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枸橼酸他莫昔芬

枸橼酸他莫昔芬用途

Tamoxifen Citrate是一种选择性雌激素受体调节剂 (SERM)。

枸橼酸他莫昔芬名称

[ CAS 号 ]:
54965-24-1

[ 中文名 ]:
枸橼酸他莫昔芬

[ 英文名 ]:
Tamoxifen citrate

[中文别名 ]:

[英文别名 ]:

EINECS 259-415-2
Tamoxifen, citrate salt
MFCD00058321
Tamoxifen citrate salt
2YR&UYR&R DO2N1&1 &&Z Form citrate
Tamoxifen citrate
Tamoxifen (Citrate)

枸橼酸他莫昔芬生物活性

[ 描述 ]:

Tamoxifen Citrate是一种选择性雌激素受体调节剂 (SERM)。

[ 相关类别 ]:

信号通路 >> 自噬 >> 自噬

信号通路 >> 其他 >> 雌激素受体/ERR

研究领域 >> 癌症

[ 靶点 ]

Estrogen receptor[1]

[体外研究]

他莫昔芬显示出对MCF-7细胞的强烈抑制作用(EC50 =1.41μM)和较小程度的T47D细胞(EC50 =2.5μM),但不影响MDA-MB-231细胞[2]。

[体内研究]

他莫昔芬诱导型基因敲除策略具有明显的优点,即基因的表达可以在组织特异性方式中随意消除在成年小鼠中。为了研究Med1在成年心脏中的作用,给予7周龄TmcsMed1 -/-小鼠每天腹膜内注射剂量为65mg/kg的他莫昔芬5天,然后在选定的时间间隔内杀死。 RNA的qPCR分析显示,在注射他莫昔芬3天后,Med1表达开始下降(约70％减少),并且注射5天后,心脏中的Med1表达几乎不可检测。成年小鼠中他莫昔芬诱导的心脏特异性Med1(TmcsMed1 -/-)破坏引起扩张性心肌病[3]。

[动物实验]

小鼠[3]然后给予7周龄的TmcsMed1 - / - 小鼠和野生型同窝小鼠，以65mg / kg体重的日剂量腹膜内给予他莫昔芬5天，然后在开始他莫昔芬治疗后以选定的间隔杀死。对于每个实验，使用3至5只小鼠作为对照和csMed1 - / - 。为了获得存活曲线，使用41 csMed1 - / - 和41 csMed1fl / fl小鼠。使用他莫昔芬诱导模型，将13只TmcsMed - / - 小鼠和相同数量的同窝仔畜用于存活曲线实验。动物安乐死的具体标准包括缺乏食物或水摄入，缓慢或无活动，心跳加弱或缺乏，胸部无心悸以及无呼吸运动。通过腹膜内戊巴比妥注射以150mg / kg体重的剂量对小鼠实施安乐死，以使痛苦最小化。

[参考文献]

[1]. Osborne CK. Tamoxifen in the treatment of breast cancer. N Engl J Med. 1998 Nov 26;339(22):1609-18.

[2]. Hawariah A, et al. In vitro response of human breast cancer cell lines to the growth-inhibitory effects of styrylpyrone derivative (SPD) and assessment of its antiestrogenicity. Anticancer Res. 1998 Nov-Dec;18(6A):4383-6.

[3]. Jia Y, et al. Cardiomyocyte-Specific Ablation of Med1 Subunit of the Mediator Complex Causes Lethal DilatedCardiomyopathy in Mice. PLoS One. 2016 Aug 22;11(8):e0160755.

[相关活性小分子]

枸橼酸他莫昔芬物理化学性质

[ 沸点 ]:
665.9ºC at 760 mmHg

[ 熔点 ]:
140-144 °C

[ 分子式 ]:
C₃₂H₃₇NO₈

[ 分子量 ]:
563.638

[ 闪点 ]:
356.5ºC

[ 精确质量 ]:
563.251892

[ PSA ]:
144.60000

[ LogP ]:
4.74760

[ 外观性状 ]:
白色至灰白色粉末

[ 储存条件 ]:
2-8°C

[ 水溶解性 ]:
slightly soluble

枸橼酸他莫昔芬MSDS

详细MSDS(安全技术说明书)

枸橼酸他莫昔芬毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: KH2387000

CAS REGISTRY NUMBER :: 54965-24-1

LAST UPDATED :: 199703

DATA ITEMS CITED :: 39

MOLECULAR FORMULA :: C26-H29-N-O.C6-H8-O7

MOLECULAR WEIGHT :: 563.70

WISWESSER LINE NOTATION :: L6TJ AYR&UY2&R& DO2N1&1 &QV1XQVQ1VQ

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 154 mg/kg/1Y-I

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - visual field changes Sense Organs and Special Senses (Eye) - retinal changes (pigmentary depositions, retinitis, other)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 3600 ug/kg/9D-I

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Gastrointestinal - nausea or vomiting Nutritional and Gross Metabolic - changes in calcium

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1190 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Lungs, Thorax, or Respiration - respiratory depression Nutritional and Gross Metabolic - weight loss or decreased weight gain

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 575 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Lungs, Thorax, or Respiration - respiratory depression Nutritional and Gross Metabolic - weight loss or decreased weight gain

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >5 gm/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 62500 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 :: 3100 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 - mouse

DOSE/DURATION :: 218 mg/kg

TOXIC EFFECTS :: Skin and Appendages - hair

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >5 gm/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 62500 ug/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 :: Rodent - rat

DOSE/DURATION :: 2450 ug/kg/5W-I

TOXIC EFFECTS :: Kidney, Ureter, Bladder - changes in bladder weight Blood - changes in platelet count Related to Chronic Data - changes in prostate weight

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 127 mg/kg/26W-I

TOXIC EFFECTS :: Liver - changes in liver weight Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol) Blood - changes in leukocyte (WBC) count

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 15512 mg/kg/1Y-I

TOXIC EFFECTS :: Tumorigenic - Carcinogenic by RTECS criteria Liver - tumors

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 1216 ug/kg

SEX/DURATION :: female 22 week(s) pre-mating

TOXIC EFFECTS :: Reproductive - Maternal Effects - uterus, cervix, vagina Reproductive - Maternal Effects - menstrual cycle changes or disorders Reproductive - Maternal Effects - other effects

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 200 ug/kg

SEX/DURATION :: female 4 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - female fertility index (e.g. # females pregnant per # sperm positive females; # females pregnant per # females mated)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 90 ug/kg

SEX/DURATION :: female 2-4 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - pre-implantation mortality (e.g. reduction in number of implants per female; total number of implants per corpora lutea)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 300 ug/kg

SEX/DURATION :: female 3 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Maternal Effects - uterus, cervix, vagina

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 24500 ug/kg

SEX/DURATION :: male 35 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Paternal Effects - testes, epididymis, sperm duct Reproductive - Paternal Effects - prostate, seminal vesicle, Cowper's gland, accessory glands

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 100 ug/kg

SEX/DURATION :: female 1 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Fertility - other measures of fertility

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 500 ug/kg

SEX/DURATION :: female 1 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Maternal Effects - ovaries, fallopian tubes Reproductive - Maternal Effects - uterus, cervix, vagina

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

DOSE :: 50 ug/kg

SEX/DURATION :: female 4 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - pre-implantation mortality (e.g. reduction in number of implants per female; total number of implants per corpora lutea)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

DOSE :: 500 ug/kg

SEX/DURATION :: female 1 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Fertility - other measures of fertility

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

DOSE :: 3 ug/kg

SEX/DURATION :: female 3 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Maternal Effects - uterus, cervix, vagina

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 5 mg/kg

SEX/DURATION :: female 3-7 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - pre-implantation mortality (e.g. reduction in number of implants per female; total number of implants per corpora lutea)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 34 mg/kg

SEX/DURATION :: female 10-26 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Effects on Newborn - live birth index (measured after birth)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 14 mg/kg

SEX/DURATION :: female 20-26 day(s) after conception

TOXIC EFFECTS :: Reproductive - Maternal Effects - parturition

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intramuscular

DOSE :: 1500 ug/kg

SEX/DURATION :: female 1-3 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - female fertility index (e.g. # females pregnant per # sperm positive females; # females pregnant per # females mated) Reproductive - Fertility - pre-implantation mortality (e.g. reduction in number of implants per female; total number of implants per corpora lutea)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 500 ug/kg

SEX/DURATION :: female 1 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Fertility - other measures of fertility

TYPE OF TEST :: DNA adduct

TYPE OF TEST :: Cytogenetic analysis

TYPE OF TEST :: Sex chromosome loss and nondisjunction

TYPE OF TEST :: Micronucleus test

TYPE OF TEST :: Cytogenetic analysis

MUTATION DATA

TEST SYSTEM :: Rodent - hamster

DOSE/DURATION :: 10 mg/kg

REFERENCE :: CNREA8 Cancer Research. (Public Ledger Building, Suit 816, 6th & Chestnut Sts., Philadelphia, PA 19106) V.1- 1941- Volume(issue)/page/year: 52,1360,1992 *** 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: 66,253,1996 IARC Cancer Review:Human 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: 66,253,1996 IARC Cancer Review:Group 1 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: 66,253,1996 TOXICOLOGY REVIEW PBPSDY Pharmacological and Biochemical Properties of Drug Substances. (American Pharmaceutical Assoc., 2215 Constitution Ave., NW, Washington, DC 20037) V.1- 1977- Volume(issue)/page/year: 2,355,1979 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X4010 No. of Facilities: 66 (estimated) No. of Industries: 1 No. of Occupations: 2 No. of Employees: 2077 (estimated) No. of Female Employees: 1054 (estimated)

枸橼酸他莫昔芬安全信息

[ 符号 ]:

GHS07, GHS08

[ 信号词 ]:
Danger

[ 危害声明 ]:
H302-H350-H360

[ 警示性声明 ]:
P201-P280-P301 + P312 + P330-P308 + P313

[ 个人防护装备 ]:
Eyeshields;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) ]:
R22;R45

[ 安全声明 (欧洲) ]:
S53-S36/37/39-S45

[ 危险品运输编码 ]:
UN 3077 9 / PGIII

[ WGK德国 ]:
3

[ RTECS号 ]:
KH2387000

[ 海关编码 ]:
2922199090

枸橼酸他莫昔芬合成路线

详细合成路线

枸橼酸他莫昔芬上下游产品

枸橼酸他莫昔芬上游产品

枸橼酸他莫昔芬下游产品

枸橼酸他莫昔芬海关

[ 海关编码 ]: 2922199090

[ 中文概述 ]:
2922199090. 其他氨基醇及其醚，酯和它们的盐（但含一种以上含氧基的除外）. 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, 乙醇胺及其盐应报明色度, 乙醇胺及其盐应报明包装

[ Summary ]:
2922199090. other amino-alcohols, other than those containing more than one kind of oxygen function, their ethers and esters; salts thereof. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:30.0%

枸橼酸他莫昔芬文献

TGF-beta receptor type-2 expression in cancer-associated fibroblasts regulates breast cancer cell growth and survival and is a prognostic marker in pre-menopausal breast cancer.

Oncogene 34(1) , 27-38, (2015)

Transforming growth factor-beta (TGF-β) is a pleiotropic cytokine with the capability to act as tumour suppressor or tumour promoter depending on the cellular context. TGF-beta receptor type-2 (TGFBR2...

Comparison of tamoxifen and letrozole response in mammary preneoplasia of ER and aromatase overexpressing mice defines an immune-associated gene signature linked to tamoxifen resistance.

Carcinogenesis 36(1) , 122-32, (2015)

Response to breast cancer chemoprevention can depend upon host genetic makeup and initiating events leading up to preneoplasia. Increased expression of aromatase and estrogen receptor (ER) is found in...

Exposure to the polyester PET precursor--terephthalic acid induces and perpetuates DNA damage-harboring non-malignant human breast cells.

Carcinogenesis 36(1) , 168-76, (2015)

Identification of early perturbations induced in cells from non-cancerous breast tissue is critical for understanding possible breast cancer risk from chemical exposure. We have demonstrated previousl...

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