Name | Exemestane |
Synonyms | PNU155971 Exemestan ExeMestine Exemestone Exemestane ExeMestane (USP) Exemestane(Aromasin) ExeMestane(AroMasin) 6-Methylenandrosta-1,4-diene-3,17-dione 1,4-Androstadien-3,17-dione-6-Methylene-d2 6-methylideneandrosta-1,4-diene-3,17-dione (8ξ,9ξ,14ξ)-6-methylideneandrosta-1,4-diene-3,17-dione ExeMestane SynonyMs 6-Methylenandrosta-1,4-diene-3,17-dione 10,13-Dimethyl-6-methylidene-7,8,9,10,11,12,13,14,15,16-decahydrocyclopenta[a]phenanthrene- (8R,9S,10R,13S,14S)-10,13-Dimethyl-6-methylene-7,8,9,11,12,13,15,16-octahydro-6H-cyclopenta[a]phenanthrene-3,17(10H,14H)-dione (8R,9S,10R,13S,14S)-10,13-diMethyl-6-Methylene-7,8,9,10,11,12,13,14,15,16-decahydro-3H-cyclopenta[a]phenanthrene-3,17(6H)-dione |
CAS | 107868-30-4 |
EINECS | 643-090-2 |
InChI | InChI=1/C20H24O2/c1-12-10-14-15-4-5-18(22)20(15,3)9-7-16(14)19(2)8-6-13(21)11-17(12)19/h6,8,11,14-16H,1,4-5,7,9-10H2,2-3H3/t14?,15?,16?,19-,20+/m1/s1 |
InChIKey | BFYIZQONLCFLEV-DAELLWKTSA-N |
Molecular Formula | C20H24O2 |
Molar Mass | 296.4 |
Density | 1.13±0.1 g/cm3(Predicted) |
Melting Point | 155.13°C |
Boling Point | 453.7±45.0 °C(Predicted) |
Flash Point | 169°C |
Solubility | DMSO: ≥20mg/mL |
Vapor Presure | 2.02E-08mmHg at 25°C |
Appearance | powder |
Color | white to off-white |
Storage Condition | 2-8°C |
Refractive Index | 1.572 |
Physical and Chemical Properties | Melting Point: 155.13°C |
Risk Codes | R60 - May impair fertility R61 - May cause harm to the unborn child R51 - Toxic to aquatic organisms |
Safety Description | S53 - Avoid exposure - obtain special instructions before use. S22 - Do not breathe dust. S36/37 - Wear suitable protective clothing and gloves. S57 - Use appropriate container to avoid environmental contamination. |
WGK Germany | 3 |
HS Code | 29372900 |
white solid. mp 188~191 deg C; UV maximum absorption of 247nm(& epsilon;13750). Soluble in DMF, soluble in methanol, almost insoluble in water.
androstin-4-ene-3, 17-= ketone and triethyl orthoformate are dissolved in tetrahydrofuran and anhydrous ethanol and reacted in the presence of p-toluenesulfonic acid, N-methylaniline and formaldehyde solution were then added and the reaction was continued. The resulting reaction product was dissolved in benzoic acid and anhydrous dioxane, dichlorodicyanobenzoquinone (DDQ) to give exemestane.
This product is 6-methylidene-1, 4-dien-3, 17-Dione. The content of C20H2402 shall be 98.0% ~ 102.0% calculated as dry product.
This product is white or white crystalline powder; Odorless.
This product is soluble in three gas methane, dissolved in ethyl acetate, acetone, methanol or ethyl alcohol, almost insoluble in water.
melting point
The melting point of this product (General 0612) is 192~196°C.
take about 0.5g of this product, accurately weigh it, put it in a 50ml measuring flask, add ethanol to dissolve and dilute to the scale, shake well, and determine it according to law (General rule 0621), the specific rotation was 88 ° to 298 °.
take about 25mg of this product, precision weighing, put it in 50ml measuring flask, add ethanol to dissolve and dilute to the scale, shake, take 2ml, put it in 100ml measuring flask, the absorbance was measured at a wavelength of 0401 Mn by ultraviolet-visible spectrophotometry (General 475) after being diluted to a scale with ethanol, and the absorption coefficient was 495.
developed by Pharmacia & Upj ohn. It was approved by FDA in October 1997. Antineoplastic agents, second-generation aromatase inhibitors. Exemestane is the first oral hormonal agent that selectively targets and permanently binds to aromatase, an enzyme that can never remanufacture estrogens once binding of exemestane to the enzyme occurs. Can inhibit the supply of estrogen to cancer cells and help prevent cells from continuing to grow. For the treatment of metastatic breast cancer and as an adjuvant therapy for early breast cancer.
take 0.10g of this product and add 10ml of ethanol to dissolve. The solution should be clear and colorless.
take an appropriate amount of this product, such as the mobile phase is dissolved and diluted to make a solution containing about 0.5mg per lml, as a test solution; Take 1ml for precision measurement, and put it in a 200ml measuring flask, dilute to the scale with mobile phase, shake, as a control solution, according to the chromatographic conditions under the content determination item, take 20 u1 of the test solution and the control solution, human liquid chromatograph was injected respectively, and the chromatogram was recorded to 2.5 times of the retention time of the main component peak. If there are impurity peaks in the chromatogram of the test solution, the area of a single impurity peak shall not be greater than the area of the main peak of the control solution (0.5% ) , the sum of each impurity peak area shall not be greater than 2 times (1.0%) of the main peak area of the control solution.
take about 0.2g of this product, weigh it accurately, place it in the top empty bottle, and add the internal standard solution accurately (take the appropriate amount of n-butanol, add N-methylpyrrolidone to dissolve and dilute the solution containing 0.5mg per 1 ml) 2ml, shake to dissolve, seal, as a test solution; Take toluene, cyclohexane, tetrahydrofuran, dioxane, dichloromethane, trichloromethane and methanol in appropriate amounts, precision weighing, plus the above internal standard solution dissolved and quantitatively diluted to make each 1 ml containing about 0.089mg, 0.388mg, 0.072mg, 0.038mg, 0.06mg, 0.006mg and 0.3mg of mixed solution, the precision of 2ml, in the top empty bottle, sealed, as a reference solution. Determined according to the residual solvent assay (General 0861 second method). The capillary column with polyethylene glycol (or similar polar) as the stationary liquid is used as the chromatographic column; The initial temperature is 30°C, maintained for 30 minutes, and the temperature is raised to 300°C at a rate of 20 * C per minute for 7 minutes; the inlet temperature was 200°C; The detector temperature was 220°C; The headspace bottle equilibrium temperature was 80°C and the equilibrium time was 20 minutes. Take the reference solution into the headspace, the separation degree between the peaks of each component shall meet the requirements. The test solution and the reference solution were respectively injected in the headspace, and the chromatogram was recorded, and the peak area was calculated according to the internal standard method. Toluene, cyclohexane, Tetrahydrofuran, dioxane, dichloromethane, chloroform and methanol residues shall be in accordance with the provisions.
take this product, dry to constant weight at 105°C, weight loss shall not exceed 0.5% (General rule 0831).
take l.Og of this product and check it according to law (General rule 0841). The residue left shall not exceed 0.1%.
The residue left under the item of burning residual Tong shall be inspected according to law (General rule 0821, Law 2), and the content of heavy metals shall not exceed 10 parts per million.
measured by high performance liquid chromatography (General 0512).
silica gel bonded with eighteen alkyl silane was used as a filler, and acetonitrile-water (35:65) was used as a mobile phase; The detection wavelength was 249nm; And the column temperature was 40°C. Take appropriate amount of exemestane control and impurity I control, add mobile phase to dissolve and dilute to make a mixed solution containing 2.5ug of exemestane and impurity I per 1 ml, as the system applicable solution, take 20ul injection liquid chromatograph and record the chromatogram. The resolution between exemestane peak and impurity I peak should be greater than 2.5.
take about 25mg of this product, weigh it accurately, put it in 50ml measuring flask, add appropriate amount of mobile phase to dissolve and dilute to the scale, shake well, take 5ml accurately, put it in 100ml measuring flask, dilute to the scale with mobile phase, shake well, as a test solution, and inject 20ul into the liquid chromatograph with precision, record the chromatogram; Take the exemestane reference substance, and determine with the same method. According to the external standard method to calculate the peak area, that is.
antineoplastic agents.
light shielding, sealed storage.
This product contains exemestane (C20H2402) should be 93.0% to 107.0% of the label.
This product is white or white-like tablets or film-coated tablets, white or white-like after removing the coating.
Take 20 tablets of this product, precision weighing, fine grinding, precision weighing appropriate amount (about equivalent to exemestane 25mg), put it in 50ml measuring flask, add appropriate amount of mobile phase, shake to dissolve exemestane, dilute to the scale with mobile phase, shake, filter, Take 5ml of filtrate accurately, put it in a 100ml measuring flask, dilute to the scale with mobile phase, shake well, as a test solution, precision measure 20 u1, according to the method under the determination of exemestane content, that is obtained.
Same as exemestane.
25mg
light shielding, sealed storage.
This product contains exemestane (C20H2402) should be 93.0% to 107.0% of the label.
The contents of this product are white or off-white powder or granular powder.
take the contents under the difference of loading amount, mix evenly, accurately weigh an appropriate amount (about 25mg equivalent to exemestane), put it in a 50ml measuring flask, and add an appropriate amount of mobile phase, shake to dissolve exemestane, dilute to scale with mobile phase, shake well, filter, Take 5ml of continued filtrate precisely, put it in 100ml measuring flask, dilute to scale with mobile phase, shake well, as a test solution, 20UL was accurately measured and obtained according to the method under the item of exemestane content determination.
Same as exemestane.
25mg
light shielding, sealed storage.