We supply Enzalutamide( MDV3100)

We're proud to offer Enzalutamide MDV3100 to our guests. It's a drug used in the treatment of prostate cancer. It works by blocking the goods of androgens, which are hormones that can promote the growth of cancer cells.
It's an effective treatment option for cases with advanced prostate cancer who have formerly experienced hormone remedy. It can extend the time before the cancer progresses and can indeed shrink excrescences in some cases.
Our platoon of experts is available to answer any questions you may have about Enzalutamide or any of our other specifics. communicate us moment to learn further about our products and services.

What's MDV3100?

MDV3100 has the chemical formula 4-( 3-( 4- cyano- 3-( trifluoromethyl) phenyl) -5,5-dimethyl-4-oxo-2-thio-1-imidazolyl)-2-fluoro-N-methylbenzamide. Its clinical medicine was developed in collaboration with Agreement and Astellas, and was approved by the US Food and Drug Administration( FDA) on August 31, 2012 for the treatment of advanced manly castration resistant prostate cancer that has spread or regressed. The medicine is retailed as Xtandi( 1) and is an oral medication. Enzalutamide MDV3100 is an androgen receptor antagonist that blocks androgen list to androgen receptors and prevents nuclear translocation of ligand receptor complexes and reclamation of co activators. It has also been shown to induce excrescence cell apoptosis and has no agonist exertion. It's a seeker for the treatment of castration resistant prostate cancer.
 

Basic Information

Product Name: Enzalutamide (MDV3100)

CAS NO: 915087-33-1

MF: C21H16F4N4O2S

MW: 464.44

EINECS NO: 805-022-1

MDL No.:MFCD14155804

Purity: 99%+

MOQ: 1kg

Origin: China

Application: Antineoplastic；Anti-Cancer

Delivery Time: stock

Structural formula:

Melting point: 198-200 ° C

Density: 1.49

Solubility: soluble in DMSO (>25mg/ml)

Stability: Can be stably stored for 1 year when supplied. DMSO solution can be stored at -20 ° C for up to 3 months.

Technical Specification:

Package: 10g/bag; 100g/ bag or according to your demands

Storage conditions: Stored in an airtight container and protected from light

Synthetic route

The synthesis route of enzalutamide is based on N-methyl-2-fluoro-4-bromobenzamide as the starting material, which is substituted, esterified, and then reacted with 3-trifluoromethyl-4-cyanophenyl isothiocyanate to obtain the target compound. The synthesis route is as follows

Pharmacological action

Enzalutamide MDV3100 is an oral androgen receptor antagonist that has been clinically studied and approved by the US Food and Drug Administration (FDA) for the treatment of metastatic castration tolerant prostate cancer that progresses after chemotherapy (i.e., patients with prostate cancer who still have tumors or cancer cells growing after chemotherapy), and can prolong patient survival. The incidence rate of prostate cancer in the United States is very high, with an annual increase of nearly 240000 patients (the highest of all cancers), and an annual death of nearly 30000 people (second only to lung cancer, breast cancer, and colorectal cancer). The incidence rate of prostate cancer in China is low. It is a type of androgen receptor inhibitor with a different target from cabataxel approved in 2010 and abiraterone approved in 2011. It can competitively inhibit the binding of androgens to receptors, as well as inhibit the nuclear transport of the androgen receptor and its interaction with DNA. In vitro experimental studies have shown that it can inhibit the proliferation of prostate cancer cells and induce their death. In mouse prostate cancer xenograft model experiments, it can reduce tumor volume. The main metabolite of Enzalutamide is N-demethyl Enzalutamide, which exhibits similar inhibitory activity in vitro to it. The recommended adult dose for this drug is daily. 160mg should be rapidly absorbed after administration, and the plasma concentration should reach its highest level within 0.5-3 hours. The average end half-life is 5.8 days, and the main metabolic enzymes are CYP2C8 and CYP3A4. This drug should be avoided in combination with strong CYP2C8 inhibitors (such as gemfibrozil). If co administration is required, the dosage should be reduced to 80mg, once a day.

What is the application of Enzalutamide

Enzalutamide can currently be applied to almost all stages of prostate cancer, such as pre - and late stage patients, significantly delaying the start of chemotherapy in patients. In addition, for post-chemotherapy CRPC and mCRPC, it can significantly improve the overall survival time and progression free survival time of patients.

Reference materials

1. TRAN C, OUT S, CLEGG N, et al. Development of a second generation antagonist for treatment of advanced status cancer [J] Science, 2009,3 24 (5928): 787-790

2. Encyclopedia of Enzalutamide and Mobe Compounds [Cited 2017-04-7]

3. SAWYERS C, JUNG M, CHEN C, et al. Diarylhydantoin compounds: WO, 2006124118 [P]. 2006-11-23

4. JUNG M, YOO D, SAWYERS C, et al. Diarylthiohydantoin compounds: US, 20070254933 [P]. 2007-11-01

5. THOMPSON A, LAMBERSON C, GREENFIELD S, et al. Processes for the synthesis of diabetes and diabetes compounds: WO, 2011106570 [P]. 2011-01-09

6. MICHAEL E, SAMEDY O, DONGWON Y, et al. Structure activity relationship for thyroid androgen receptor antagonists for casting resistant status cancer (CRPC) [J]. J Med Chem, 2010, 53 (7): 2779-2796

7. Lin Nengming, editor in chief of Ma Shenglin; Yang Bo, He Qiaojun, Yang Guonong and other deputy editors in chief; Ding Haiying, Ma Yueguang, Wang Gang et al., newly edited anti-tumor pharmacology, Military Medical Science Press, May 2014, p. 284

Contact information:

In summary, as a supplier of MDV3100 , Xi'an Yihui has rich production experience and technical knowledge, high-quality products, flexible production capacity, and quality customer service, which can provide better support and service to customers.

if you need it, pls feel free to contact us any time. we will reply you asap.

Our contact information:

E-mail: sales@yihuipharm.com
Tel: 0086-29-89695240
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