Buy Nilotinib (AMN-107) | Bcr-Abl Inhibitors | Price | IC50

Validation & Quality Control

Product Citations(3)

Leuk Res, 2012, ahead of print

Leuk Res, 2012, 36(10):1311-4

FASEB J, 2011, 25(10), 3661-3673

Customer Reviews(2) in vivo invitation

Quality Control & MSDS

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Nilotinib (AMN-107) is available in the following compound libraries:

Cambridge Cancer Compound Library(96-well) Chemical Library (96-well) FDA Approved Drug Library (96-well) Inhibitor Library (96-well) Kinase Inhibitor Library (96-well) Stem Cell Small Molecule Compound Library (96-well) Tyrosine Kinase Inhibitor Library (96-Well)

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S1021	Dasatinib (BMS-354825)	<1 mg/mL	98 mg/mL	<1 mg/mL
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S1033	Nilotinib (AMN-107)	<1 mg/mL	36 mg/mL	<1 mg/mL
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S1107	Danusertib (PHA-739358)	<1 mg/mL	95 mg/mL	<1 mg/mL
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S2899	GNF-2	<1 mg/mL	75 mg/mL	<1 mg/mL

Combination Therapy

Dr. Antonino Maria Sparta demonstrates a breakthrough in leukemia research by utilizing two inhibitors produced by Selleck Chemicals.

Product Description

Biological Activity Protocol Chemical Information Customer Reviews Product Citations Tech Support & FAQs

Biological Activity

Description	Nilotinib (AMN-107, Tasigna) is a Bcr-Abl inhibitor with IC50 less than 30 nM.
Targets	Bcr-Abl
IC50	30 nM ^[1]
In vitro	Nilotinib inhibits proliferation, migration, and actin filament formation, as well as the expression of α-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 PPARγ 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 TGFβ-simulated phosphorylation of ERK and Akt. Furthermore, PDGF- and TGFβ-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 PDGFRβ 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-β1 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 α-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)-β1 and PDGFRβ. ^[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]
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.
Features	Nilotinib is a selective inhibitor of native and mutant Bcr-Abl.

Protocol(Only for Reference)

Cell Assay: ^[4]

Cell lines	Human primary Schwann and schwannoma cells
Concentrations	1-10 μM
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 100–300 cells/well.

Animal Study: ^[6]

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
Formulation	10% NMP-90% PEG300, PEG300
Dosages	75 mg/kg, 100 mg/kg
Administration	Oral administration

1

References

Chemical Information

Download Nilotinib (AMN-107) SDF

Molecular Weight (MW)	529.52
Formula	C₂₈H₂₂F₃N₇O
CAS No.	641571-10-0
Synonyms	Tasigna

Solubility (25°C) DMSO 36 mg/mL Water <1 mg/mL Ethanol <1 mg/mL
Storage	2 years -20°CPowder
	2 weeks4°Cin DMSO
	6 months-80°Cin DMSO

Chemical Name	4-methyl-N-(3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)phenyl)-3-(4-(pyridin-3-yl)pyrimidin-2-ylamino)benzamide

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Research Area

Customer Reviews (2)

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Rating

Source

Leukemia Research, 36 (2012) 1311– 1314. Nilotinib (AMN-107) purchased from Selleck

Method

Thymidine uptake Uptake assay

Cell Lines

K562, MEG-01 cells

Concentrations

0.1-10uM

Incubation Time

20 min

Results

Nilotinib was much more potent than imatinib to inhibit nucleoside transport. It prevented the uptake of thymidine in K562 cells by 97% at 10 uM, a level that was similar to the one obtained with the vasodilatator molecule dipyridamole. Nilotinib was also very efficient at 1 and 0.1 uM; it blocked the entry of thymidine by 90 and 74%, respectively (Fig. 2a). With the MEG-01 cell line, nilotinib was also extremely potent and blocked the entry of thymidine by 96, 92 and 60% with 10, 1 and 0.1 uM nilotinib, respectively (Fig. 2b).

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Rating

Source

FASEB J , 2011, 25(10), 3661-3673. Nilotinib (AMN-107) purchased from Selleck

Method

Analyzing cell apoptosis

Cell Lines

Ba/F3-p210T315I cells

Concentrations

0-5 μM

Incubation Time

24 h

Results

In a parallel study using imatinib/PDMP or nilotinib/PDMP combinations, to our surprise, similar signiﬁcant synergy in Ba/F3-p210T315I cells was observed.

Product Citations (3)

Imatinib and Nilotinib inhibit Bcr-Abl-induced ROS through targeted degradation of the NADPH oxidase subunit p22phox. [Landry WD, et al. Leuk Res 2012;ahead of print]
PubMed: 23218026
Nilotinib and imatinib inhibit cytarabine cellular uptake: Implications for combination therapy. [Naud JS, et al. Leuk Res 2012;36(10):1311-4]
PubMed: 22796208
Glucosylceramide synthase inhibitor PDMP sensitizes chronic myeloid leukemia T315I mutant to Bcr-Abl inhibitor and cooperatively induces glycogen synthase kinase-3-regulated apoptosis. [Huang WC, et al. FASEB J 2011;25(10), 3661-3673]
PubMed: 21705667

Tech Support & FAQs

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Related Bcr-Abl Inhibitors

Saracatinib (AZD0530)

Saracatinib (AZD0530) is a Src inhibitor for c-Src and v-Abl with IC50 of 2.7 nM and 30 nM, respectively.
Danusertib (PHA-739358)

Danusertib (PHA-739358) is an Aurora inhibitor for Aurora A/B/C, Bcr-Abl, c-RET and FGFR with IC50 of 13 nM/79 nM/61 nM, 25 nM, 31 nM and 47 nM, respectively.
AT9283

AT9283 is a potent pan-Aurora inhibitor for Aurora A, Aurora B, JAK3, JAK2 and Abl with IC50 of 3 nM, 3 nM, 1.1 nM, 1.2 nM and 4 nM, respectively.
Bafetinib (INNO-406)
Bafetinib (INNO-406) is a potent and selective dual Bcr-Abl/Lyn inhibitor with IC50 of 5.8 nM and 19 nM, respectively.
KW 2449

KW-2449 potently inhibits Flt3, Abl and Aurora A with IC50 of 6.6 nM, 14 nM and 48 nM, respectively.
NVP-BHG712
NVP-BHG712 is a specific inhibitor of c-Raf, c-Src and c-Abl with IC50 of 0.395 μM, 1.266 μM and 1.667 μM and also inhibits EphB4 and VEGFR2 with ED50 of 25 nM and 4.2 μM, respectively.
WP1130
WP1130 (degrasyn) is a selective deubiquitinase (DUB) inhibitor and also inhibits Bcr/Abl with IC50 of 1.8 μM.
DCC-2036 (Rebastinib)
DCC-2036 is a conformational control inhibitor of Abl1 and Abl1(T315I) with IC50 of 0.8 nM and 4 nM, respectively.
GNF-2

GNF-2 is a highly selective non-ATP competitive inhibitor of Bcr-Abl, inhibiting the proliferation of the Bcr-Abl-expressing cells with IC50 of 138 nM.
FG-4592
FG-4592 is an HIF α prolyl hydroxylase inhibitor.

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Nilotinib (AMN-107)

Validation & Quality Control

Product Citations(3)

Customer Reviews(2) in vivo invitation

Quality Control & MSDS

Related Compound Libraries

Nilotinib (AMN-107) is available in the following compound libraries:

Product Information

Compare Bcr-Abl Inhibitors

Research Area

Combination Therapy

Product Description

Biological Activity

Protocol(Only for Reference)

Cell Assay: ^[4]

Animal Study: ^[6]

References

Chemical Information

Research Area

Customer Reviews (2)

Product Citations (3)

Tech Support & FAQs

If you have any other enquiries, please leave a message.

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Product Categories

Nilotinib (AMN-107)

Validation & Quality Control

Product Citations(3)

Customer Reviews(2) in vivo invitation

Quality Control & MSDS

Related Compound Libraries

Nilotinib (AMN-107) is available in the following compound libraries:

Product Information

Compare Bcr-Abl Inhibitors

Research Area

Combination Therapy

Product Description

Biological Activity

Protocol(Only for Reference)

Cell Assay: [4]

Animal Study: [6]

References

Chemical Information

Research Area

Customer Reviews (2)

Product Citations (3)

Tech Support & FAQs

If you have any other enquiries, please leave a message.

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Cell Assay: ^[4]

Animal Study: ^[6]