description Clinical Use Uses
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Nilotinib Hydrochloride Monohydrate

description Clinical Use Uses
Product Name
Nilotinib Hydrochloride Monohydrate
CAS No.
923288-90-8
Chemical Name
Nilotinib Hydrochloride Monohydrate
Synonyms
Nilotinib hydrochloride Monohydrate;Nilotinib HCl;Nilotinib HCl Hydrate;Nilotinib Hydrochloride Hydrate;4-Methyl-N-[3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)phenyl]-3-{[4-(3-pyridinyl)-2-pyrimidinyl]amino}benzamide hydrochloride hydrate;NILOTINIB;TASIGNA;Nilotinib monohydrate;AMN-107;AMN107;TASIGNA;Nilotinib hcl monohydrate;Nilotinib hydrochloride H2O
CBNumber
CB32469912
Molecular Formula
C28H25ClF3N7O2
Formula Weight
583.9920096
MOL File
923288-90-8.mol
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Nilotinib Hydrochloride Monohydrate Property

Melting point:
198-201°C
storage temp. 
-20°C Freezer
solubility 
Aqueous Acid (Slightly), DMSO (Slightly), Ethanol (Slightly, Heated)
form 
Solid
color 
Off-White to Pale Beige
InChIKey
YCBPQSYLYYBPDW-UHFFFAOYSA-N
SMILES
N1(C=C(N=C1)C)C1C=C(C=C(C=1)NC(=O)C1C=CC(=C(NC2=NC=CC(C3=CC=CN=C3)=N2)C=1)C)C(F)(F)F.Cl.O
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

TRC
Product number
N465295
Product name
NilotinibMonohydrochlorideMonohydrate
Packaging
250mg
Price
$80
Updated
2021/12/16
TRC
Product number
N465295
Product name
NilotinibMonohydrochlorideMonohydrate
Packaging
5g
Price
$485
Updated
2021/12/16
Biorbyt Ltd
Product number
orb611890
Product name
Nilotinib monohydrochloride monohydrate
Purity
>98%
Packaging
1g
Price
$615.4
Updated
2021/12/16
ChemScene
Product number
CS-1212
Product name
Nilotinibmonohydrochloridemonohydrate
Purity
99.97%
Packaging
5g
Price
$960
Updated
2021/12/16
ApexBio Technology
Product number
A3660
Product name
Nilotinibmonohydrochloridemonohydrate
Packaging
250mg
Price
$70
Updated
2021/12/16
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Nilotinib Hydrochloride Monohydrate Chemical Properties,Usage,Production

description

Nilotinib Hydrochloride Monohydrate(923288-90-8) is the monohydrate monohydrochloride form of nilotinib, an orally bioavailable aminopyrimidine-derivative Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity. Designed to overcome imatinib resistance resulting from Bcr-Abl kinase mutations, upon administration, nilotinib binds to and stabilizes the inactive conformation of the kinase domain of the Abl portion of the Bcr-Abl fusion protein, resulting in the inhibition of the constitutive kinase activity of Bcr-Abl protein. This inhibits the Bcr-Abl-mediated proliferation of Philadelphia chromosome-positive (Ph+) chronic myeloid leukemia (CML) cells. Nilotinib also inhibits the receptor tyrosine kinases platelet-derived growth factor receptor (PDGF-R; PDGFR), mast/stem cell growth factor receptor Kit (c-Kit), and, to a lesser extent, colony-stimulating factor 1 receptor (CSF-1R; CSF1R), and discoidin domain-containing receptor 1 (DDR1).
Nilotinib Hydrochloride Monohydrate (Code C95229)

Clinical Use

Nilotinib hydrochloride monohydrate(923288-90-8) was approved by FDA in 2007 for the treatment of chronic and accelerated phase Ph chromosome-positive CML adult patients which have developed resistance or intolerance to prior therapy that included imatinib. In 2012, apart from these previous indications, nilotinib hydrochloride monohydrate has also been indicated for the treatment of newly diagnosed adult patients with Ph chromosome-positive CML in chronic phase.

Uses

Nilotinib Monohydrochloride Monohydrate might be useful in treatment of chronic myelogenous leukemia. It is a COVID19-related research product.

Chemical Properties

Nilotinib hydrochloride monohydrate (NHM) lacks a chiral center, making it incapable of tautomerism. NHM is a chemical compound with the following name: 4-methyl-N-[3-(4-methyl-1H-imidazol1-yl)-5-(trifuoromethyl) phenyl]-3-[(4-pyridin-3-ylpyrimidin-2-yl) amino] benzamide hydrochloride monohydrate. It is a white powder with a slight yellowish or greenish-yellowish shade. At 25 °C, the aqueous solubility of NHM markedly decreases with pH. Moreover, it is almost insoluble in bufer solutions with pH values higher than 4.5. NHM shows slight solubility in ethanol and methanol. Nilotinib Hydrochloride Monohydrate is the monohydrate monohydrochloride form of nilotinib, an orally bioavailable aminopyrimidine-derivative Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity.

Chemical Properties

Uses

Nilotinib Monohydrochloride Monohydrate might be useful in treatment of chronic myelogenous leukemia. It is a COVID19-related research product.

Definition

Nilotinib, also known as AMN107, is a tyrosine kinase inhibitor under investigation as a possible treatment for chronic myelogenous leukemia (CML). A Phase I clinical trial in 2006 showed that this drug was relatively safe and offered significant therapeutic benefits in cases of CML which were found to be resistant to treatment with imatinib (Gleevec), another tyrosine kinase inhibitor used as a first-line treatment for CML.

Mechanism of action

Tasigna (nilotinib hydrochloride monohydrate) is an orally available signal transduction inhibitor of the Bcr-Abl kinase, c-kit and Platelet Derived Growth Factor (PDGF). Nilotinib binds to and stabilizes the inactive conformation of the kinase domain of Abl protein. In vitro, nilotinib inhibited Bcr-Abl mediated proliferation of murine leukemic cell lines and human cell lines derived from Ph+ CML patients. In vivo, nilotinib reduced the tumor size in a murine Bcr-Abl xenograft model.

Side effects

a headache, fatigue, gastrointestinal problems such as nausea, vomiting, diarrhea and constipation, muscle and joint pain, rash and other skin conditions, flu-like symptoms, and reduced blood cell count. Less typical side effects are those of the cardiovascular system, such as hypertension (high blood pressure), various types of arrhythmia, and prolonged QT interval. Interaction of nilotinib with OATP1B1 and OATP1B3 may alter its hepatic disposition and can lead to transporter mediated drug-drug interactions.

in vitro

In vitro, nilotinib inhibited Bcr-Abl mediated proliferation of murine leukemic cell lines and human cell lines derived from Ph+ CML patients. Under the conditions of the assays, nilotinib was able to overcome imatinib resistance resulting from Bcr-Abl kinase mutations, in 32 out of 33 mutations tested. In vivo, nilotinib reduced the tumor size in a murine Bcr-Abl xenograft model. Nilotinib inhibited the autophosphorylation of the following kinases at IC50 values as indicated: Bcr-Abl (20-60 nM), PDGFR (69 nM) and c-Kit (210 nM). Nilotinib is currently being trialed in people with Parkinson's disease, as it appears to be able to halt progression of the disease and even improve their symptoms.

Nilotinib Hydrochloride Monohydrate Preparation Products And Raw materials

Raw materials

Preparation Products

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Nilotinib Hydrochloride Monohydrate Suppliers

Yangzhou QinYuan Pharmaceutical Co., Ltd.
Tel
0514-80939770 13773367191
Fax
0514-82664689
Email
yzqyyykj@163.com
Country
China
ProdList
240
Advantage
55
Biopole Pharmatech Co., Ltd.
Tel
0512-65974739-0 15151475053
Email
mengqi_biopole@163.com
Country
China
ProdList
45
Advantage
58
Xiamen Halosyntech Co., Ltd
Tel
0592-6688068 18106901346
Fax
0592-6686768
Email
qbl2015@halolife.cn
Country
China
ProdList
100
Advantage
55
Shanghai Boyle Chemical Co., Ltd.
Tel
Fax
86-21-57758967
Email
sales@boylechem.com
Country
China
ProdList
2922
Advantage
55
Chembest Research Laboratories Limited
Tel
+86-21-20908456
Fax
021-58180499
Email
sales@BioChemBest.com
Country
China
ProdList
6005
Advantage
61
Shanghai T&W Pharmaceutical Co., Ltd.
Tel
+86 21 61551611
Fax
+86 21 50676805
Country
China
ProdList
9891
Advantage
58
Haoyuan Chemexpress Co., Ltd.
Tel
021-58950125
Fax
(86) 21-58955996
Email
info@chemexpress.com
Country
China
ProdList
7552
Advantage
61
Guangzhou Isun Pharmaceutical Co., Ltd
Tel
020-39119399 18927568969
Fax
020-39119999
Email
isunpharm@qq.com
Country
China
ProdList
4428
Advantage
55
Nanjing Sunlida Biological Technology Co., Ltd.
Tel
025-57798810
Fax
025-57019371
Email
sales@sunlidabio.com
Country
China
ProdList
3239
Advantage
55
TargetMol Chemicals Inc.
Tel
021-021-33632979 15002134094
Fax
021-33632979
Email
marketing@targetmol.com
Country
China
ProdList
7783
Advantage
58
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View Lastest Price from Nilotinib Hydrochloride Monohydrate manufacturers

Nanjing Fred Technology Co., Ltd
Product
Nilotinib hydrochloride hydrate 923288-90-8
Price
US $0.00-0.00/kg
Min. Order
1kg
Purity
99%,single impurity<0.1
Supply Ability
1 ton
Release date
2023-12-20
BEIJING SJAR TECHNOLOGY DEVELOPMENT CO., LTD.
Product
Nilotinib Hydrochloride Monohydrate 923288-90-8
Price
US $0.00/g
Min. Order
1g
Purity
More Than 99%
Supply Ability
100kg/Month
Release date
2024-08-02
Biopole Pharmatech Co., Ltd.
Product
Nilotinib Hydrochloride Monohydrate 923288-90-8
Price
US $0.00/g
Min. Order
1g
Purity
0.99
Supply Ability
100kg
Release date
2024-01-22

923288-90-8, Nilotinib Hydrochloride MonohydrateRelated Search:


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  • Nilotinib monohydrochloride monohydrate 4-Methyl-N-[3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)phenyl]-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]-benzamide hydrochloride hydrate (1:1:1)
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  • 4-METHYL-N-[3-(4-METHYLIMIDAZOL-1-YL)-5-(TRIFLUOROMETHYL)PHENYL]-3-[(4-PYRIDIN-3-YLPYRIMIDIN-2-YL)AM
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  • C28H22F3N7OHClH2O
  • C28H25ClF3N7O2
  • C28H22F3N7OClHH2O