXIC EFFECTS :
Gastrointestinal - hypermotility, diarrhea Liver - jaundice, other or unclassified Kidney, Ureter, Bladder - urine volume increased
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
50350 ug/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
38 mg/kg
TOXIC EFFECTS :
Gastrointestinal - hypermotility, diarrhea Liver - jaundice, other or unclassified Kidney, Ureter, Bladder - urine volume increased
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
53 mg/kg
TOXIC EFFECTS :
Gastrointestinal - hypermotility, diarrhea Liver - jaundice, other or unclassified Kidney, Ureter, Bladder - urine volume increased
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
54 mg/kg
TOXIC EFFECTS :
Gastrointestinal - hypermotility, diarrhea Liver - jaundice, other or unclassified Kidney, Ureter, Bladder - urine volume increased
TYPE OF TEST :
LD10 - Lethal Dose
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
40 mg/kg
TOXIC EFFECTS :
Tumorigenic - active as anti-cancer agent
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Unreported
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
30 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
TYPE OF TEST :
LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
10 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
TYPE OF TEST :
LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
5 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
35 mg/kg/14D-I
TOXIC EFFECTS :
Blood - leukopenia Blood - changes in bone marrow (not otherwise specified) Nutritional and Gross Metabolic - weight loss or decreased weight gain
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Primate - monkey
DOSE/DURATION :
140 mg/kg/14D-I
TOXIC EFFECTS :
Liver - fatty liver degeneration Blood - normocytic anemia Blood - changes in bone marrow (not otherwise specified)
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
50 mg/kg
TOXIC EFFECTS :
Tumorigenic - equivocal tumorigenic agent by RTECS criteria Liver - tumors
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
60 mg/kg/7W-I
TOXIC EFFECTS :
Tumorigenic - equivocal tumorigenic agent by RTECS criteria Lungs, Thorax, or Respiration - tumors Skin and Appendages - tumors
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
64 mg/kg/60W-I
TOXIC EFFECTS :
Tumorigenic - equivocal tumorigenic agent by RTECS criteria Gastrointestinal - tumors
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Administration onto the skin
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
276 mg/kg/23W-I
TOXIC EFFECTS :
Tumorigenic - equivocal tumorigenic agent by RTECS criteria Skin and Appendages - hair Skin and Appendages - tumors
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
98 mg/kg/26W-I
TOXIC EFFECTS :
Tumorigenic - equivocal tumorigenic agent by RTECS criteria Blood - leukemia Blood - lymphoma, including Hodgkin's disease
TYPE OF TEST :
TD - Toxic dose (other than lowest)
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
127 mg/kg/60W-I
TOXIC EFFECTS :
Tumorigenic - equivocal tumorigenic agent by RTECS criteria Lungs, Thorax, or Respiration - tumors Gastrointestinal - tumors
TYPE OF TEST :
TD - Toxic dose (other than lowest)
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
178 mg/kg/42W-I
TOXIC EFFECTS :
Tumorigenic - equivocal tumorigenic agent by RTECS criteria Lungs, Thorax, or Respiration - tumors
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intraperitoneal
DOSE :
16 mg/kg
SEX/DURATION :
female 6-9 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Specific Developmental Abnormalities - Central Nervous System Reproductive - Specific Developmental Abnormalities - eye/ear
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intraperitoneal
DOSE :
16 mg/kg
SEX/DURATION :
female 6-9 day(s) after conception
TOXIC EFFECTS :
Reproductive - Specific Developmental Abnormalities - body wall Reproductive - Specific Developmental Abnormalities - cardiovascular (circulatory) system Reproductive - Specific Developmental Abnormalities - urogenital system
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intraperitoneal
DOSE :
22500 ug/kg
SEX/DURATION :
male 9 week(s) pre-mating
TOXIC EFFECTS :
Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Fertility - litter size (e.g. # fetuses per litter; measured before birth)
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intraperitoneal
DOSE :
8 mg/kg
SEX/DURATION :
female 9-12 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Specific Developmental Abnormalities - musculoskeletal system
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intraperitoneal
DOSE :
9 mg/kg
SEX/DURATION :
male 1 day(s) pre-mating
TOXIC EFFECTS :
Reproductive - Paternal Effects - spermatogenesis (incl. genetic material, sperm morphology, motility, and count)
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intravenous
DOSE :
39 mg/kg
SEX/DURATION :
female 6-18 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Effects on Newborn - sex ratio Reproductive - Fertility - abortion
TYPE OF TEST :
DNA inhibition
TYPE OF TEST :
DNA adduct
TYPE OF TEST :
DNA damage
TYPE OF TEST :
DNA damage
TYPE OF TEST :
DNA inhibition
TYPE OF TEST :
Sperm Morphology

MUTATION DATA

TYPE OF TEST :
DNA damage
TEST SYSTEM :
Mammal - species unspecified Lymphocyte
DOSE/DURATION :
10 mmol/L
REFERENCE :
CNREA8 Cancer Research. (Public Ledger Building, Suit 816, 6th & Chestnut Sts., Philadelphia, PA 19106) V.1- 1941- Volume(issue)/page/year: 44,1887,1984 *** REVIEWS *** IARC Cancer Review:Animal Sufficient Evidence IMEMDT IARC Monographs on the Evaluation of Carcinogenic Risk of Chemicals to Man. (WHO Publications Centre USA, 49 Sheridan Ave., Albany, NY 12210) V.1- 1972- Volume(issue)/page/year: 26,137,1981 IARC Cancer Review:Human Inadequate Evidence IMEMDT IARC Monographs on the Evaluation of Carcinogenic Risk of Chemicals to Man. (WHO Publications Centre USA, 49 Sheridan Ave., Albany, NY 12210) V.1- 1972- Volume(issue)/page/year: 26,137,1981 IARC Cancer Review:Group 2A IMSUDL IARC Monographs, Supplement. (WHO Publications Centre USA, 49 Sheridan Ave., Albany, NY 12210) No.1- 1979- Volume(issue)/page/year: 7,150,1987 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X4755 No. of Facilities: 103 (estimated) No. of Industries: 1 No. of Occupations: 3 No. of Employees: 2457 (estimated) No. of Female Employees: 1069 (estimated)
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洛莫司汀安全信息

[ 符号 ]:

GHS06, GHS08

[ 信号词 ]:
Danger

[ 危害声明 ]:
H301-H350

[ 警示性声明 ]:
P201-P301 + P310-P308 + P313

[ 个人防护装备 ]:
Eyeshields;Faceshields;full-face particle respirator type N100 (US);Gloves;respirator cartridge type N100 (US);type P1 (EN143) respirator filter;type P3 (EN 143) respirator cartridges

[ 危害码 (欧洲) ]:
T: Toxic;

[ 风险声明 (欧洲) ]:
R45

[ 安全声明 (欧洲) ]:
S53-S45

[ 危险品运输编码 ]:
3249

[ RTECS号 ]:
YS4900000

[ 包装等级 ]:
II

[ 危险类别 ]:
6.1(a)

[ 海关编码 ]:
2924299090

洛莫司汀合成路线

详细合成路线

洛莫司汀上下游产品

洛莫司汀上游产品

洛莫司汀下游产品

洛莫司汀制备

由2-氨基乙醇与尿素环合为2-噁唑烷酮，再与环已胺反应生成N-（2-羟乙基）-N'-环乙基脲，然后用氯化亚砜氯化得到N-（2-氯乙基）-N'-环已基脲，最后经亚硝化反应制得环已亚硝脲。

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洛莫司汀海关

[ 海关编码 ]: 2924299090

[ 中文概述 ]:
2924299090. 其他环酰胺（包括环氨基甲酸酯）（包括其衍生物以及他们的盐）. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:30.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 包装

[ Summary ]:
2924299090. other cyclic amides (including cyclic carbamates) and their derivatives; salts thereof. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:30.0%

洛莫司汀文献

Expression of O(6)-methylguanine-DNA methyltransferase causes lomustine resistance in canine lymphoma cells.

Can. J. Vet. Res. 79 , 201-9, (2015)

The DNA repair protein O (6)-methylguanine-DNA methyltransferase (MGMT) causes resistance to nitrosoureas in various human cancers. In this study, we analyzed the correlation between canine lymphomas ...

Preliminary study of lomustine in the treatment of intracranial masses in dogs following localization by imaging techniques.

Semin. Vet. Med. Surg. Small Anim. 5(4) , 241-5, (1990)

The nitrosoureas: carmustine (BCNU) and lomustine (CCNU).

Cancer Treat. Rev. 9(4) , 313-30, (1982)


更多文献

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公司名：上海吉至生化科技有限公司

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￥728.0/250mg ￥2418.0/1g

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区域：上海市浦东新区

价格：
￥需询单/1g

联系人：赖经理

产品详情：Lomustine (CeeNU)

公司名：上海脉铂医药科技有限公司

区域：上海市嘉定区

价格：
￥1509.0/500mg ￥539.0/1g ￥849.0/250mg ￥需询单/1g

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价格：
￥1489.9/1g ￥484.9/250mg ￥187.9/50mg ￥265.9/1ml

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￥515.0/250mg ￥1584.0/1g ￥1489.6/500mg ￥需询单/1ml

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