Anastrozole Anti Estrogen Steroids for Treatment of Breast Cancer CAS 120511-73-1

Basic Information
Place of Origin: China
Brand Name: ChineseHormone
Certification: GMP, ISO 9001, USP
Model Number: CAS 120511-73-1
Minimum Order Quantity: Free samples Available
Price: negotiated
Packaging Details: as your required
Delivery Time: 3-7 working days
Payment Terms: Western Union, MoneyGram, T/T, Bitcoin
Supply Ability: 500-1000 kg / month
MW: 293.3663 MF: C17H19N5
Melting Point: 130.14 °C Half Life: 50 Hours
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Anastrozole Anti Estrogen Steroids for Treatment of Breast Cancer CAS 120511-73-1

 

CAS number120511-73-1

WeightAverage: 293.3663
Monoisotopic: 293.164045633

Chemical Formula:C17H19N5

chemical structure:

Anastrozole Anti Estrogen Steroids for Treatment of Breast Cancer CAS 120511-73-1 0

Half life :50 hours

melting point130.14 °C

water solubility0.5 mg/mL

 

Description

 

Anastrozole is a drug indicated in the treatment of breast cancer in post-menopausal women. It is used both in adjuvant therapy (i.e. following surgery) and in metastatic breast cancer. It decreases the amount of estrogens that the body makes. Anastrozole belongs in the class of drugs known as aromatase inhibitors. It inhibits the enzyme aromatase, which is responsible for converting androgens (produced by women in the adrenal glands) to estrogens.

 

Pharmacodynamics

 

Anastrozole is a potent and selective non-steroidal aromatase inhibitor indicated for the treatment of advanced breast cancer in post-menopausal women with disease progression following tamoxifen therapy. Many breast cancers have estrogen receptors and growth of these tumors can be stimulated by estrogens. In post-menopausal women, the principal source of circulating estrogen (primarily estradiol) is conversion of adrenally-generated androstenedione to estrone by aromatase in peripheral tissues, such as adipose tissue, with further conversion of estrone to estradiol.

 

Many breast cancers also contain aromatase; the importance of tumor-generated estrogens is uncertain. Treatment of breast cancer has included efforts to decrease estrogen levels by ovariectomy premenopausally and by use of anti-estrogens and progestational agents both pre- and post-menopausally, and these interventions lead to decreased tumor mass or delayed progression of tumor growth in some women. Anastrozole is a potent and selective non-steroidal aromatase inhibitor. It significantly lowers serum estradiol concentrations and has no detectable effect on formation of adrenal corticosteroids or aldosterone.

 

Mechanism of action

 

Anastrozole selectively inhibits aromatase. The principal source of circulating estrogen (primarily estradiol) is conversion of adrenally-generated androstenedione to estrone by aromatase in peripheral tissues. Therefore, aromatase inhibition leads to a decrease in serum and tumor concentration of estrogen, leading to a decreased tumor mass or delayed progression of tumor growth in some women. Anastrozole has no detectable effect on synthesis of adrenal corticosteroids, aldosterone, and thyroid hormone.

 

Research

 

Usage in men

 

Anastrozole has been tested for reducing estrogens, including estradiol, in men. Excess estradiol in men can cause benign prostatic hyperplasia, gynecomastia, and symptoms of hypogonadism. It can also contribute to increased risk of stroke, heart attack, chronic inflammation, prostate enlargement and prostate cancer. Some athletes and body builders use anastrozole as part of their steroid cycle to reduce and prevent symptoms of excess estrogen--gynecomastia, emotional lability and water retention.Study data suggest dosages of 0.5 mg to 1 mg a day reduce serum estradiol by approximately 50% in men, which differs in postmenopausal women.

 

Usage in children

 

Anastrozole may be used off-label in children with precocious puberty, or children with pubertal gynecomastia. Following the onset of puberty, the epiphyseal plate begins to close due to an increased amount of estrogen production escaping local metabolism and spreading to the circulatory system.It is shown to help slow this process, and increase adult height prediction in adolescent males treated with protein-based peptide hormones for the treatment of growth hormone deficiency.

 

Predicted Properties

 

Property

Value

Source

Water Solubility

0.0661 mg/mL

ALOGPS

logP

2.31

ALOGPS

logP

3.03

ChemAxon

logS

-3.6

ALOGPS

pKa (Strongest Basic)

2.25

ChemAxon

Physiological Charge

0

ChemAxon

Hydrogen Acceptor Count

4

ChemAxon

Hydrogen Donor Count

0

ChemAxon

Polar Surface Area

78.29 Å2

ChemAxon

Rotatable Bond Count

4

ChemAxon

Refractivity

97.47 m3·mol-1

ChemAxon

Polarizability

31.97 Å3

ChemAxon

Number of Rings

2

ChemAxon

Bioavailability

1

ChemAxon

Rule of Five

Yes

ChemAxon

Ghose Filter

Yes

ChemAxon

Veber's Rule

Yes

ChemAxon

MDDR-like Rule

Yes

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