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2,4,6-三(二甲氨基)均三嗪

2,4,6-三(二甲氨基)均三嗪用途

Altretamine 是一种烷化剂 (alkylator),具有抗肿瘤活性。

2,4,6-三(二甲氨基)均三嗪名称

[ CAS 号 ]:
645-05-6

[ 中文名 ]:
六甲蜜胺

[ 英文名 ]:
Altretamine

[中文别名 ]:

[英文别名 ]:

HTM
Hexastat
2,4,6-tris<dimethylamino>-1,3,5-triazine
HMM
Hexalen
EINECS 211-428-4
hexamethylmelamine
Altretamine
Hexylen
MFCD00549245

2,4,6-三(二甲氨基)均三嗪生物活性

[ 描述 ]:

Altretamine 是一种烷化剂 (alkylator),具有抗肿瘤活性。

[ 相关类别 ]:

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

[体外研究]

Altretamine是一种抗肿瘤药物[1]。

[体内研究]

Altretamine(100,133 mg/kg,ip。)与Irofulven联合使用可增加携带MV522细胞的小鼠的抗肿瘤作用[1]。

[动物实验]

小鼠[1] Balb / c nu / nu 4周龄雌性小鼠体重18-22g，接受sc注射8-10百万MV522细胞。在肿瘤植入后第10天开始，每周三次腹膜内施用阿尔特雷明，持续3周。以两个垂直直径测量肿瘤大小，并根据下式估计肿瘤重量（TW）：w = [（宽度）2×长度/ 2]。将阿尔特赖胺制备成在40％DMSO /生理盐水中的1-10mg / mL的储备溶液，并根据需要用10％DMSO /生理盐水稀释[1]。

[参考文献]

[1]. Kelner MJ, et al. Synergy of irofulven in combination with other DNA damaging agents: synergistic interaction with altretamine, alkylating, and platinum-derived agents in the MV522 lung tumor model. Cancer Chemother Pharmacol. 2008 Dec;63(1):19-26.

[相关活性小分子]

2,4,6-三(二甲氨基)均三嗪物理化学性质

[ 密度 ]:
1.1±0.1 g/cm3

[ 沸点 ]:
339.4±25.0 °C at 760 mmHg

[ 熔点 ]:
171-175 °C(lit.)

[ 分子式 ]:
C₉H₁₈N₆

[ 分子量 ]:
210.279

[ 闪点 ]:
159.1±23.2 °C

[ 精确质量 ]:
210.159302

[ PSA ]:
48.39000

[ LogP ]:
2.42

[ 外观性状 ]:
无色结晶固体

[ 蒸汽压 ]:
0.0±0.7 mmHg at 25°C

[ 折射率 ]:
1.610

[ 储存条件 ]:
Refrigerator

[ 水溶解性 ]:
Insoluble

2,4,6-三(二甲氨基)均三嗪毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: OS1050000

CHEMICAL NAME :: Melamine, hexamethyl-

CAS REGISTRY NUMBER :: 645-05-6

BEILSTEIN REFERENCE NO. :: 0195058

LAST UPDATED :: 199612

DATA ITEMS CITED :: 26

MOLECULAR FORMULA :: C9-H18-N6

MOLECULAR WEIGHT :: 210.33

WISWESSER LINE NOTATION :: T6N CN ENJ BN1&1 DN1&1 FN1&1

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human

DOSE/DURATION :: 8 mg/kg

TOXIC EFFECTS :: Gastrointestinal - nausea or vomiting Blood - leukopenia

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 350 mg/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 :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 265 mg/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 :: 437 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - chromodacryorrhea Blood - hemorrhage

TYPE OF TEST :: LD10 - Lethal Dose

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 200 mg/kg

TOXIC EFFECTS :: Blood - granulocytopenia Blood - changes in bone marrow (not otherwise specified)

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 171 mg/kg

TOXIC EFFECTS :: Cardiac - cardiomyopathy including infarction Liver - hepatitis (hepatocellular necrosis), zonal

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 100 mg/kg

TOXIC EFFECTS :: Blood - pigmented or nucleated red blood cells Blood - changes in leukocyte (WBC) count Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - transaminases

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - guinea pig

DOSE/DURATION :: 255 mg/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 :: Bird - chicken

DOSE/DURATION :: 341 mg/kg

TOXIC EFFECTS :: Peripheral Nerve and Sensation - flaccid paralysis without anesthesia (usually neuromuscular blockage) Behavioral - ataxia

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 3080 mg/kg/77D-I

TOXIC EFFECTS :: Gastrointestinal - changes in structure or function of endocrine pancreas Endocrine - hyperglycemia Related to Chronic Data - death

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 625 mg/kg/5D-I

TOXIC EFFECTS :: Related to Chronic Data - death

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 625 mg/kg/5D-I

TOXIC EFFECTS :: Related to Chronic Data - death

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 250 mg/kg/5D-I

TOXIC EFFECTS :: Blood - changes in bone marrow (not otherwise specified) Blood - other changes Related to Chronic Data - death

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 3108 mg/kg/3Y-I

TOXIC EFFECTS :: Tumorigenic - equivocal tumorigenic agent by RTECS criteria Blood - leukemia

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 7 gm/kg/46W-C

TOXIC EFFECTS :: Tumorigenic - neoplastic by RTECS criteria Kidney, Ureter, Bladder - Kidney tumors Skin and Appendages - tumors

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 1240 mg/kg

SEX/DURATION :: male 62 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Paternal Effects - testes, epididymis, sperm duct Reproductive - Fertility - male fertility index (e.g. # males impregnating females per # males exposed to fertile nonpregnant females) Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 320 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 - Fertility - litter size (e.g. # fetuses per litter; measured before birth)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 320 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)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 1160 mg/kg

SEX/DURATION :: female 15-22 day(s) after conception lactating female 21 day(s) post-birth

TOXIC EFFECTS :: Reproductive - Effects on Newborn - viability index (e.g., # alive at day 4 per # born alive) Reproductive - Effects on Newborn - weaning or lactation index (e.g., # alive at weaning per # alive at day 4)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 80 mg/kg

SEX/DURATION :: female 15-22 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 780 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)

TYPE OF TEST :: Sex chromosome loss and nondisjunction

TYPE OF TEST :: Cytogenetic analysis

MUTATION DATA

TYPE OF TEST :: DNA damage

TEST SYSTEM :: Mammal - species unspecified Lymphocyte

DOSE/DURATION :: 250 umol/L

REFERENCE :: CNREA8 Cancer Research. (Public Ledger Building, Suit 816, 6th & Chestnut Sts., Philadelphia, PA 19106) V.1- 1941- Volume(issue)/page/year: 43,500,1983

2,4,6-三(二甲氨基)均三嗪安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302-H315-H319-H335

[ 警示性声明 ]:
P261-P305 + P351 + P338

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Faceshields;Gloves

[ 危害码 (欧洲) ]:
Xn: Harmful;

[ 风险声明 (欧洲) ]:
R22;R36/37/38

[ 安全声明 (欧洲) ]:
S26-S36

[ 危险品运输编码 ]:
NONH for all modes of transport

[ WGK德国 ]:
3

[ RTECS号 ]:
OS1050000

[ 海关编码 ]:
2933699090

2,4,6-三(二甲氨基)均三嗪上下游产品

2,4,6-三(二甲氨基)均三嗪上游产品

2,4,6-三(二甲氨基)均三嗪下游产品

2,4,6-三(二甲氨基)均三嗪制备

由三氯三聚氰与二甲胺缩合而得

2,4,6-三(二甲氨基)均三嗪海关

[ 海关编码 ]: 2933699090

[ 中文概述 ]:
2933699090 其他结构上含非稠合三嗪环化合物. 增值税率:17.0% 退税率:9.0% 监管条件:无最惠国关税:6.5% 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期

[ Summary ]:
2933699090 other compounds containing an unfused triazine ring (whether or not hydrogenated) in the structure。Supervision conditions:None。VAT:17.0%。Tax rebate rate:9.0%。MFN tariff:6.5%。General tariff:20.0%

2,4,6-三(二甲氨基)均三嗪文献

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Drug-induced liver injury (DILI) is a leading cause of drugs failing during clinical trials and being withdrawn from the market. Comparative analysis of drugs based on their DILI potential is an effec...

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