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Nilotinib

Nilotinib

Item no.	S1033-100
Manufacturer	Selleckchem
CASRN	641571-10-0
Amount	100 mg
Quantity options	100 mg 1 g 10 g 10 mM/1 mL 200 mg 25 mg 300 mg 50 mg 5 g
Category	Oncology Neuroscience Neural Signaling Inhibitors & Compound Libraries Small Molecules By Organ Lung Cancer Colorectal Cancer Heart & Blood Cancer Testicular & Prostate Cancer Brain Cancer Bone Cancer
Type	Inhibitors
Specific against	other
Smiles	CC1=C(C=C(C=C1)C(=O)NC2=CC(=CC(=C2)C(F)(F)F)N3C=C(N=C3)C)NC4=NC=CC(=N4)C5=CN=CC=C5
ECLASS 10.1	32160490
ECLASS 11.0	32160490
UNSPSC	12000000
Alias	AMN-107
Similar products	Nilotinib
Available
Manufacturer - Targets	BCR
Storage Conditions	2 years -80 in solvent
Molecular Weight	529, 52
Administration	Oral administration
Animal Models	Systemic 32D Bcr-Abl leukemia model in Female BALB/c mice, Bioluminescent Bcr-Abl model of CML in Female NOD-SCID mice and Bone marrow transplant Bcr-Abl model of CML in syngeneic Balb/c recipient mice
Cell lines	Human primary Schwann and schwannoma cells
Clinical Trials	Nilotinib has entered in a phase IV clinical trial in the treatment of philadelphia chromosome positive and chronic myelogenous leukemia in chronic phase.
Concentrations	1-10 uM
Dosages	75 mg/kg, 100 mg/kg
Formulation	10% NMP-90% PEG300, PEG300
IC50	30 nM [1], 30 nM [1], 30 nM [1], 30 nM [1], 30 nM [1], 30 nM [1]
In vitro	Nilotinib inhibits proliferation, migration, and actin filament formation, as well as the expression of alpha-SMA and collagen in activated HSCs. Nilotinib induces apoptosis of HSCs, which is correlated with reduced bcl-2 expression, increases p53 expression, cleavage of PARP, as well as increases expression of PPARgamma and TRAIL-R. Nilotinib also induces cell cycle arrest, accompanied by increased expression of p27 and downregulation of cyclin D1. Interestingly, Nilotinib not only inhibits activation of PDGFR, but also TGFRII through Src. Nilotinib significantly inhibits PDGF and TGFbeta-simulated phosphorylation of ERK and Akt. Furthermore, PDGF- and TGFbeta-activated phosphorylated form(s) of Abl in human HSCs are inhibited by Nilotinib. [2] Nilotinib inhibits most imatinib-resistant Bcr-Abl mutations, except for T315I. [3] Nilotinib inhibits PDGF-DD-mediated ERK1/2 activation, basal and PDGF-DD-mediated activation of PDGFRbeta and Akt, and schwannoma proliferation. Nilotinib is more potent than imatinib, exerting its maximal inhibitory effect at concentrations lower than steady-state trough plasma levels. [4] Nilotinib also significantly reduces the expression levels of the genes for TGF-beta1 and platelet-derived growth factor (PDGF). Nilotinib treatment also significantly inhibits the PDGF-induced proliferation of lung fibroblasts. [5] Nilotinib inhibits the proliferation of Ba/F3 cells expressing p210- and p190-Bcr-Abl, or K562 and Ku-812F cells with IC50 values <=12 nM. [6]
In vivo	Nilotinib reduces collagen deposition and alpha-SMA expression in CCl4 and BDL-induced fibrosis. Nilotinib could induce HSC undergoing apoptosis, which is correlated with downregulation of bcl-2. [2] Nilotinib attenuates the extent of lung injury and fibrosis. Nilotinib therapy significantly reduces the levels of hydroxyproline on days 14 and 21, which is accompanied by decreased expression levels of transforming growth factor (TGF)-beta1 and PDGFRbeta. [5] AMN107 prolongs survival of mice injected with Bcr-Abl-transformed hematopoietic cell lines or primary marrow cells, and prolongs survival in imatinib-resistant CML mouse models. [6]
Incubation Time	72 hours
Method	Human primary Schwann and schwannoma cells are seeded on precoated 96-well plates. Nilotinib is added 40 minutes before stimulation with 100 ng/mL PDGF-DD, and cells are cultured for 72 hours (3 days). Because the half-life of Nilotinib is 18 hours, one-half of the originally added concentrations are added freshly every day. In addition to DAPI staining and determination of the total cell number, the more sensitive and accurate BrdU incorporation method is used to detect proliferating cells. Total cell amount (DAPI) and number of dividing cells (BrdU-positive) are blindly counted using an inverted fluorescent microscope and 200, magnification. All cells in every well are counted. The total cell number per well differed between various cell batches and is 100â€“300 cells/well.
Solubility (25C)	DMSO 36 mg/mL, Water <1 mg/mL, Ethanol <1 mg/mL
Information	Nilotinib is a selective Bcr-Abl inhibitor with IC50 less than 30 nM in Murine myeloid progenitor cells. Nilotinib induces autophagy through AMPK activition.
Chemical Name	4-methyl-N-(3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)phenyl)-3-(4-(pyridin-3-yl)pyrimidin-2-ylamino)benzamide
Features	Nilotinib is a selective inhibitor of native and mutant Bcr-Abl.

Note: The presented information and documents (Manual, Product Datasheet, Safety Datasheet and Certificate of Analysis) correspond to our latest update and should serve for orientational purpose only. We do not guarantee the topicality. We would kindly ask you to make a request for specific requirements, if necessary.

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S1033-100-datasheet.pdf

S1033-100-safety-datasheet.pdf