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枸橼酸托瑞米芬

枸橼酸托瑞米芬用途

Toremifene(NK 622; FC 1157a)柠檬酸盐是第二代选择性雌激素受体调节剂,对雌激素受体的IC50为1μM。

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枸橼酸托瑞米芬名称

[ CAS 号 ]:
89778-27-8

[ 中文名 ]:
枸橼酸托瑞米芬

[ 英文名 ]:
Toremifene Citrate

[中文别名 ]:

柠檬酸托瑞米芬

[英文别名 ]:

Toremifene Citrate
Toremifene (Citrate)

枸橼酸托瑞米芬生物活性

[ 描述 ]:

Toremifene(NK 622; FC 1157a)柠檬酸盐是第二代选择性雌激素受体调节剂,对雌激素受体的IC50为1μM。

[ 相关类别 ]:

信号通路 >> 其他 >> 雌激素受体/ERR

研究领域 >> 癌症

[参考文献]

[1]. Matthew R Smith, Selective Estrogen Receptor Modulators to Prevent Treatment-Related Osteoporosis.Rev Urol. 2005; 7(Suppl 3): S30-S35.

[2]. Gauri J Sabnis, Luciana Macedo, Olga Goloubeva, Toremifene - Atamestane; Alone or In Combination: Predictions from the Preclinical Intratumoral Aromatase Model. J Steroid Biochem Mol Biol. 2008 January; 108(1-2): 1-7.

[3]. Taneja SS, Morton R, Barnette G, Prostate cancer diagnosis among men with isolated high-grade intraepithelial neoplasia enrolled onto a 3-year prospective phase III clinical trial of oral toremifene. J Clin Oncol. 2013 Feb 10;31(5):523-9.

[相关活性小分子]

枸橼酸托瑞米芬物理化学性质

[ 密度 ]:
1.045g/cm3

[ 沸点 ]:
535.1ºC at 760 mmHg

[ 熔点 ]:
158-164ºC

[ 分子式 ]:
C₃₂H₃₆ClNO₈

[ 分子量 ]:
598.083

[ 闪点 ]:
277.4ºC

[ 精确质量 ]:
597.212952

[ PSA ]:
144.60000

[ LogP ]:
4.96650

[ 外观性状 ]:
白色或近乎于白色粉末

[ 折射率 ]:
1.416-1.418

[ 储存条件 ]:
-20°C Freezer

[ 水溶解性 ]:
DMSO: >10mg/mL

枸橼酸托瑞米芬毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: KH2156800

CAS REGISTRY NUMBER :: 89778-27-8

LAST UPDATED :: 199706

DATA ITEMS CITED :: 10

MOLECULAR FORMULA :: C26-H28-Cl-N-O.C6-H8-O7

MOLECULAR WEIGHT :: 598.14

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 3 gm/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - effect, not otherwise specified Kidney, Ureter, Bladder - incontinence Skin and Appendages - hair

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 520 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Kidney, Ureter, Bladder - incontinence Skin and Appendages - hair

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Primate - monkey

DOSE/DURATION :: >2 gm/kg

TOXIC EFFECTS :: Gastrointestinal - hypermotility, diarrhea

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 364 mg/kg/52W-C

TOXIC EFFECTS :: Brain and Coverings - changes in brain weight Blood - changes in erythrocyte (RBC) count Related to Chronic Data - changes in uterine weight

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 87360 ug/kg/2Y-C

TOXIC EFFECTS :: 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 :: 3640 mg/kg/52W-C

TOXIC EFFECTS :: Liver - changes in liver weight Blood - pigmented or nucleated red blood cells Related to Chronic Data - changes in ovarian weight

MUTATION DATA

TEST SYSTEM :: Rodent - rat

DOSE/DURATION :: 35 mg/kg

REFERENCE :: CRNGDP Carcinogenesis (London). (Oxford Univ. Press, Pinkhill House, Southfield Road, Eynsham, Oxford OX8 1JJ, UK) V.1- 1980- Volume(issue)/page/year: 17,1051,1996 *** REVIEWS *** 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: 66,367,1996 IARC Cancer Review:Animal 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: 66,367,1996 IARC Cancer Review:Group 3 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: 66,367,1996

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枸橼酸托瑞米芬安全信息

[ 符号 ]:

GHS05, GHS07, GHS09

[ 信号词 ]:
Danger

[ 危害声明 ]:
H302-H318-H410

[ 警示性声明 ]:
P280-P301 + P312 + P330-P305 + P351 + P338 + P310

[ 危害码 (欧洲) ]:
Xi: Irritant;

[ 风险声明 (欧洲) ]:
R36/37/38

[ 安全声明 (欧洲) ]:
26-37/39

[ 危险品运输编码 ]:
UN 3077 9 / PGIII

[ RTECS号 ]:
KH2156700

[ 海关编码 ]:
2942000000

枸橼酸托瑞米芬海关

[ 海关编码 ]: 2942000000

枸橼酸托瑞米芬文献

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• FDA approved selective estrogen receptor modulators (SERMs) prevent and treat breast cancer, osteoporosis and dyspareunia. • SERMs have varying agonist and antagonist activities at the level of the ...

Novel off-target effect of tamoxifen--inhibition of acid ceramidase activity in cancer cells.

Biochim. Biophys. Acta 1831(12) , 1657-64, (2013)

Acid ceramidase (AC), EC 3.5.1.23, a lysosomal enzyme, catalyzes the hydrolysis of ceramide to constituent sphingoid base, sphingosine, and fatty acid. Because AC regulates the levels of pro-apoptotic...

Prostate cancer diagnosis among men with isolated high-grade intraepithelial neoplasia enrolled onto a 3-year prospective phase III clinical trial of oral toremifene.

J. Clin. Oncol. 31(5) , 523-9, (2013)

Prostate cancer (PCa) prevention remains an appealing strategy for the reduction of overtreatment and secondary adverse effects. We evaluated the efficacy of toremifene citrate 20 mg in PCa prevention...

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