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Nilotinib

The treatment drug for the new chronic myelogenous leukemia (CML) Imatinib mesylate Side effects
Nilotinib
Nilotinib structure
CAS No.
641571-10-0
Chemical Name:
Nilotinib
Synonyms
AMN 107;Tasigna;Nilotinib;Nilotinib-d6;Nilotinib &aMp;Nilotinib, >=99%;Nilotinib(AMN 107);Nilotinib(TINIBS );Nilotinib for research;Nilotinib, AMN107, Tasigna
CBNumber:
CB5966228
Molecular Formula:
C28H22F3N7O
Formula Weight:
529.52
MOL File:
641571-10-0.mol

Nilotinib Properties

Density 
1.36
storage temp. 
-20°C Freezer
CAS DataBase Reference
641571-10-0(CAS DataBase Reference)

SAFETY

Nilotinib price More Price(4)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Cayman Chemical 10010422 Nilotinib ≥95% 641571-10-0 5mg $19 2018-11-19 Buy
Cayman Chemical 10010422 Nilotinib ≥95% 641571-10-0 10mg $29 2018-11-19 Buy
Cayman Chemical 10010422 Nilotinib ≥95% 641571-10-0 25mg $59 2018-11-19 Buy
Cayman Chemical 10010422 Nilotinib ≥95% 641571-10-0 50mg $96 2018-11-19 Buy

Nilotinib Chemical Properties,Uses,Production

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

Raw materials

Preparation Products


Nilotinib Suppliers

Global( 241)Suppliers
Supplier Tel Fax Email Country ProdList Advantage
Frapp's ChemicalNFTZ Co., Ltd.
+86 (576) 8169-6106
+86 (576) 8169-6105 sales@frappschem.com China 887 50
Capot Chemical Co.,Ltd.
+86 (0)571-855 867 18
+86 (0)571-858 647 95 sales@capotchem.com China 19954 60
Henan DaKen Chemical CO.,LTD.
+86-371-55531817
info@dakenchem.com CHINA 22043 58
Beijing Cooperate Pharmaceutical Co.,Ltd.
+86-10-60279497 +86(0)15646567669
+86-10-60279497 sales01@cooperate-pharm.com CHINA 1530 55
Henan Tianfu Chemical Co.,Ltd.
0371-55170693
0371-55170693 info@tianfuchem.com CHINA 20786 55
Mainchem Co., Ltd.
+86-0592-6210733
+86-0592-6210733 sales@mainchem.com CHINA 32651 55
Hubei XinRunde Chemical Co., Ltd.
+8615102730682; +8618874586545
02783214688 bruce@xrdchem.cn CHINA 552 55
ATK CHEMICAL COMPANY LIMITED
+86 21 5161 9050/ 5187 7795
+86 21 5161 9052/ 5187 7796 ivan@atkchemical.com CHINA 16534 60
Anqing Chico Pharmaceutical Co., Ltd.
15380796838
chloewu@chicopharm.cn CHINA 209 58
Biochempartner
0086-13720134139
candy@biochempartner.com CHINA 956 58

View Lastest Price from Nilotinib manufacturers

Image Release date Product Price Min. Order Purity Supply Ability Manufacturer
2019-04-10 Nilotinib
641571-10-0
US $1.00 / kg 1kg 99.8% 100kg Hebei Jimi Trading Co., Ltd.
2018-08-06 Nilotinib
641571-10-0
US $1.00 / KG 1KG 98% 1 career henan chemical co
2018-03-08 Nilotinib
641571-10-0
US $100.00 / KG 10G 99% 2Kg Hubei XinRunde Chemical Co., Ltd.

641571-10-0(Nilotinib)Related Search:


  • 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%
  • 4-Methyl-N-(3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)-phenyl)-3-((4-(pyridin-3-yl)pyri
  • Nilotinib
  • AMN 107
  • Benzamide, 4-methyl-N-[3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)phenyl]-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]-
  • -
  • AMN-107
  • Cardiovascular APIs
  • Inhibitors
  • API
  • Molecular Targeted Antineoplastic
  • Nucleotides and Nucleosides
  • 4-methyl-N-[3-(4-methylimidazol-1-yl)-5-(trifluoromethyl)phenyl]-3-[(4 -pyridin-3-ylpyrimidin-2-yl)amino]benzamide
  • Nilotinib(TINIBS )
  • 4-Methyl-3-((4-(3-pyridinyl)-2-pyrimidinyl)amino)-N-(5-(4-methyl-1H-imidazol-1-yl)-3-(trifluoromethyl)phenyl)benzamide
  • Nilotinib for research
  • Tasigna
  • 4-methyl-N-(3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)phenyl)-3-(4-(pyridin-3-yl)pyrimidin-2-ylamino)benzamide
  • Nilotinib & its intermediates
  • 641571-10-0
  • C28H22F3N7O
  • Bases & Related Reagents
  • Intermediates & Fine Chemicals
  • Nucleotides
  • Pharmaceuticals
  • Pharmaceutical intermediate
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