Exemestane (Aromasin)

Exemestane is an oral steroidal aromatase inhibitor used in the adjuvant treatment of hormonally-responsive (also called hormone-receptor-positive, estrogen-responsive) breast cancer in postmenopausal women. It acts as a false substrate for the aromatase enzyme, and is processed to an intermediate that binds irreversibly to the active site of the enzyme causing its inactivation.

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General Details

Natural Aromatase Inhibitors Bulking Cycle Steroid Exemestane Aromasin CAS 107868-30-4 

 

Description:

 

Exemestane is an oral steroidal aromatase inhibitor used in the adjuvant treatment of hormonally-responsive

(also called hormone-receptor-positive, estrogen-responsive) breast cancer in postmenopausal women.

It acts as a false substrate for the aromatase enzyme, and is processed to an intermediate that binds irreversibly

to the active site of the enzyme causing its inactivation.

 

Details:

 

English name: Exemestane

English alias: Exemestan; 6-Methylenandrosta-1,4-diene-3,17-dione; Exemestane;Exemestano;

Exemestanum;10,13-Dimethyl-6-methylidene-7,8,9,10,11,12,13,14,15,16 -decahydrocyclopenta

[a] phenanthrene-; 6-methylideneandrosta-1,4-diene-3,17-dione; (8ξ, 9ξ, 14ξ) -6-methylideneandrosta-

1,4-diene-3,17-dione; Exemestane ( Aromasin); Exemestone

CAS: 107868-30-4

Molecular formula: C20H24O2

MW: 296.4034

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

Molecular Structure:

Exemestane

Density: 1.13g / cm3

Melting point: 155.13 ℃

Boiling point: 453.7 ° C at 760 mmHg

Flash Point: 169 ° C

Vapor Pressure: 2.02E-08mmHg at 25 ° C

Manufacturer:HKYCGC

Assay: 99% min.

Character: White crystalline powder.

Usage:Developed to help fight breast cancer, Aromasin is one of the most powerful estrogen suppressing

compounds available for body builders taking anabolic steroids. Additionally, it also raises testosterone

in the body, which is a bonus for bodybuilders during post-cycle-therapy.

Aromasin (Exemestane) is one of those weird compounds that nobody really knows what to do with. It’s

a third generation Aromatase Inhibitor (AI) just like Arimidex (Anastrozole) and Femera (Letrozole).

 

 

 

Place of Origin: China
Brand Name: HKYCGC
Certification: KOSHER/ISO9001/SGS
Model Number: 107868-30-4

Payment & Shipping Terms:

Minimum Order Quantity: 10g
Price: Negotiation
Packaging Details: As your requirements
Delivery Time: After receipt of your payment
Payment Terms: Western Union,Bitcoin or T/T
Supply Ability: 1000 kg per month

 

 

 

COA:

 

TEST ITEMS SPECIFICATION RESULTS
Description : White Crystalline Powder White Powder
Identification : Positive Positive
Assay(by HPLC) : 98.0~102.0% 98.64%
Absorbance(E1cm) : 465~495 482.5
Melting Point : 191~195°C 193.5~195.0°C
Loss On Drying : 0.5%max 0.19%
Specific Rotation : +288°~ +298° +290.2°
Residue On Ignition : 0.1%max 0.03%
Related Substances : Total:1.5%max <1.3%
Single:0.5%max <0.4%
Residue Solvents : 0.2%max 0.10%
Heavy Metals : 20PPm max <10PPm
Conclusion The specification conform with enterprise standard.

 

 

Applications:

 

High Purity Exemestane/Aromasin/Exemestan/CAS No: 107868-30-4

the third generation aromatase inhibitors, used in the treatment of metastatic breast cancer and used

as aid in the treatment of early breast cancer.

Many breast cancers are stimulated to grow by the female sex hormones oestrogen and progesterone.

These breast cancers are called hormone sensitive or hormone receptor positive and can be treated with

drugs that block the effects of these hormones.

In women who have had their menopause, oestrogen is mainly produced by changing androgens (sex

hormones produced by the adrenal glands) into oestrogens. This process is called aromatisation and

happens mainly in the fatty tissues, muscle and the skin. It needs a particular enzyme called aromatase.

Exemestane blocks the process of aromatisation. So it lowers the amount of oestrogen in the body. In early

breast cancer, taking exemestane can help to stop breast cancer coming back. In advanced breast cancer

the cancer cells may grow more slowly or stop growing completely.

Hormones are chemical substances that are produced by glands in the body, which enter the bloodstream

and cause effects in other tissues. For example, the hormone testosterone made in the testicles and is responsible

for male characteristics such as deepening voice and increased body hair. The use of hormone therapy to treat

cancer is based on the observation that receptors for specific hormones that are needed for cell growth are

on the surface of some tumor cells. Hormone therapies work by stopping the production of a certain hormone,

blocking hormone receptors, or substituting chemically similar agents for the active hormone, which cannot be

used by the tumor cell. The different types of hormone therapies are categorized by their function and/or the

type of hormone that is affected.

Exemestane is an aromatase inhibitor. This means it blocks the enzyme aromatase (found in the body’s muscle,

skin, breast and fat), which is used to convert androgens (hormones produced by the adrenal glands) into estrogen.

In the absence of estrogen, tumors dependent on this hormone for growth will shrink.

Note: We strongly encourage you to talk with your health care professional about your specific medical condition

and treatments. The information contained in this website is meant to be helpful and educational, but is not a

substitute for medical advice.

 

 

Pharmacology

 

Indication:

 

For the treatment of advanced breast cancer in postmenopausal women whose disease has progressed following

tamoxifen therapy.

 

Pharmacodynamics:

 

Aromatase is an enzyme that converts hormones to estrogen in the body’s adrenal glands. The aromatase

inhibitors (AIs) are drugs that reduce estrogen levels by blocking the action of aromatase in the adrenal glands.

The selective AIs (SAIs) selectively reduce levels of estrogen without interfering with levels of other steroid

hormones that are produced by the adrenal gland. Drugs in this class include anastrozole (Arimidex ™),

letrozole (Femara ™) and exemestane (Aromasin ™).

 

Mechanism of action:

 

Breast cancer cell growth may be estrogen-dependent. Aromatase (exemestane) is the principal enzyme

that converts androgens to estrogens both in pre- and postmenopausal women. While the main source of

estrogen (primarily estradiol) is the ovary in premenopausal women, the principal source of circulating

estrogens in postmenopausal women is from conversion of adrenal and ovarian androgens (androstenedione

and testosterone) to estrogens (estrone and estradiol) by the aromatase enzyme in peripheral tissues.

Estrogen deprivation through aromatase inhibition is an effective and selective treatment for some

postmenopausal patients with hormone-dependent breast cancer. Exemestane is an irreversible, steroidal

aromatase inactivator, structurally related to the natural substrate androstenedione. It acts as a false substrate

for the aromatase enzyme, and is processed to an intermediate that binds irreversibly to the active site

of the enzyme causing its inactivation, an effect also known as “suicide inhibition”. Exemestane significantly

lowers circulating estrogen concentrations in postmenopausal women, but has no detectable effect on the

adrenal biosynthesis of corticosteroids or aldosterone. This reduction in serum and tumor concentrations of

estrogen delays tumor growth and disease progression. Exemestane has no effect on other enzymes involved

in the steroidogenic pathway up to a concentration at least 600 times higher than that inhibiting the aromatase

enzyme.

 

 

 

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