Shaanxi BLOOM Tech Co., Ltd. is one of the most experienced manufacturers and suppliers of anastrozole powder cas 120511-73-1 in China. Welcome to wholesale bulk high quality anastrozole powder cas 120511-73-1 for sale here from our factory. Good service and reasonable price are available.
Anastrozole powder, a chemical drug with significant medical value, has unique physical properties and provides an important foundation for medical research and clinical applications. From the appearance, Anatrazole is a white or almost white crystalline powder with the chemical formula CHN5 and a molecular weight of 293.366. It is odorless and has a bitter taste. It is easily soluble in acetonitrile or ethyl acetate, which provides convenience for its dissolution and extraction in laboratory research and pharmaceutical processes. At the same time, it dissolves in ethanol, but is almost insoluble in water. For example, its molar refractive index is 90.01, and its molar volume (cm) ³/ The mol value is 270.2, and the isotonic specific volume (90.2K) is 688.7. Surface tension (dyne/cm) is 42.1, and polarization rate (10cm) ³) It is 35.68. It is a potent selective triazole aromatase inhibitor. It can inhibit the aromatase dependent on cytochrome P-450, thereby blocking the biosynthesis of estrogen. Estrogen is one of the main factors that stimulate the growth of breast cancer cells, so anastrozole provides an effective way for the treatment of breast cancer by inhibiting the synthesis of estrogen. The chemicals in this laboratory are for laboratory use only and are strictly prohibited from being used for other purposes.
|
|
|
|
Chemical Formula |
C17H19N5 |
|
Exact Mass |
293 |
|
Molecular Weight |
293 |
|
m/z |
293 (100.0%), 294 (18.4%), 294 (1.8%), 295 (1.6%) |
|
Elemental Analysis |
C, 69.60; H, 6.53; N, 23.87 |
Anastrozole powder is a powerful and selective nonsteroidal aromatase inhibitor. Its core purpose is to treat specific types of breast cancer by inhibiting estrogen synthesis, and plays an important role in adjuvant treatment, recurrence prevention and exploratory application.
Core use: treatment of postmenopausal breast cancer
The core mechanism of action is to inhibit aromatase activity and block the conversion of androgens (such as androstenedione) to estrogens (such as estradiol) in the adrenal gland and adipose tissue. As estrogen is the main factor to stimulate the growth of breast cancer cells, reducing its level can effectively inhibit the proliferation of tumor cells. This mechanism makes it a key drug for the treatment of postmenopausal women's breast cancer:
Treatment of advanced breast cancer
It is applicable to postmenopausal women with advanced breast cancer who cannot be controlled by tamoxifen or other anti estrogen therapy. For patients with estrogen receptor negativity, if there is a positive clinical response to tamoxifen, it may also be considered for use. Its curative effect is particularly significant in patients with locally advanced or metastatic breast cancer, which can prolong disease-free survival and improve prognosis.
Adjuvant treatment of early breast cancer
As an adjuvant treatment drug for postmenopausal estrogen receptor positive early breast cancer, it can replace tamoxifen or be used sequentially (for example, tamoxifen should be used for 2-3 years first, then anastrozole). Adjuvant treatment lasting for 5 years can effectively reduce the incidence of contralateral breast cancer and the risk of distant metastasis, especially for high-risk groups such as lymph node positive.
Adjuvant therapy: optimizing management strategies for breast cancer
The auxiliary role in the treatment of breast cancer is reflected in many aspects. Through individualized programs, the curative effect is improved and side effects are reduced:
Postoperative adjuvant therapy
After breast cancer surgery, it can significantly reduce the risk of recurrence. For high-risk patients with positive lymph nodes, adjuvant therapy can reduce distant metastasis and local recurrence, and improve 5-year survival rate.
Sequential treatment strategy
For patients who initially use tamoxifen as adjuvant therapy, if disease progression or intolerable side effects occur, they can switch to continue treatment with anastrozole. This sequential strategy has shown better efficacy than a single drug in clinical trials.
Exploration of Combination Therapy
Can be used in combination with other drugs (such as ovarian function inhibitors, CDK4/6 inhibitors) to enhance efficacy.
For example, in premenopausal patients with breast cancer, anastrozole combined with ovarian function inhibitors can simulate postmenopausal status and expand its scope of application.
Preventing recurrence: interventions targeting high-risk populations
It shows potential in the field of breast cancer prevention, especially for high-risk people:
Definition of high-risk population:
It includes patients with family genetic history, BRCA gene mutation, breast atypical hyperplasia or previous breast cancer history. The risk of breast cancer in these populations is significantly higher than that in the general population.
Evidence of preventive treatment:
Clinical trials show that long-term use of anastrozole can reduce the incidence rate of breast cancer in high-risk population.
For example, in the IBIS-II trial, anastrozole reduced the risk of breast cancer by 53%, and the side effects were controllable.
Risk and Benefit Assessment:
Although preventive treatment can reduce the risk of disease, it is necessary to strictly evaluate the risks and benefits of medication. For example, long-term use may increase the risk of osteoporosis and fractures, so it is necessary to combine bone density monitoring with preventive measures such as calcium supplements and vitamin D.
Other exploratory applications: expanding treatment boundaries
In addition to breast cancer, exploratory applications in other hormone dependent diseases are also under way:
Prostate cancer
As an anti-tumor drug, prostate cancer can be treated by inhibiting androgen synthesis. Its mechanism is similar to that of breast cancer treatment, that is, inhibiting tumor growth by reducing hormone levels.
Endometriosis
By inhibiting estrogen synthesis, symptoms of endometriosis such as pain and menstrual disorders can be alleviated. However, its efficacy and safety still need further verification.
Polycystic ovary syndrome (PCOS)
Anastrozole may improve ovulation function and metabolic indicators in PCOS patients by regulating hormone levels. However, there is currently limited research on this topic, and its applicability needs to be carefully evaluated.
There are two common synthesis methods for anastrozole powder, which are described separately:
Method 1
1) а,а,а′,а′- Synthesis of Tetramethyl-5- (1H-1,2,4-triazol-1-yl methyl) -1,3-diacetonitrile benzene
Add 25g of intermediate bromate of anastrazole and 200ml of DMF to a 2000ml three necked bottle, stir at room temperature until clear, control the temperature to 25-30 ℃, add 9g of sodium triazole, complete the stirring reaction, HPLC detect the reaction endpoint, stop the reaction, add 250ml of 0.2mol/L dilute acid and 500ml of toluene, stir to separate phases, treat the organic phase twice with 100ml and 100ml of 0.2mol/L dilute hydrochloric acid, merge the dilute acid phase, wash once with 200ml of toluene, merge the toluene phase, wash twice with 300ml and 200ml of 2N hydrochloric acid, merge the acid phase, add sodium carbonate to the acid phase, adjust the pH to 6-7, stir to crystallize, and reduce to 0. Incubate at ℃ for 2 hours, filter and wash with cold water to obtain 15.2g of crude Anatrazole with a weight yield of 60.8%;
2) Purification of Anatrazole:
Add 15g of crude Anatrazole to a mixed solution of 30ml isopropanol and 30ml of water, stir and heat to 40-45 ℃ for dissolution, add 0.075g of activated carbon, decarbonize for 15 minutes, filter, add 120ml of water dropwise to the filtrate, stir and crystallize, cool to 0 ℃, stir and incubate for 2 hours, filter, and wash with cold water to obtain 14.3g of Anatrazole, with a weight yield of 95.3%.
Method 2
1) Add 5-bromomethyl sequentially to the glass reactor- α,α,α′,α′- 30g of tetramethyl-1,3-phenylenediamine, 30g of 4-amino-1,2,4-triazole, and 80ml of acetonitrile were stirred and heated to reflux. After 12 hours of reaction, they were cooled and crystallized at 0 ℃ for 8 hours. Filter and dry to obtain intermediate I35.58g with a yield of 93.0%;
2) Add 30g of intermediate I30g, 225ml of anhydrous methanol, 2ml of purified water, and 2g of copper sulfate to the glass reactor in sequence. Stir and add 24.0g of concentrated sulfuric acid dropwise. After stirring, heat until reflux is achieved. Slowly add 12.0g of sodium azide, complete the addition, and continue the reflux reaction for 1 hour. Filter the reaction solution while it is hot, discard the filter residue, reduce the pressure and concentrate the filtrate to 0.5 times the original volume, cool and crystallize, filter the solid, and then adjust the pH of the solution with saturated potassium carbonate solution to a pH value of 8.0-9.0. Extract twice with dichloromethane, 75ml each time, merge the organic layers, and wash the organic layers twice with purified water, 75ml each time. Dry anhydrous sodium sulfate, concentrate the filtrate under reduced pressure until no dichloromethane drips out, and cool and solidify the residue. Dry, obtain 18.04g of crude Anatrazole (single impurity less than 0.1%, total impurity less than 0.3%), with a yield of 79.8%.
3) 150ml of isopropanol and 15g of crude anastrozole were added to a glass reactor, heated and refluxed. After the solid was completely dissolved, 0.75g of medicinal charcoal was added for refluxing and decolorization for 1 hour. The medicinal charcoal was removed by filtration. The filtrate was placed at 0 ℃ and crystallized for more than 48 hours. After filtration, it was dried under reduced pressure at 60 ℃ to obtain 12.3g of refined anastrozole with a yield of 82.0%. The isomer was not detected, with a purity of 99.84%.
Anastrozole, a nonsteroidal aromatase inhibitor, has shown significant efficacy in the adjuvant treatment of breast cancer. The following is a detailed analysis of anastrozole as an adjuvant treatment standard for breast cancer:
Anastrozole reduces the conversion of androgen to estrogen by inhibiting the activity of aromatase, thus reducing the estrogen level. In breast cancer cells, estrogen is one of the main growth factors, so lowering estrogen level can inhibit the growth and proliferation of breast cancer cells.
Applicable population:
Estrogen receptor-positive breast cancer patients:
Since anastrozole can reduce estrogen level, it is especially suitable for estrogen receptor-positive breast cancer patients.
Postmenopausal women:
Anastrozole is mainly used for breast cancer treatment in postmenopausal women because the ovarian function of postmenopausal women has declined and estrogen is mainly converted from androgens secreted by adrenal glands under the action of aromatase.
Efficacy and Safety:
Significant efficacy:
Studies have shown that anastrozole in adjuvant treatment of breast cancer can significantly reduce the recurrence rate and mortality rate, and improve the survival rate of patients.
Good safety:
Anastrozole has relatively few side effects, mainly including headache, nausea, fatigue, etc., and most patients can tolerate them.
Dosage and regimen:
Safe dosage standard:
The safe dosage standard of anastrozole is usually 1mg/day.
Recommended course of treatment:
For patients with early-stage breast cancer, the recommended course of treatment is 5 years.
However, the specific course of treatment should be determined according to the specific conditions of the patient and the recommendations of the doctor.
Combined application with Fulvestrant:
Studies have shown that anastrozole in combination with fulvestrant (a selective estrogen receptor degrader) can significantly improve the survival rate of postmenopausal women with estrogen receptor-positive HER2-negative advanced breast cancer. However, the advantages of this combination in patients with early-stage breast cancer are unclear.
Combinations with other chemotherapeutic agents:
In some cases, anastrozole can be used in combination with other chemotherapy agents to improve treatment outcomes. However, this combination application needs to be carried out under the supervision of a physician to ensure safety and effectiveness.
Rationale for Anastrozole as a standard of adjuvant treatment for breast cancer
Clinical trial results: Several clinical trials have shown that anastrozole can significantly reduce the recurrence rate and mortality rate in the adjuvant treatment of breast cancer, and the safety is good.
Guideline recommendation:
Anastrozole has been listed as one of the standard drugs for adjuvant treatment of breast cancer in several authoritative guidelines (e.g. NCCN guidelines) at home and abroad.
With the in-depth research on the pathogenesis and treatment of breast cancer, the application of anastrozole in the adjuvant treatment of breast cancer will have a broader prospect. In the future, Anastrozole can be expected to make greater breakthroughs in the following aspects:
through genetic testing and biomarker analysis, provide patients with more precise individualized treatment plans.
Combination application with other drugs or treatments (e.g. immunotherapy, targeted therapy, etc.) in order to improve the therapeutic efficacy and survival rate of patients.
based on the mechanism of action of anastrozole, to develop a new generation of aromatase inhibitors with more efficient and safer.
In summary, anastrozole has become one of the important drugs in the adjuvant treatment of breast cancer, and it has significant advantages in reducing the recurrence rate and mortality rate, and improving the survival rate of patients. In the future, with the deepening of research and the continuous progress of technology, the application prospect of anastrozole in breast cancer treatment will be even broader.
faq
What does anastrozole do to your body?
Anastrozole is an aromatase inhibitor that works by blocking the enzyme aromatase, significantly lowering estrogen levels in postmenopausal women to slow or stop the growth of hormone-receptor-positive breast cancer, but its estrogen reduction can lead to side effects like hot flashes, joint pain, bone thinning (osteoporosis), mood changes, and vaginal dryness, affecting energy and physical well-being.
What is the dark side of anastrozole?
Anastrozole can make your bones weaker and there is an increased risk of osteoporosis or bone injuries. Ask your doctor for advice if you get this side effect. Your doctor may suggest using a steroid cream or taking an antihistamine. You can buy these at a pharmacy without a prescription.
What to avoid when taking anastrozole?
When taking anastrozole, you should avoid estrogen-containing products (like HRT), other hormone therapies, certain supplements (e.g., soy, flaxseed), and alcohol, as they can reduce the drug's effectiveness, while also steering clear of fatty, spicy, and sugary foods that worsen side effects like nausea and joint pain, and always discuss new medications or therapies with your doctor.
Is anastrozole a form of chemotherapy?
No, anastrozole (Arimidex) is not a traditional chemotherapy drug; it's a hormone therapy (specifically an aromatase inhibitor) that works by lowering estrogen levels to stop hormone-sensitive breast cancer from growing, rather than killing rapidly dividing cells like chemo. It's a systemic treatment, often used after surgery, to prevent recurrence in postmenopausal women with hormone-receptor-positive cancer, and can also be used for prevention or in men with breast cancer.
What does anastrozole do to your brain?
We found that women with breast cancer who received anastrozole therapy experienced poorer verbal and visual learning and memory than women with breast cancer who received tamoxifen. These findings may be related to the changes in estrogen levels experienced by women receiving this therapy.
Will anastrozole make you gain weight?
Yes, anastrozole (Arimidex) can cause weight gain, often as a reported side effect, though studies show many women have stable weight, with some gaining, but significant gain (over 11 lbs) is less common; weight changes are often seen in the first year, influenced by menopause and lifestyle, and may involve increased body fat despite stable weight.
Hot Tags: anastrozole powder cas 120511-73-1, suppliers, manufacturers, factory, wholesale, buy, price, bulk, for sale, 4 4 Diaminodiphenylsulfone CAS 80 08 0, pure benzocaine powder, 1 5 Dimethylhexylamine, Meprednisone Hemisuccinate CAS 27303 92 0, 99 9 pure lidocaine powder, pure procaine powder