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Ruxolitinib

CAS NO.941678-49-5

  • Min.Order: 1 Gram
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Product Details

Keywords

  • (R)-3-(4-(7H-Pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile
  • 941678-49-5 supplier
  • 941678-49-5 price

Quick Details

  • ProName: Ruxolitinib
  • CasNo: 941678-49-5
  • Molecular Formula: C17H18N6
  • Appearance: solid or liquid
  • Application: Intermediate
  • DeliveryTime: Within 7 working days
  • PackAge: 1g,5g,10g...1kg,5kg...more
  • Port: Shanghai Port
  • ProductionCapacity: 10 Kilogram/Month
  • Purity: 98% Min
  • Storage: Protected from light, stored hermetica...
  • Transportation: By air or sea
  • LimitNum: 1 Gram
  • Molecular Weight: 306.371

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Details

Ruxolitinib Basic information
Pharmacological effects Biological Activity Indications Dosage Adverse reactions Other clinical research
Product Name: Ruxolitinib
Synonyms: Ruxolitinib;(R)-3-(4-(7H-Pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile;(betaR)-beta-Cyclopentyl-4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazole-1-propanenitrile;1H-Pyrazole-1-propanenitrile,.beta.-cyclopentyl-4-(7H-pyrrolo[2,3-d]pyriMidin-4-yl)-,(.beta.R)-;(3R)-3-(4-(7H-pyrrolo[2,3-d]pyriMidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile;(3R)-3-cyclopentyl-3-(4-{7H-pyrrolo[2,3-d]pyriMidin-4-yl}-1H-pyrazol-1-yl)propanenitrile;INCB018424 (Ruxolitinib);Jakafi
CAS: 941678-49-5
MF: C17H18N6
MW: 306.371
EINECS: -0
Product Categories: APIs;Aromatics;Chiral Reagents;Heterocycles;Intermediates & Fine Chemicals;Pharmaceuticals;Tyrosine Kinase Inhibitors;Inhibitor;Antineoplastic;Anti-cancer&immunity;Inhibitors
Mol File: 941678-49-5.mol
Ruxolitinib Structure
 
Ruxolitinib Chemical Properties
density  1.40
 
Safety Information
MSDS Information
 
 
Ruxolitinib Usage And Synthesis
Pharmacological effects Myelofibrosis (MF) is a rarely-occurring disease of myelodysplastic disorders. It is caused by the replacement of in vivo bone marrow by scar tissue, leading to the production of blood cells in the liver and spleen and other organs, which is characterized by splenomegaly, anemia, leukopenia, and thrombocytopenia, and different degrees of bone sclerosis. Symptoms include fatigue, abdominal discomfort, pain under the ribs, muscle and bone pain, itching and night sweats. 
Ruxolitinib is the first oral medication approved by the US Food and Drug Administration (FDA) for the treatment of myelofibrosis. It is a small-molecule inhibitor of the tyrosine kinase (namely, JAK1 and JAK2) and is suitable for the treatment of intermediate or high-risk myelofibrosis, including primary myelofibrosis, post-polycythemia Vera myelofibrosis and post essential thrombocythemia myelofibrosis.
August 29, 2012, the EU has approved the first drug for the treatment of myelofibrosis, ruxolitinib. Ruxolitinib can be used for the treatment of intermediate or high-risk myelofibrosis, including primary myelofibrosis, post-polycythemia Vera myelofibrosis and post essential thrombocythemia myelofibrosis. Currently, ruxolitinib has been approved by more than 50 countries around the world, including the EU, Canada and some Asian, Latin American and South American countries.
US Novartis has obtained authorization from Incyte Company of the development and commercialization right of Ruxolitinib outside the United States. The European Commission and the FDA have both granted the status of Ruxolitinib as the orphan drug in the treatment of myelofibrosis. Currently, Incyte has sold it under the trade name Jakafi in the United States for the treatment of intermediate or high-risk myelofibrosis.

Figure 1 is the ruxolitinib tablet produced by the US Novartis Company (trade name: Jakafi)
Biological Activity Ruxolitinib, INCB18424 is a potent and selective JAK1 and JAK2 inhibitor (IC50 were 2.7 and 4.5nM, respectively). It has potent anti-tumor and immunomodulatory activity. Ruxolitinib can inhibit IL-6 signal (IC50 = 281nM) and the proliferation of JAK2V617F + Ba / F3 cell. Ruxolitinib can also inhibit the STA3 phosphorylation of wild-type JAK2 and JAK2 V617F mutant inside the body of patients. Clinical application of it can significantly cause reduction in the circulating levels of inflammatory cytokines. Ruxolitinib also has an effective role in model of the adjuvant arthritis and the multiple-cause murine arthritis.
This information is edited by Xiongfeng Dai from Chemicalbook.
Indications Ruxolitinib is a kind of kinase inhibitor which is suitable for the treatment of intermediate or high-risk myelofibrosis, including primary myelofibrosis, post-polycythemia Vera myelofibrosis and post essential thrombocythemia myelofibrosis.
Dosage 1. For patients with platelet counts being greater than 200 / μl, ruxolitinib should be applied at a start dose of 20 mg with being administered orally twice per day while for patients with platelet counts between 100 / μl and 200 / μl, they should apply a dose of 15mg twice a day. 
2. Before starting to apply ruxolitinib treatment, you should perform complete blood count. Monitor the complete blood count in every 2-4 weeks and lower the adjusted dose for platelet count.
3. According to the result of the reaction, the patients can increase the dose to the maximum recommended dose of 25 mg twice per day. The patient should discontinue if the spleen gets no reduction or the symptoms are not improved, the patients should discontinue after 6 months.
Adverse reactions The most common hematological adverse reactions (incidence> 20%) is lower platelet counts and anemia. The most common non-hematologic adverse reactions (incidence> 10%) are bruising, dizziness and headache.
Other clinical research Columbia University Medical Center has conducted a test of a drug designed to treat bone marrow diseases to investigate whether it can help people get rid of alopecia areata. The study found that, for human participating in human body test, including seven women and five men, after they have administrated a drug called Ruxolitinib, the symptoms of most people has been greatly alleviated. Part of their research has been published in the "Nature Medicine" magazine.
Usage A JAK family kinase inhibitor of JAK1, JAK2 and JAK3 with IC50s of 2.7 nM, 4.5 nM and 322 nM, respectively
Usage Ruxolitinib is a selective Janus tyrosine kinase (JAK1 and JAK2) inhibitor used in the treatment of myeloproliferative neoplasms and psoriasis.
Usage INCB018424 is the first potent, selective, JAK1/2 inhibitor to enter the clinic with IC50 of 3.3 nM/2.8 nM, >130-fold selectivity for JAK1/2 versus JAK3. Phase 3

Company Information

Henan Sunlake Enterprise Corporation is located in Henan Province , The central plain of China , Which enjoys favorable geogeaphical position and convenient transportion. The com[any was established in june. 1998, until now having more than 18 years experience in manufacturing & exporting chemical raw material . 

Sunlake is a professional manufacturer engaged in producing and selling chemicals,including Organic & inorganic chemicals , pigments & Dyestuffs , Water treatment chemicals , Food & FEED additives and others. These products have been being well exported to europe, southeast Asia, the Middle East ,Africa, South America and some other countries and areas. 

We sincerely welcome foreign friends to visit our plant for cooperation. With the idea of "quality first,credit priority, Excellent service", We are highly acknowledged by customers for good quality and competitive price. More importantly , the company has a strong R & D team, who are professional engineers and scholars with Ph. D. .So we are confident to serve you better with our high - quality products and professional team. We are taking great efforts to provide our customers with demanded goods and professional services, and continuously improve our core ability of competition and get the momentum for sustainable development, and finally make us being a reliable and professional supplier in international market. 

We welcome any serious inquiries from all customers of the world, and sincerely hope to cooperate with you for a brilliant future!

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

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