Axitinib

Axitinib
Axitinib
Axitinib

Axitinib

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Benzamide AG 013736 AVERMECTINB

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  • Appearance: Off-White Solid
  • Application: 319460-85-0 A tyrosine kinase inhibitor; used in cancer therapy.
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Axitinib Basic information
FDA approved axitinib use of treating advanced kidney cancer
Product Name: Axitinib
Synonyms: AXITINIB;Benzamide, N-methyl-2-[[3-[(1E)-2-(2-pyridinyl)ethenyl]-1H-indazol-6-yl]thio]-;N-METHYL-2-{[3-((E)-2-PYRIDIN-2-YLVINYL)-1H-INDAZOL-6-YL]SULFANYL}BENZAMIDE;N-Methyl-2-((3-((1E)-2-(pyridin-2-yl)ethenyl)-1H-indazol-6-yl)sulfanyl)benzamide;AVERMECTINB;Axitinib for research;AG 013736;N-Methyl-2-[[3-[(1E)-2-(2-pyridinyl)ethenyl]-1H-indazol-6-yl]thio]benzamide
CAS: 319460-85-0
MF: C22H18N4OS
MW: 386.47
EINECS:  
Product Categories: All Inhibitors;Inhibitors;Intermediates & Fine Chemicals;Pharmaceuticals;Protein Kinase Inhibitors and Activators;Pfizer compounds;API;AG 013736
Mol File: 319460-85-0.mol
Axitinib Structure
 
Axitinib Chemical Properties
mp  213-215°C
storage temp.  -20°C Freezer
CAS DataBase Reference 319460-85-0(CAS DataBase Reference)
 
Safety Information
Hazard Codes  Xn,N
Risk Statements  22-50/53
Safety Statements  60-61
MSDS Information
 
 
Axitinib Usage And Synthesis
FDA approved axitinib use of treating advanced kidney cancer January 27, 2012, the FDA approved axitinib for the treatment of advanced kidney cancer (renal cell carcinoma) which other drugs unanswer . Inlyta is manufactured and sold by Pfizer,and is a oral pill taken twice a day. 
Renal cell carcinoma is a type of tumor originating from the tubular endothelial cells. Axitinib can prevent certain protein called kinases playing a role in tumor growth and metastasis . 
Axitinib is a small molecule tyrosine kinase inhibitor, effective against multiple targets, including VEGF receptors 1, 2 and 3. 
Dr. Richard Pazdur, hematology and oncology drugs office director of FDA Drug Evaluation and Research Centre, said: "This is the seven kind of drugs allowed treating metastatic or advanced renal cell carcinoma since 2005 . Overall, during this time ,record level of drug development has dramatically changed the treatment of metastatic renal cell carcinoma paradigm, and offers a variety of treatment options for patients. "
In recent years, the drug has been approved for the treatment of kidney cancer include sorafenib (2005), sunitinib (2006), temsirolimus(2007), everolimus (2009), bevacizumab(2009) and pazopanib(2009). 
The above information is edited by the chemicalbook of Tian Ye.
Chemical Properties Off-White Solid
Usage A tyrosine kinase inhibitor; used in cancer therapy.
Usage Axitinib (AG-013736) is a multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ and c-Kit with IC50 of 0.1 nM, 0.2 nM, 0.1-0.3 nM, 1.6 nM and 1.7 nM, respectively.
Usage Axitinib is a multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ and c-Kit with IC50 of 0.1 nM, 0.2 nM, 0.1-0.3 nM, 1.6 nM and 1.7 nM, respectively.
Usage Axitinib is a tyrosine kinase inhibitor. Axitinib is used in cancer therapy.

 

 

 

 

 

 

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Pazopanib Basic information
product description The efficacy of the treatment of advanced renal cell carcinoma Adverse reactions
Product Name: Pazopanib
Synonyms: Pazopanib for research;5-[[4-[(2,3-Dimethyl-2H-indazol-6-yl)(methyl)amino]pyrimidin-2-yl]amino]-2-methylbenzenesulfonamide;Pazopanib;Pazopanib(GW786034);5-(4-((2,3-diMethyl-3,3a-dihydro-2H-indazol-6-yl)(Methyl)aMino)pyriMidin-2-ylaMino)-2-MethylbenzenesulfonaMide;5-[(4-{[(2,3-diMethyl-2H-indazol-6-yl)Methyl]aMino}pyriMidin-2-yl)aMino]-2-Methylbenzene-1-sulfonaMide;5-({4-[(2,3-diMethyl-2H-indazol-6-yl)(Methyl)aMino]pyriMidin-2-yl}aMino)-2-MethylbenzenesulfonaMide 5-(4-(N-(2,3-diMethyl-2H-indazole-6-yl)- N-MethylaMino)pyriMidine-2-ylaMino)-2-MethylbenzenesulfonaMide;Votrient
CAS: 444731-52-6
MF: C21H23N7O2S
MW: 437.52
EINECS:  
Product Categories: Intermediates & Fine Chemicals;Pharmaceuticals;HFC80010;Inhibitors
Mol File: 444731-52-6.mol
Pazopanib Structure
 
Pazopanib Chemical Properties
mp  285-289°C (dec.)
density  1.40
storage temp.  Refrigerator
 
Safety Information
MSDS Information
 
 
Pazopanib Usage And Synthesis
product description Pazopanib is researched and developed by a GlaxoSmithKline ,it is a novel oral vascular generation inhibitor which may interfere stubborn tumor survival and new blood vessels generation growth needed .Targeting vascular endothelial growth factor receptor (VEGFR),it works by inhibiting angiogenesis of tumor blood supply.it is suitable for advanced renal cell carcinoma ( a discovery of cancer cells in the renal tubules), soft tissue sarcoma (STS), epithelial ovarian cancer and non-small cell lung cancer (NSCLC) treatment. 
Minnesota Rochester, Mayo Clinical Research Clinical Research Center researches show that pazopanib (trade name Votrient) can effectively cure thyroid cancer,and can make half of the patients tumor volume reduced, compared to the commonly used drugs ,it is more prolonged stable ,and can be maintained for a considerable period of treatment, the drug has the highest response rate in treatment of thyroid cancer so far.
The US Food and Drug Administration (FDA) approved on October 19, 2009 that pazopanib (trade name Votrient) is listed ,the sixth approved drug treatment of kidney cancer since 2005. In 2009, approximately 49,000 patients were diagnosed with renal cell carcinoma, 11,000 patients died of the disease. 
June 15, 2010, pazopanib, EU conditionally approved it for advanced renal cell cancer and first-line treatment in patients with previously received cytokine therapy. Once the European Commits to give final marketing authorization for this drug, GlaxoSmithKline will have exclusive marketing rights pazopanib for ten years.
The efficacy of the treatment of advanced renal cell carcinoma In order to investigate the efficacy of molecule targeting drug tyrosine kinase inhibitor pazopanib which inhibist the angiogenesis in patients with advanced renal cell carcinoma, People's Liberation Army General Hospital, in June 2006 to May 2007, the participation of pazopanib in patients with advanced renal cell carcinoma randomized clinical drug trials of outpatient 14 cases, were divided into pazopanib group (n = 10) and placebo group ( 4 cases), were treated with pazopanib 800mg / d and placebo after 12 weeks of treatment duration, according to the results of CT scan before and after medication , efficacy was determined . 
The results showed that the reduced average ratios of measurable disease focus of pazopanib and placebo patients were 27.6%, - 2.8% (P A clinical trail study phase I showed that compared with placebo, pazopanib can reduce the risk of death and tumor progression by 54%. Overall,in the product group of patients ,disease progression-free survival (PFS) mean survival time was 9.2 months ,in the placebo group was 4.2 months. In previously treated patients who had not received in this product group average survival time was 11.1 months in the placebo group was 2.8 months; previously received cytokine therapy patients, pazopanib group survived an average of 7.4 months, the placebo group was 4.2 months. 
The above information is edited by the chemicalbook of Tian Ye.
Adverse reactions Diarrhea, hypertension, hair color change, nausea, loss of appetite, vomiting, fatigue, weakness, headache, abdominal pain and so on. 
Cause serious liver problems, so health care workers should take blood tests to monitor liver function before using the drug in patients and during treatment of patients.
Hazardous to the fetus,people during pregnancy are forbid using this drug. 
Pazopanib can also lead to arrhythmias, during treatment patients should have regular electrocardiogram measuring heart rate, and regular blood tests to monitor electrolytes since an electrolyte imbalance will also play a role in arrhythmia.
Chemical Properties Off-White Solid
Usage Pazopanib Hydrochloride (GW786034, Votrient, Armala) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM, respectively.
Usage Pazopanib is a potent and selective multi-targeted receptor tyrosine kinase inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR-α/β, and c-Kit.
Usage Pazopanib is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM, respectively.
Usage An oral angiogenesis inhibitor targeting VEGFR and PDGFR.

 

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