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Newblue-CHEM - 6-Aminoindazole CAS NO.6967-12-0
- FOB Price: USD: 1,000.00-1,000.00 /Kilogram Get Latest Price
- Min.Order: 1 Gram
- Payment Terms: L/C,D/A,D/P,T/T,Other
- Available Specifications:
1(1-100)Kilogram
- Product Details
Keywords
- 6-Aminoindazole
- 6967-12-0?
- C21H16F4N4O2S
Quick Details
- ProName: Newblue-CHEM - 6-Aminoindazole
- CasNo: 6967-12-0
- Molecular Formula: C21H16F4N4O2S
- Appearance: Solid
- Application: Organic synthesis
- DeliveryTime: PROMPT
- PackAge: IN 25kg drums
- Port: SHANGHAI
- ProductionCapacity: 10 Metric Ton/Month
- Purity: 99.0%
- Storage: In Room Temperature
- Transportation: As per MSDS
- LimitNum: 1 Gram
- Heavy metal: N/A
- Grade: Industrial Grade,Food Grade,Pharma Gra...
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Henan Newblue Chemical Co., Ltd. is located in Zhengzhou High-tech Development Zone with import and export license.
We passed ISO 9001:2008 in 2009, and won "High-tech Enterprise" by provincial government in 2013.The objective of the company is to put quality first and put our customer’s needs first - the satisfaction of our customers is the company's ultimate goal.
Improving product quality and service level is our responsibility, and creating more value for our customer’s is our purpose. We are constantly striving to make Henan Newblue a leading chemical supplier, and hope to create a better future with you.
Details
Enzalutamide (MDV3100) Basic information
Pharmacological action Indications Clinical evaluation Side effects Biological activity In vivo studies
Product Name: Enzalutamide (MDV3100)
Synonyms: MDV-3100;4-[3-[4-Cyano-3-(trifluoromethyl)phenyl]-5,5-dimethyl-4-oxo-2-thioxo-1-imidazolidinyl]-2-fluoro-N-methylbenzamide;4-(3-(4-Cyano-3-(trifluoromethyl)phenyl)-5,5-dimethyl-4-oxo-2-thioxoimidazolidin-1-yl)-2-fluoro-N-methylbenzamide;4-{3-[4-cyano-3-(trifluoroMethyl)phenyl]-5,5-diMethyl-4-oxo-2-sulfanylideneiMidazolidin-1-yl}-2-fluoro-N-MethylbenzaMide;EnzalutaMide;MDV3100 (EnzalutaMide);MDV 3100,4-[3-[4-Cyano-3-(trifluoroMethyl)phenyl]-5,5-diMethyl-4-oxo-2-thioxo-1-iMidazolidinyl]-2-fluoro-N-MethylbenzaMide;4-(3-(4-Cyano-3-(trifluoromethyl)phenyl)-5,5-dimethyl-4-oxo-2-thioxoimidazolidin-1-yl)-2-fluoro-N
CAS: 915087-33-1
MF: C21H16F4N4O2S
MW: 464.4359528
EINECS: -0
Product Categories: Apoptosis;Aromatics;Heterocycles;Inhibitors;Intermediates & Fine Chemicals;Pharmaceuticals;Sulfur & Selenium Compounds;Inhibitor
Mol File: 915087-33-1.mol
Enzalutamide (MDV3100) Structure
Enzalutamide (MDV3100) Chemical Properties
density 1.49
Safety Information
MSDS Information
Enzalutamide (MDV3100) Usage And Synthesis
Pharmacological action Enzalutamide (XTANDI) is an oral androgen receptor antagonist, which is approved by the current clinical research and the US FDA (Food and Drug Administration), for the development of post-chemotherapy metastatic castration tolerance of prostate cancer Treatment (i.e. patients with prostate cancer after chemotherapy, cancer or cancer cells are still growing in such patients), can extend the survival of patients. The incidence of prostate cancer in the United States is very high, with an annual increase of nearly 240,000 patients (the highest among all cancers), nearly 30,000 deaths every year (second only to lung cancer, breast cancer, colorectal cancer),but its incidence is low in China.
Enzalutamide is an androgen receptor inhibitor, the target of action is different from the approved cabbitaxel in 2010 and the approved abbitolone in 2011, and can competitively inhibit androgen and receptor binding, and can inhibition of androgen receptor nuclear transport and the interaction of the receptor and DNA. Vitro studies have shown that enzalutamide can inhibit prostate cancer cell proliferation and induce death, and enzalutamide reduces tumor volume in mouse prostate cancer xenograft model experiment. The main metabolite of enzalutamide is N-demethylol enamine, which shows similar inhibitory activity with enzalutamide in vitro. The recommended adult dose for the drug is daily 160mg, rapidly absorbed after medication, plasma concentrations to reach the highest level in 0.5~3h, the average terminal half-life is 5.8d, the main metabolic enzymes are CYP2C8 and CYP3A4. The drug should be avoided with strong CYP2C8 inhibitors (such as gemfibrozil), if it is needed for co-administration, should reduce the dose of enzalutamide to 80mg, 1 day.
Indications For the treatment of metastatic or recurrence of advanced male castration tolerance of prostate cancer.
Clinical evaluation Enzalutamide is an oral androgen receptor inhibitor that reduces the risk of radiation-related disease progression and death.
Although anti-androgen therapy has been the preferred treatment option for patients with metastatic prostate cancer for more than 70 years, researchers have found that male hormone receptors play an important role in the development of prostate cancer throughout the course of disease with the in-depth exploration of disease at the molecular level. FDA-approved new generation of androgen receptor antagonists such as abiraterone and enzolatamide have shown that it is benefit for patients with advanced prostate cancer after chemotherapy with docetaxel.
Astellas in Japan and Johnson in the United States treat prostate cancer both through the target, according to statistics, similar to the treatment results, only a few differences, such as: abitron to be used simultaneously with steroid drugs , and enzalutamide is not required; abitron need to limit the diet, and enzalutamide does not need. Drugs in different countries is not the same as different the crowd, so there are price differences, but the effect is the same.
This information was compiled by the Editor of the Chemicalbook (2015-09-20).
Side effects The main side effects of enxtran (XTANDI) are hypertension and fatigue. The most common adverse reactions (≥ 5%) are weakness/fatigue, back pain, diarrhea, joint pain, hot flashes, peripheral blood edema, musculoskeletal pain, headache, upper respiratory tract infection, muscle weakness, dizziness, insomnia, lower respiratory tract infection, spinal cord compression syndrome and cauda equina syndrome, hematuria, paresthesia, anxiety and hypertension.
Biological activity Enzalutamide (MDV3100) is an androgen receptor (AR) antagonist with an IC50 of 36 nM.
Enzalutamide is an androgen receptor (AR) antagonist with an IC50 of 36 nM in vitro studies. In competitive experiments with 16β-[18F] fluoro-5α-DHT (18-FDHT), enzalutamide was found to have higher affinity for bilirubin than Bicalutamide when administered to AR. While enzalutamide had no effect on LNCaP/AR (AR-overexpression) of prostate cells. In parental LNCaP cells, Enzalutamide inhibits the production of prostate specific antigen (PSA) and transmembrane serine protease 2 (TMPRSS2), and inhibits their binding to the synthetic and rogen R1881. Enzalutamide inhibits the translation activity of the mutant AR protein (W741C, Trp at position 741 mutanting to Cys). MDV310 also blocked the nuclear translocation and coordination receptor complexes that recruit coactivators.
In vivo studies Enzalutamide treatment of castrated male mice carrying LNCa/AR xenografts, mice treated with 10 mg MDV310 per kilogram of body weight, can induce significant tumor regression.
Chemical Properties White Solid
Uses MDV 3100 is an androgen-receptor antagonist that blocks androgens from binding to the androgen receptor and prevents nuclear translocation and co-activator recruitment of the ligand-receptor complex. MDV 3100 has also been shown to induce tumor cell apoptosis, and has no agonist activity. MDV 3100 is a candidate for the treatment of castration-resistant prostate cancer.
Uses Enzalutamide (MDV3100) is an androgen-receptor (AR) antagonist with IC50 of 36 nM
Definition ChEBI: A benzamide obtained by formal condensation of the carboxy group of 4-{3-[4-cyano-3-(trifluoromethyl)phenyl]-5,5-dimethyl-4-oxo-2-thioxoimidazolidin-1-yl}-2-fluorobenzoic acid with methylamine. Used for the treatment of of metastatic castration-resistant p ostate cancer.
Enzalutamide (MDV3100) Preparation Products And Raw materials