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

2-{4-[(1E)-1,2-diphenylbut-1-en-1-yl]phenoxy}-N,N-dimethylethanamine 2-hydroxypropane-1,2,3-tricarboxylate (salt) - Names and Identifiers

Name	Tamoxifen citrate
Synonyms	TAMOXIPHEN Tamoxifen citrate Tamoxiphen Citrate TomixipheneCitrate TAMOXIFENCITRATE,USP TAMOXIFEN CITRATE ANTI-ESTROGEN, PROTEI (Z)-1-(4-Dimethylaminoethoxyphenyl)-1,2-diphenyl-1-butene Citrate 1-p-beta-dimethylaminoethoxyphenyl-trans-1,2-diphenylbut-1-ene citrate (z)-2-[4-(1,2-diphenyl-1-butenyl)phenoxyl]-n,n-dimethyl-ethanamine-citrate 2-{4-[(1E)-1,2-diphenylbut-1-en-1-yl]phenoxy}-N,N-dimethylethanamine 2-hydroxypropane-1,2,3-tricarboxylate (salt) (Z)-[2-[4-(1,2-diphenylbut-1-enyl)phenoxy]ethyl]dimethylammonium dihydrogen 2-hydroxypropane-1,2,3-tricarboxylate
CAS	54965-24-1
EINECS	259-415-2
InChI	InChI=1/C26H29NO.C6H8O7/c1-4-25(21-11-7-5-8-12-21)26(22-13-9-6-10-14-22)23-15-17-24(18-16-23)28-20-19-27(2)3;7-3(8)1-6(13,5(11)12)2-4(9)10/h5-18H,4,19-20H2,1-3H3;13H,1-2H2,(H,7,8)(H,9,10)(H,11,12)/p-3/b26-25-

2-{4-[(1E)-1,2-diphenylbut-1-en-1-yl]phenoxy}-N,N-dimethylethanamine 2-hydroxypropane-1,2,3-tricarboxylate (salt) - Physico-chemical Properties

Molecular Formula	C32H37NO8
Molar Mass	563.64
Melting Point	140-144 °C
Water Solubility	slightly soluble
Solubility	methanol: soluble50mg/mL, clear, colorless
Appearance	Powder
Color	White to off-white
Merck	14,9048
Storage Condition	2-8°C
Stability	Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 2 months.
Sensitive	Light Sensitive & Hygroscopic
MDL	MFCD00058321
Physical and Chemical Properties	Melting point 140-144°C water-soluble snyly soluble
Use	For the treatment of advanced, recurrent breast and ovarian cancer and other conditions

2-{4-[(1E)-1,2-diphenylbut-1-en-1-yl]phenoxy}-N,N-dimethylethanamine 2-hydroxypropane-1,2,3-tricarboxylate (salt) - Risk and Safety

Risk Codes	R45 - May cause cancer R60 - May impair fertility R61 - May cause harm to the unborn child R22 - Harmful if swallowed R64 - May cause harm to breast-fed babies R36/37/38 - Irritating to eyes, respiratory system and skin.
Safety Description	S53 - Avoid exposure - obtain special instructions before use. S36/37/39 - Wear suitable protective clothing, gloves and eye/face protection. S45 - In case of accident or if you feel unwell, seek medical advice immediately (show the label whenever possible.) S36 - Wear suitable protective clothing. S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice.
UN IDs	UN 3077 9 / PGIII
WGK Germany	3
RTECS	KH2387000
HS Code	29225090
Hazard Class	IRRITANT
Toxicity	LD50 in mice, rats (mg/kg): 200, 600 i.p.; 62.5, 62.5 i.v.; 3000-6000, 1200-2500 orally (Furr, Jordan)

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

Authoritative Data Verified Data

This product is (Z )-N, n-dimethyl-2-[4-(1, 2-diphenyl-1-butenyl) phenoxy] ethylamine citrate. Calculated as dry, containing no. C6H807 C26H29NO. Not less than 99.0%.

Last Update：2024-01-02 23:10:35

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

Authoritative Data Verified Data

This product is white or off-white crystalline powder; Odorless.
This product is dissolved in methanol, slightly soluble in ethanol or acetone, very slightly soluble in chloroform, almost insoluble in water; Soluble in glacial acetic acid.

melting point

The melting point of this product (General rule 0612) is 142~148°C, and it is decomposed at the same time during melting.

Last Update：2022-01-01 13:38:50

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

Authoritative Data Verified Data

take an appropriate amount of this product, add 5ml of vinegar-pyridine (1:5), shake well, heat on a water bath, and change the color of the solution from yellow to red.
take this product, add anhydrous ethanol to dissolve and dilute to prepare a solution containing about 10ug per lml, and measure by UV-Vis spectrophotometry (General rule 0401), there is a maximum absorption at wavelengths of 238nm and 278nm.
The infrared absorption spectrum of this product should be consistent with that of the control (Spectrum set 265); If not, the product is recrystallized with acetone for determination.

Last Update：2022-01-01 13:38:51

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

Authoritative Data Verified Data

Related substances

operation in the dark, ready to use the new system. Take this product, precision weighing, add mobile phase dissolution and quantitative dilution to make a solution containing about 1.5mg per lml, as a test solution; Take appropriate amount of precision, A solution containing 7.5ug per 1 ml was prepared by quantitative dilution with mobile phase and used as a control solution. In addition, the reference substance of tamoxifen isomer (impurity I) was selected and precision weighed, the mobile phase was added to dissolve and quantitatively dilute to prepare a solution containing about 7.5ug per 1 ml as a control solution. According to the high performance liquid chromatography (General 0512) test, using eighteen alkyl silane bonded silica gel as filler, phosphate buffer solution (sodium dihydrogen phosphate 4.8g and N,N-dimethyl octylamine g, water was added to dissolve and diluted to 3.0 ML, and the pH was adjusted to with phosphoric acid. Acetonitrile (60:40) was used as mobile phase, and the detection wavelength was 240mn. Take the same amount of mixed solution 10 u1 of control solution and reference solution, and inject it into human Liquid Chromatograph. The number of theoretical plates shall not be less than 2000 according to the peak of tamoxifen E-isomer, the degree of separation of the tamoxifen E-isomer peak from the principal component peak (tamoxifen Z-isomer) should be greater than 3.0. The test solution, the control solution and the reference solution are respectively injected into the human liquid chromatograph, and the chromatogram is recorded to 2 times of the retention time of the main component peak. If there is a peak in the chromatogram of the test solution that is consistent with the retention time of the peak of tamoxifen E-isomer in the chromatogram of the reference solution, the peak area shall be calculated according to the external standard method, and shall not exceed 0.5%; if there are other impurity peaks, the single impurity peak area shall not be greater than the main peak area of the control solution (0.5%), and the sum of other impurity peak areas shall not be greater than 2 times (1.0%) of the main peak area of the control solution.

loss on drying

take this product and dry it at 105°C for 4 hours, and the weight loss shall not exceed 0.5% (General rule 0831).

Last Update：2022-01-01 13:38:51

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

Authoritative Data Verified Data

take this product about 0.35g, precision weighing, add glacial acetic acid 50ml, micro temperature to dissolve, add crystal violet indicator solution 1 drop, with perchloric acid titration solution (O. 1 mol/L) titration to the solution is blue-green, and the result of the titration is corrected with a blank test. Each 1 ml of perchloric acid titration solution (0.1 mol/ L) corresponds to 56.36mg of C26H29NO. C6H807.

Last Update：2022-01-01 13:38:52

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

Authoritative Data Verified Data

antineoplastic agents.

Last Update：2022-01-01 13:38:52

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

Authoritative Data Verified Data

light-shielded, sealed, and stored in a dry place.

Last Update：2022-01-01 13:38:52

2-{4-[(1E)-1,2-diphenylbut-1-en-1-yl]phenoxy}-N,N-dimethylethanamine 2-hydroxypropane-1,2,3-tricarboxylate (salt) - Tamoxifen Citrate Tablets

Authoritative Data Verified Data

This product contains tamoxifen citrate according to tamoxifen (C26H29NO), should be 90.0% ~ 110.0% of the label amount.

trait

This product is white tablet.

identification

take an appropriate amount of the fine powder of this product, and show the same reaction according to the Identification Test (1) under the item of tamoxifen citrate.
the sample solution under the content measurement item was taken and measured by ultraviolet-visible spectrophotometry (General 0401), and the maximum absorption was found at wavelengths of NM and Nm.

examination

the related substances were operated in the dark, and the new system was ready for use. Accurately weigh an appropriate amount of the fine powder of this product (about 50mg equivalent to tamoxifen), put it in a 50ml measuring flask, add an appropriate amount of mobile phase, sonicate for 5 minutes, let it cool, and dilute it to the scale with mobile phase, shake well, centrifuge, take the supernatant as the test solution; Take the appropriate amount of precision, quantitative dilution with mobile phase to make a solution containing 5ul per 1 ml, as a control solution; in addition, the reference substance of tamoxifen isomer was carefully weighed, dissolved and quantitatively diluted with mobile phase to prepare a solution containing about 7.5ug per 1 ml, which was used as the reference solution. The method for the determination of related substances of tamoxifen citrate was used. If there is a peak in the chromatogram of the test solution that is consistent with the retention time of the peak of tamoxifen E-isomer in the chromatogram of the reference solution, the peak area shall not be greater than the main peak area of the reference solution (0.75% ); if there are other impurity peaks, the single impurity peak area shall not be greater than the main peak area of the control solution (0.5%), and the sum of other impurity peak areas shall not be greater than 2 times (1.0%) of the main peak area of the control solution.
Content uniformity: Take 1 tablet of this product, put it in a mortar, grind it finely, grind it with an appropriate amount of absolute ethanol, and transfer it to a 100ml measuring flask in portions with absolute ethanol, from the "shaking for 15 minutes", the content shall be determined according to law and shall comply with the regulations (General rule 0941).
the dissolution of this product, according to the dissolution and release determination method (General 0931 second method), with 0.02mol/L hydrochloric acid solution as the dissolution medium, the speed is 100 rpm, operate according to law, after 30 minutes, take 10ml of solution, filter, continue filtrate according to UV-visible spectrophotometry (General rule 0401), measure absorbance at 275nm wavelength, the elution amount of each tablet was calculated as the absorption coefficient of C26H29NO was 311. The limit is 75% of the labeled amount and shall be in accordance with the provisions.
others shall be in accordance with the relevant provisions under the item of tablets (General rule 0101).

Content determination

Take 20 tablets of this product, precision weighing, fine grinding, precision weighing appropriate amount (about equivalent to tamoxifen 10 mg), put it in a 100ml measuring flask, add the right amount of anhydrous ethanol, shake for 15 minutes, sonicate for 15 minutes, dissolve tamoxifen citrate, let it cool, dilute to the scale with absolute ethanol, shake well, filter, and take 5ml continuous filtrate with precision, place in 50ml measuring flask, dilute to the scale with absolute ethanol, shake well, as a test solution, according to UV-visible spectrophotometry (General rule 0401), the absorbance was measured at a wavelength of 238nm and calculated as an absorption coefficient of C26H29NO of 531.

specification

lOmg (as tamoxifen)

storage

light shielding, sealed storage.

Last Update：2022-01-01 13:38:53

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

Shanghai Worldyang Chemical Co.,Ltd.

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

Tamoxifen citrate

CAS: 54965-24-1

Molecular Formula: C32H37NO8

2-{4-[(1E)-1,2-diphenylbut-1-en-1-yl]phenoxy}-N,N-dimethylethanamine 2-hydroxypropane-1,2,3-tricarboxylate (salt) - Names and Identifiers

2-{4-[(1E)-1,2-diphenylbut-1-en-1-yl]phenoxy}-N,N-dimethylethanamine 2-hydroxypropane-1,2,3-tricarboxylate (salt) - Physico-chemical Properties

2-{4-[(1E)-1,2-diphenylbut-1-en-1-yl]phenoxy}-N,N-dimethylethanamine 2-hydroxypropane-1,2,3-tricarboxylate (salt) - Risk and Safety

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

Authoritative Data Verified Data

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

Authoritative Data Verified Data

melting point

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

Authoritative Data Verified Data

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

Authoritative Data Verified Data

Related substances

loss on drying

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

Authoritative Data Verified Data

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

Authoritative Data Verified Data

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

Authoritative Data Verified Data

2-{4-[(1E)-1,2-diphenylbut-1-en-1-yl]phenoxy}-N,N-dimethylethanamine 2-hydroxypropane-1,2,3-tricarboxylate (salt) - Tamoxifen Citrate Tablets

Authoritative Data Verified Data

trait

identification

examination

Content determination

category

specification

storage

Supplier List

2-{4-[(1E)-1,2-diphenylbut-1-en-1-yl]phenoxy}-N,N-dimethylethanamine 2-hydroxypropane-1,2,3-tricarboxylate (salt) Request for Quotation

Tamoxifen citrate

CAS: 54965-24-1

Molecular Formula: C32H37NO8

2-{4-[(1E)-1,2-diphenylbut-1-en-1-yl]phenoxy}-N,N-dimethylethanamine 2-hydroxypropane-1,2,3-tricarboxylate (salt) - Names and Identifiers

2-{4-[(1E)-1,2-diphenylbut-1-en-1-yl]phenoxy}-N,N-dimethylethanamine 2-hydroxypropane-1,2,3-tricarboxylate (salt) - Physico-chemical Properties

2-{4-[(1E)-1,2-diphenylbut-1-en-1-yl]phenoxy}-N,N-dimethylethanamine 2-hydroxypropane-1,2,3-tricarboxylate (salt) - Risk and Safety

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

Authoritative Data Verified Data

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

Authoritative Data Verified Data

melting point

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

Authoritative Data Verified Data

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

Authoritative Data Verified Data

Related substances

loss on drying

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

Authoritative Data Verified Data

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

Authoritative Data Verified Data

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

Authoritative Data Verified Data

2-{4-[(1E)-1,2-diphenylbut-1-en-1-yl]phenoxy}-N,N-dimethylethanamine 2-hydroxypropane-1,2,3-tricarboxylate (salt) - Tamoxifen Citrate Tablets

Authoritative Data Verified Data

trait

identification

examination

Content determination

category

specification

storage

Supplier List

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