Nilotinib

Nilotinib
Nilotinib
Nilotinib

Nilotinib

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10 Kilogram

Negotiable

  • Min.Order :10 Kilogram
  • Purity: 99（%）
  • Payment Terms : L/C,D/A,D/P,T/T,,MoneyGram,Other

Keywords

Nilotinib 641571-10-0 C28H22F3N7O

Quick Details

  • Appearance:white-off powder or granule
  • Application:Pharmaceutical Intermediates
  • PackAge:As required
  • ProductionCapacity:5|Metric Ton|Month
  • Storage:Keep in a cool & dry place
  • Transportation:by sea or by air

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Details:

Nilotinib Basic information
The treatment drug for the new chronic myelogenous leukemia (CML) Imatinib mesylate Side effects
Product Name: Nilotinib
Synonyms: Nilotinib(AMN 107);Nilotinib, AMN107, Tasigna;Nilotinib-d6;4-Methyl-N-(3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)-phenyl)-3-((4-(pyridin-3-yl)pyrimid;Nilotinib &aMp;4-Methyl-3-((4-(3-pyridinyl)-2-pyrimidinyl)amino)-N-(5-(4-methyl-1H-imidazol-1-yl)-3-(trifluoromethyl)phenyl)benzamide Nilotinib (AMN-107);Nilotinib 4-Methyl-3-((4-(3-pyridinyl)-2-pyrimidinyl)amino)-N-(5-(4-methyl-1H-imidazol-1-yl)-3-(trifluoromethyl)phenyl)benzamide;Nilotinib, >=99%
CAS: 641571-10-0
MF: C28H22F3N7O
MW: 529.52
EINECS: 700-544-5
Product Categories: AMN-107;Cardiovascular APIs;-;Inhibitors;API;Molecular Targeted Antineoplastic;Nucleotides and Nucleosides;Bases & Related Reagents;Intermediates & Fine Chemicals;Nucleotides;Pharmaceuticals;Pharmaceutical intermediate
Mol File: 641571-10-0.mol
Nilotinib Structure
 
Nilotinib Chemical Properties
density  1.36
storage temp.  -20°C Freezer
CAS DataBase Reference 641571-10-0(CAS DataBase Reference)
 
Safety Information
HS Code  29335990
MSDS Information
 
 
Nilotinib Usage And Synthesis
The treatment drug for the new chronic myelogenous leukemia (CML) Nilotinib is a novel drug for targeted cancer therapy and belongs to tyrosine kinase inhibitors for the treatment of patients of chronic myelogenous leukemia (CML) which is resistant to the Gleevec (imatinib) with an excellent efficacy. Gleevec is the primary-choice drug developed by Novartis Company for the treatment of chronic myelogenous leukemia (CML) . 
Nilotinib is the developed through the improvement of the molecular structure of imatinib with a stronger selectivity on the BCR-ABL kinase activity. The inhibitory effect of nilotinib on the tyrosine kinase is 30 times as high as that of imatinib. It is capable of suppressing the activity of the imatinib-resistant BCR-ABL mutant kinase while also being able to inhibit the activity of KIT and PDGFR kinase. 
With administration twice daily, nilotinib can targeted to the Bcr-Abl protein, interact with it and inhibit the emergence of cancer cells containing abnormal chromosomes. Bcr-Abl protein is produced by cells containing the abnormal Philadelphia chromosome. For patients of CML, this protein is considered to be an important factor for causing the excessive proliferation of cancer-causing white blood cells.
In clinical trials, after being subject to the Tasigna treatment, 42% of the patients who have Gleevec-resistant chronic phase Philadelphia chromosome-positive (Ph +) CML had their abnormal chromosomes reduced or disappear; for patients in accelerated phase, there were also 31% of patients can obtain the same effect.
A pivotal phase II clinical study has been designed to evaluate the oral formulation of nilotinib in the clinical treatment of patients of Ph+CML (resistant imatinib mesylate) and who had clear toxicity slow-phase and accelerated phase. There are several positive results including high efficiency, good tolerance and manageable security. Switzerland has worldwide first approved the potent and novel targeted treatment drug: nilotinib oral tablets (trade name: Tasigna) developed by the Novartis company. This is for the treatment of life-threatening chronic myeloid leukemia (CML) which can’t be cured by imatinib mesylate (trade name: Glivec) therapy or patients of CML who can’t tolerate imatinib mesylate. Dose Specifications: nilotinib: 300 mg/tablet, 400 mg /tablet.
Imatinib mesylate Imatinib mesylate is a new-generation targeted anti-cancer drugs of inhibitory effect on the platelet-derived growth factor (PDGF) receptor protein kinase. Of all kinds of anti-tumor drugs, it is of the best efficacy with its effectiveness rate in curing newly diagnosed chronic myelogenous leukemia (CML) being over 94% and 76% of patients can get cytological relief, the main indications are as follows: 
1, it can be used for the treatment of newly diagnosed Philadelphia chromosome-positive (Ph +) adult chronic myelogenous leukemia in chronic phase. 
2, it can be used for the treatment of Philadelphia chromosome-positive chronic myelogenous leukemia in acute transformation phase and accelerated phase.
3, it can be used for the treatment of chronic myelogenous leukemia in the chronic phase and has also been subject to treatment of interferon.
4, it can be used for the treatment of children chronic myelogenous leukemia relapsed after bone marrow suppression or can’t be cured by interferon therapy.
5, it can be used for the treatment of malignant gastrointestinal stromal tumors of KIT (CD117) positive which is unresectable or metastatic.
Side effects It has been conducted of safety studies on the oral administration of nilotinib oral formulation in 438 patients. The most common grade 3 or 4 adverse reactions are mainly on hematologic such as neutropenia and thrombocytopenia. Liver function tests can find elevated level of bilirubin, ester enzymes and blood sugar which is often temporary and can recover after certain time. These cases are easy to deal with can rarely led to discontinuation. Pancreatitis is <1%. Common adverse reactions induced by non-hematologic drug include eruption, pruritus, nausea, fatigue, headache, constipation and diarrhea. The severity degree is usually mild to moderate.
The above information is edited by the chemicalbook of Dai Xiongfeng.
Description Chronic myeloid leukemia (CML), a hematological stem-cell disorder, is definitively diagnosed by the detection of the Philadelphia chromosome, a truncated version of chromosome 22 resulting from the reciprocal translocation of chromosomes 9 and 22 induced by a single mutagenic event. The consequence is the juxtaposition of two genes creating a fusion gene BCR-ABL. This gene leads to the translation of a fusion protein with increased tyrosine kinase activity that contributes to the pathogenesis of CML. Targeting the BCR-ABL protein has led to the successful intervention of the disease. Now established as first-line therapy for CML, imatinib was the first selective tyrosine kinase inhibitor of BCR-ABL. Since imatinib only binds to an inactive conformation of the ABL kinase portion, the conformational restrictions contribute to its selectivity.
Chemical Properties Off-White Solid
Originator Novartis (Switzerland)
Uses Nilotinib (AMN1O7) might be useful in treatment of chronic myelogenous leukemia
Uses Nilotinib (AMN-107) is a Bcr-Abl inhibitor with IC50 less than 30 nM.
Uses Nilotinib-d6, is the labeled analogue of Nilotinib, which might be useful in treatment of chronic myelogenous leukemia.
Brand name Tasigna
Chemical Synthesis The first step in the synthesis of nilotinib involves the nucleophilic aromatic substitution of 3-fluoro-5-(trifluoromethyl)benzonitrile with 2-methylimidazole. The nitrile is then hydrolyzed with sodium hydroxide in aqueous dioxane. A Curtius rearrangement employing diphenylphosphoryl azide in tert-butanol affords the tert-butyl carbamate. Deprotection of the Boc group provides the 3-(4-methylimidazol-1-yl)-5-(trifluoromethyl)aniline piece for the convergent synthesis. Construction of the other half begins with the condensation of 3-amino-4- methylbenzoic acid methyl ester with cyanamide in refluxing ethanolic HCl to generate the 3-guanidinobenzoate. An enamino ketone, prepared by a Claisen condensation of 3-acetylpyridine with ethyl formate in the presence of sodium metal in hot toluene, is then cyclized with the guanidine to yield the pyridylpyrimidine. Following saponification of the ethyl ester, the resultant 4-methyl-3-[4-(3-pyridyl)pyrimidin-2-ylamino]benzoic acid is finally coupled with the aniline utilizing diethyl cyanophosphate to provide nilotinib.
 
Nilotinib Preparation Products And Raw materials

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