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Chemical Structure| 923288-90-8 Chemical Structure| 923288-90-8

Structure of 923288-90-8

Chemical Structure| 923288-90-8

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Nilotinib monohydrochloride monohydrate is a second-generation tyrosine kinase inhibitor (TKI), significantly potent against BCR-ABL, and active against many BCR-ABL mutants.

Synonyms: AMN107 monohydrochloride monohydrate; Nilotinib (hydrochloride hydrate); AMN-107 hydrochloride monohydrate

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Product Details of Nilotinib monohydrochloride monohydrate

CAS No. :923288-90-8
Formula : C28H25ClF3N7O2
M.W : 583.99
SMILES Code : O=C(NC1=CC(C(F)(F)F)=CC(N2C=C(C)N=C2)=C1)C3=CC=C(C)C(NC4=NC=CC(C5=CC=CN=C5)=N4)=C3.[H]Cl.[H]O[H]
Synonyms :
AMN107 monohydrochloride monohydrate; Nilotinib (hydrochloride hydrate); AMN-107 hydrochloride monohydrate
MDL No. :MFCD18251359
InChI Key :YCBPQSYLYYBPDW-UHFFFAOYSA-N
Pubchem ID :16757572

Safety of Nilotinib monohydrochloride monohydrate

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of Nilotinib monohydrochloride monohydrate

RTK

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Ba/F3 cells 0.3–10 µM To investigate the inhibitory effects of GNF-5 in combination with nilotinib on the proliferation of T315I Bcr-Abl Ba/F3 cells, showing synergistic effects. PMC2901986
8093 lymphoblastic leukemia cells 200 nM 24 hours To evaluate the killing effect of nilotinib on lymphoblastic leukemia cells, results showed that 200 nM nilotinib reduced cell viability to 18% within 24 hours. PMC2169263
B-1 lymphoblastic leukemia cells 100 nM 24 hours To compare the killing effect of nilotinib and imatinib on B-1 cells, results showed that 100 nM nilotinib significantly reduced cell viability within 24 hours. PMC2169263
B-2 lymphoblastic leukemia cells 200 nM 24 hours To compare the killing effect of nilotinib and imatinib on B-2 cells, results showed that 200 nM nilotinib significantly reduced cell viability within 24 hours. PMC2169263
D04 cells 100nM 3 hours To investigate the effect of nilotinib on the MEK/ERK pathway, results showed that nilotinib at 100nM significantly activated MEK and ERK phosphorylation. PMC3951999
SW620 cells 1μM 3 hours To investigate the effect of nilotinib on the MEK/ERK pathway in SW620 cells, results showed that nilotinib at 1μM activated MEK and ERK phosphorylation. PMC3951999
Panc1 cells 1μM 3 hours To investigate the effect of nilotinib on the MEK/ERK pathway in Panc1 cells, results showed that nilotinib at 1μM activated MEK and ERK phosphorylation. PMC3951999
H460 cells 1μM 3 hours To investigate the effect of nilotinib on the MEK/ERK pathway in H460 cells, results showed that nilotinib at 1μM activated MEK and ERK phosphorylation. PMC3951999
BCR-ABLT315I Ba/F3 cells 1μM 4 days To investigate the effect of nilotinib on the proliferation of BCR-ABLT315I Ba/F3 cells, results showed that nilotinib in combination with the MEK inhibitor PD184352 significantly inhibited cell proliferation and induced apoptosis. PMC3951999
Nonparenchymal cells (NPCs) 1 μM 2 hours Nilotinib inhibited CpG-mediated activation of p38 MAPK and cytokine production in NPCs. PMC3437237
HCC cells 1–20μM 48 or 72 hours Nilotinib inhibited HCC cell growth PMC7387191

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
mice T315I Bcr-Abl bone marrow transplantation model orally 20 mg/kg Once daily for 20 days To evaluate the efficacy of GNF-5 in combination with nilotinib in a T315I Bcr-Abl mouse model, showing that the combination significantly prolonged survival and inhibited tumor growth. PMC2901986
mice P190 Bcr/Abl lymphoblastic leukemia model oral 75 mg/kg GNF-5 and 50 mg/kg nilotinib twice daily until day 50 post-transplantation To evaluate the therapeutic effect of nilotinib on P190 Bcr/Abl lymphoblastic leukemia in vivo, results showed that nilotinib significantly prolonged the survival of mice. PMC2169263
Nude mice BCR-ABLT315I Ba/F3 xenograft model Oral 75 mg/kg once daily for 50 days To investigate the effect of nilotinib in combination with the MEK inhibitor PD184352 on BCR-ABLT315I xenografts, results showed that the combination significantly inhibited tumor growth. PMC3951999
Mice Liver ischemia/reperfusion injury model Oral 10 mg/kg Every other day for 30 days Nilotinib significantly reduced serum ALT levels, histologic injury, and apoptosis following liver ischemia/reperfusion injury, and attenuated the inflammatory response by inhibiting JNK and p38 MAPK activation. PMC3437237
Mice MET/CAT-induced HCC model Oral 25 mg/kg Daily, for the duration of the treatment Nilotinib inhibited HCC tumor growth and prolonged survival in mice PMC7387191

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT01223898 Chronic Myeloid Leukemia PHASE1 COMPLETED 2025-12-13 Novartis Investigative Site, F... More >>rankfurt/M, 60590, Germany|Novartis Investigative Site, Jena, 07740, Germany|Novartis Investigative Site, Mannheim, 68167, Germany|Novartis Investigative Site, Ulm, 89081, Germany|Novartis Investigative Site, Glasgow, G12 0YN, United Kingdom Less <<
NCT01261429 Pigmented Villonodular Synovit... More >>is Less << PHASE2 COMPLETED 2025-04-13 Institut Bergonié, Bordeaux, F... More >>rance|Centre Oscar Lambret, Lille, France|Centre Léon Bérard, Lyon, France|H?pital La Timone, Marseille, France|Institut Paoli Calmettes, Marseille, France|Institut Curie, Paris, France|Institut Claudius Regaud, Toulouse, France|Institut Gustave Roussy, Villejuif, France|Istituto Nazionale dei Tumori, Milano, Italy|Regina Elena National Cancer Institute, Roma, Italy|Leiden University Medical Center, Leiden, Netherlands|Radboud University Nijmegen Medical Centre, Nijmegen, Netherlands|Sklodowska-Curie Memorial Cancer Center and Institute of Oncology, Warsaw, Poland|University College Hospital UCL Hospitals NHS Foundation Trust, London, United Kingdom|Oxford Cancer Centre, Oxford, United Kingdom Less <<
NCT01275586 Neurofibromatosis|NF1|Neurofib... More >>romas Less << EARLY_PHASE1 COMPLETED 2025-10-16 Riley Hospital for Children, I... More >>ndianapolis, Indiana, 46202, United States Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.71mL

0.34mL

0.17mL

8.56mL

1.71mL

0.86mL

17.12mL

3.42mL

1.71mL

References

 

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