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枸橼酸托瑞米芬

枸橼酸托瑞米芬

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?枸橼酸托瑞米芬名称


















中文名

枸橼酸托瑞米芬
英文名

Toremifene Citrate
中文别名


2(4-(4-氯-1,2-二苯基-1-丁烯基)苯氧基-N,N-二甲基乙胺枸橼酸盐




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柠檬酸托瑞米芬




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2[4-(4-氯-1,2-二苯基-1-丁烯基)苯氧基-N,N-二甲基乙胺枸橼酸盐



英文别名
更多





?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



溶解度

体外:

在DMSO中10mM


储备液

1 mM 1.6720 mL 8.3601 mL 16.7202 mL
5 mM 0.3344 mL 1.6720 mL 3.3440 mL
10 mM 0.1672 mL 0.8360 mL 1.6720 mL


存储

粉末 -20℃下 3年
4℃下 2年
在溶剂中 -80℃下 6个月
-20℃下 1个月


运输

室温;可能会有所不同
SMILES

ClCC/C(C1=CC=CC=C1)=C(C2=CC=C(OCCN(C)C)C=C2)C3=CC=CC=C3.O=C(CC(C(O)=O)(O)CC(O)=O)O
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




Elacestrant dihydrochloride



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AZD9496



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山奈酚



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3-[4-[[2,4-二(三氟甲基)苄基]氧基]-3-甲氧基苯基]-2-氰基-N-(5-三氟甲基-[1,3,4]噻二唑-2-基)丙烯酰胺



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雌酚酮



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Brilanestrant



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原人参三醇



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27-羟基胆固醇



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己烯雌酚



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PHTPP



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2,3-双(4-羟苯基)丙腈



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雌马酚



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胆固醇



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5,7-二羟黄酮



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Endoxifen Z-异构体盐酸盐






?枸橼酸托瑞米芬物理化学性质











































密度 1.045g/cm3
沸点 535.1?C at 760 mmHg
熔点 158-164?C
分子式 C32H36ClNO8
分子量 598.083
闪点 277.4?C
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




枸橼酸托瑞米芬毒性英文版






?枸橼酸托瑞米芬安全信息


































符号

GHS05

GHS07

GHS09


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33

更多文献














Use of SERMs for treatment in postmenopausal women

J. Steroid Biochem. Mol. Biol. 142 , 142-54, (2014)

? 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…









?枸橼酸托瑞米芬英文别名










































2-[4-[(Z)-4-chloro-1,2-diphenylbut-1-enyl]phenoxy]-N,N-dimethylethanamine,2-hydroxypropane-1,2,3-tricarboxylic acid


2-{4-[(1Z)-4-Chloro-1,2-diphenyl-1-buten-1-yl]phenoxy}-N,N-dimethylethanamine 2-hydroxy-1,2,3-propanetricarboxylate (salt)


2-{4-[(1Z)-4-Chloro-1,2-diphenylbut-1-en-1-yl]phenoxy}-N,N-dimethylethanamine 2-hydroxypropane-1,2,3-tricarboxylate (1:1)


2-{4-[(1Z)-4-Chloro-1,2-diphenyl-1-buten-1-yl]phenoxy}-N,N-dimethylethanamine 2-hydroxy-1,2,3-propanetricarboxylate (1:1)


Toremifene Citrate


2-{4-[(1Z)-4-chloro-1,2-diphenylbut-1-en-1-yl]phenoxy}-N,N-dimethylethanamine 2-hydroxypropane-1,2,3-tricarboxylate (salt)


ethanamine, 2-[4-[(1Z)-4-chloro-1,2-diphenyl-1-butenyl]phenoxy]-N,N-dimethyl-, 2-hydroxy-1,2,3-propanetricarboxylate (1:1) (salt)


2-Hydroxypropan-1,2,3-tricarbons?ure–2-{4-[(1Z)-4-chlor-1,2-diphenylbut-1-en-1-yl]phenoxy}-N,N-dimethylethanamin(1:1)


acide 2-hydroxypropane-1,2,3-tricarboxylique – 2-{4-[(1Z)-4-chloro-1,2-diphénylbut-1-én-1-yl]phénoxy}-N,N-diméthyléthanamine (1:1)


Ethanamine, 2-[4-[(1Z)-4-chloro-1,2-diphenyl-1-buten-1-yl]phenoxy]-N,N-dimethyl-, 2-hydroxy-1,2,3-propanetricarboxylate (1:1) (salt)


Toremifene (Citrate)








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