General
Preferred name
NILOTINIB
Synonyms
AMN-107 ()
AMN-107, Tasigna, Nilotinib Hydrochloride Monohydrate ()
Nilotinib (monohydrochloride monohydrate) ()
AMN107 (monohydrochloride monohydrate) ()
Tasigna ()
AMN107 ()
AMN-107 HCl ()
Nilotinib (AMN-107) ()
Nilotinib monohydrochloride monohydrate ()
Nilotinib hydrochloride ()
Nilotinib (hydrochloride dihydrate) ()
AMN107 (hydrochloride dihydrate) ()
Tasigna, AMN-107 hydrochloride monohydrate ()
NILOTINIB HYDROCHLORIDE MONOHYDRATE ()
NilotinibTasignaAMN107Benzamide, 4-methyl-N-[3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)phenyl]-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]- ()
AMN 107 ()
NSC-747599 ()
NILOTINIB LAURYLSULFATE ()
Nilotinib-d6 ()
Nilotinib hydrochloride hydrate ()
Nilotinib hydrochloride anhydrous ()
Nilotinib (as hydrochloride) ()
Nilotinib (hydrochloride hydrate) ()
P&D ID
PD003312
CAS
641571-10-0
1353151-22-0
923288-90-8
923288-95-3
1268356-17-7
Tags
available
drug
drug candidate
Approved by
FDA
First approval
2007
Drug indication
chronic myelogenous leukemia
Acute myeloid leukemia
Chronic myelogenous leukaemia
Neoplasm
Drug Status
approved
investigational
Max Phase
1.0
4.0
Structure
Probe scores
P&D probe-likeness score
[[ v.score ]]%
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION Nilotinib is a Type-2 kinase inhibitor and was first approved by the FDA in 2007.
Preclinical studies in rodent Parkinson's disease models suggest that nilotinib has some potential to promote autophagic degradation of α-synuclein , a brain protein whose accumulation and aggregation contributes to the formation of toxic insoluble fibrils which cause pathological changes such as neuronal loss in Parkinson's disease and other synucleinopathies. This mechanism has been evaluated in a pilot, proof-of-concept and safety clinical trial in a small number of patients with Parkinson's disease- and diffuse Lewy body disease-associated cognitive impairment (see NCT02281474; note that this trial is not placebo controlled or blinded). (GtoPdb)
DESCRIPTION Nilotinib is an orally available Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity.
PRICE 29
DESCRIPTION Nilotinib monohydrochloride monohydrate is a second generation tyrosine kinase inhibitor (TKI), is significantly potent against BCR-ABL, and is active against many BCR-ABL mutants.
PRICE 29
PRICE 60
DESCRIPTION inhibitor of ABL1, BCR, and c-KIT (Informer Set)
DESCRIPTION For the potential treatment of various leukemias, including chronic myeloid leukemia (CML). (PKIDB)
DESCRIPTION Nilotinib is a kinase inhibitor used for the chronic phase treatment of Chronic Myeloid Leukemia (CML) that is Philadelphia chromosome positive and for the treatment of CML that is resistant to therapy containing imatinib. (Enamine Bioactive Compounds)
DESCRIPTION Nilotinib (AMN107) is a Bcr-Abl tyrosine kinase inhibitor with oral activity. Nilotinib has antitumor activity and may be used for the treatment of Imatinib-resistant chronic myelogenous leukemia (CML). (TargetMol Bioactive Compound Library)
DESCRIPTION Nilotinib monohydrochloride monohydrate (Nilotinib (monohydrochloride monohydrate)) is significantly potent BCR-ABL against, is a second generation tyrosine kinase inhibitor (TKI), and is active against many BCR-ABL mutants. (TargetMol Bioactive Compound Library)
DESCRIPTION Nilotinib is an orally bioavailable Bcr-Abl tyrosine kinase inhibitor displaying antineoplastic activity. It is promisingly used for the treatment of chronic myelogenous leukemia (CML). (BOC Sciences Bioactive Compounds)
DESCRIPTION Nilotinib hydrochloride(AMN-107 HCl) is an orally available Bcr-Abl tyrosine kinase inhibitor with antitumor activity for modulation of neuroinflammation and cognitive deficits, and may be used in studies of chronic myelogenous leukemia. (TargetMol Bioactive Compound Library)
Cell lines
332
Organisms
2
Compound Sets
38
AdooQ Bioactive Compound Library
Axon Medchem Screening Library
BOC Sciences Bioactive Compounds
Cayman Chemical Bioactives
ChEMBL Approved Drugs
Clinical kinase drugs
Concise Guide to Pharmacology 2017/18
Concise Guide to Pharmacology 2019/20
Concise Guide to Pharmacology 2021/22
Concise Guide to Pharmacology 2023/24
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugBank
DrugBank Approved Drugs
DrugCentral
DrugCentral Approved Drugs
DrugMAP
DrugMAP Approved Drugs
Enamine Bioactive Compounds
EU-OPENSCREEN Bioactive Compound Library
EUbOPEN Chemogenomics Library
Guide to Pharmacology
Informer Set
LINCS compound set
LSP-MoA library (Laboratory of Systems Pharmacology)
LSP-OptimalKinase library (Laboratory of Systems Pharmacology)
MedChem Express Bioactive Compound Library
Natural product-based probes and drugs
NCATS Inxight Approved Drugs
NIH Approved Oncology Drugs
Novartis Chemogenetic Library (NIBR MoA Box)
PKIDB
ReFrame library
TargetMol Bioactive Compound Library
Welcome Trust Cancer Drugs
External IDs
81
Properties
(calculated by RDKit )
Molecular Weight
529.18
Hydrogen Bond Acceptors
7
Hydrogen Bond Donors
2
Rotatable Bonds
6
Ring Count
5
Aromatic Ring Count
5
cLogP
6.36
TPSA
97.62
Fraction CSP3
0.11
Chiral centers
0.0
Largest ring
6.0
QED
0.27
Structural alerts
0
No structural alerts detected
Custom attributes
(extracted from source data)
Target
ABL1
BCR
KIT
ABL
ABL1, KIT
Bcr-Abl inhibitor
AMPK,Autophagy,Bcr-Abl
Compound status
FDA
Pathway
ABL signaling
Angiogenesis
Autophagy
Cytoskeletal Signaling
Tyrosine Kinase/Adaptors
Protein Tyrosine Kinase/RTK
MOA
Bcr-Abl
Apoptosis Inducers
Inhibitors of Signal Transduction Pathways
Bcr-Abl Kinase Inhibitors
Abl kinase inhibitor, Bcr-Abl kinase inhibitor
Member status
member
Indication
chronic myeloid leukemia (CML)
Therapeutic Indication
Anticancer
Therapeutic Class
Anticancer Agents
VGSC Target
Nav1.5
Recommended Cell Concentration
None
Source data