Nilotinib (AMN-107)

Catalog No.S1033

Nilotinib (AMN-107) Chemical Structure

Molecular Weight(MW): 529.52

Nilotinib (AMN-107) is a selective Bcr-Abl inhibitor with IC50 less than 30 nM in Murine myeloid progenitor cells.

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Cited by 21 Publications

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  • Ba/F3-p210T315I cells were treated with indicated concentrations of nilotinib with or without PDMP for 24 h. Apoptosis was determined as in A. Data are shown as percentage of sub-G1 for apoptosis in triplicate cultures. *P<0.05.

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

    Effect of nilotinib on Bcr-Abl kinase activity in ABCB1- and ABCG2- overexpressing CD34+CD38- cells. K562 parental cells and CD34+CD38- subpopulation isolated from K562 cells were treated with nilotinib at 0.01, 0.1 and 1.0 umol/L for 12 h. Equal amount of protein was loaded for western blot analysis as described in the Experimental section. The experiments were repeated at least three times independently, and a representative experiment is shown.

    Molecules 2014 19, 3356-75. Nilotinib (AMN-107) purchased from Selleck.

  •  

    Inhibition of thymidine (a and b) and cytarabine (c and d) uptake with nilotinib. The legend is similar to Fig. 1, except that imatinib was replaced by nilotinib.

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

    Nilotinib up-regulates the ERK survival signal in prostate cancer cells. (B and C) Immunoblot analyses of DU-145 cells (B) or DU-145 cells in comparison with LNCaP and PC-3 cells (C) treated with nilotinib for the expression of phospho-ERK1/2 T202/Y204 and total ERK. Immunoblot for GAPDH is shown as a loading control.

    Urol Oncol 2014 0.1016/j.urolonc.2014.06.001. Nilotinib (AMN-107) purchased from Selleck.

  • Immunohistochemical staining of xenografted DU-145 cells after 21 days of treatment with 75 mg/kg/d of nilotinib for phospho-ERK1/2 T202/Y204 expression. It can be noted that tumors explanted from vehicle-treated mice showed mostly positivity at the tumor periphery, whereas tumors explanted from nilotinib-treated mice showed a more evenly distributed phospho-ERK immunostaining (left panels). Quantification of phospho-ERK-positive DU-145 xenografts explanted after 21 days of treatment. Mean and standard errors of positive cells per high-power field (HPF; x40) from at least 3 tumors are given (right panel).

    Urol Oncol 2014 0.1016/j.urolonc.2014.06.001. Nilotinib (AMN-107) purchased from Selleck.

Purity & Quality Control

Choose Selective Bcr-Abl Inhibitors

Biological Activity

Description Nilotinib (AMN-107) is a selective Bcr-Abl inhibitor with IC50 less than 30 nM in Murine myeloid progenitor cells.
Features A selective inhibitor of native and mutant Bcr-Abl.
Targets
Bcr-Abl [1]
(Murine myeloid progenitor cells)
<30 nM
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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
EoL-1-cell Mke4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVrJR|UxRTBwMECwNVQ1KM7:TR?= M4TETXNCVkeHUh?=
KU812 Mn7jS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3XjUGlEPTB;MD6wNFI1QCEQvF2= MmnoV2FPT0WU
EM-2 M332Nmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXXJR|UxRTBwMEC0NUDPxE1? NWPPbmsyW0GQR1XS
LAMA-84 M2DHUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnLDTWM2OD1yLkCwOFkh|ryP NHnCWoFUSU6JRWK=
MEG-01 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHXETJNKSzVyPUCuNFA5OjhizszN NV\vPXJ3W0GQR1XS
BV-173 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG[2d4tKSzVyPUCuNFExQDlizszN NVHJ[2xqW0GQR1XS
KASUMI-1 MnLFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml3DTWM2OD1yLkCyOFE{KM7:TR?= NYPQc3JUW0GQR1XS
NB7 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWrJR|UxRTBwMUO0N|kh|ryP NVy2eodrW0GQR1XS
BHT-101 NE[3W29Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHXS[WNKSzVyPUCuOlQzPjNizszN NULUXoI6W0GQR1XS
CGTH-W-1 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3S4TmlEPTB;MD62OFg4KM7:TR?= MnjhV2FPT0WU
HMV-II MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1XGTmlEPTB;MD63OFg4PCEQvF2= NWDGNVVTW0GQR1XS
NKM-1 NFfkSldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYTJR|UxRTBwOUCxOUDPxE1? M4CydHNCVkeHUh?=
LB2241-RCC NXPDd4JFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWnJR|UxRTFwMEKyNlgh|ryP M4DwbXNCVkeHUh?=
NCI-H1703 MlTrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIPndoRKSzVyPUGuNVg5PyEQvF2= NFvpOI9USU6JRWK=
BE-13 NVfMcmNUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mk\iTWM2OD1zLkK3OFE3KM7:TR?= MW\TRW5ITVJ?
ACN MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWXJR|UxRTFwNUWwO|ch|ryP NFrOU4dUSU6JRWK=
A204 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH31U3ZKSzVyPUGuOVczODVizszN MWPTRW5ITVJ?
HOP-62 NGnEdI5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVzJR|UxRTFwOEKwO|ch|ryP NFLqSppUSU6JRWK=
H9 MmTiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{HhTGlEPTB;Mj63N|c6OyEQvF2= M2fFeXNCVkeHUh?=
HCC1806 M2DLO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnK1TWM2OD1{Lke0N|I4KM7:TR?= MoC0V2FPT0WU
NOS-1 NVrLZZlFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYXJR|UxRTJwOEexNFIh|ryP MoLpV2FPT0WU
RS4-11 M{myOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mkm2TWM2OD1{LkmwOlI{KM7:TR?= MUTTRW5ITVJ?
JAR MonlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX3JR|UxRTJwOUKwPFQh|ryP NVzXc3BWW0GQR1XS
T98G MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NI\CdopKSzVyPUOuNFE{OTNizszN Mk\6V2FPT0WU
NCI-SNU-1 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVjSUYNoUUN3ME2zMlQxODl{IN88US=> MkDoV2FPT0WU
SK-MEL-1 NGjGcIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1O1[GlEPTB;Mz60N|AzQSEQvF2= NWe1dnkyW0GQR1XS
L-363 NYXrPXVLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnOzTWM2OD1|Lk[xNVA4KM7:TR?= NH\2W3NUSU6JRWK=
SW982 NX3tTJpLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3zuc2lEPTB;Mz62OFE3QSEQvF2= Mn3tV2FPT0WU
HT-1080 NGjERnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmriTWM2OD1|LkmxO|c2KM7:TR?= MVXTRW5ITVJ?
G-402 M2fadmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV\ucVZ7UUN3ME20MlMyOjB|IN88US=> Mo\SV2FPT0WU
HOS NXKxc3JtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX7JR|UxRTRwOECyPFIh|ryP M3LoOXNCVkeHUh?=
SK-NEP-1 NVzRSokyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnHsTWM2OD12LkizNVkyKM7:TR?= NXfSRYZ7W0GQR1XS
HAL-01 Mor0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXLVNGFZUUN3ME20Mlg5OjR{IN88US=> MYrTRW5ITVJ?
SBC-1 M4rwUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4PEdGlEPTB;ND65NFkxPyEQvF2= MoLvV2FPT0WU
CTV-1 NVS1T4NUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlXPTWM2OD13LkS4PVM5KM7:TR?= M124fnNCVkeHUh?=
LCLC-103H M1ruU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1KyWmlEPTB;NT63O|Q4OSEQvF2= NHHVTVFUSU6JRWK=
RVH-421 MmXOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVfJR|UxRTVwN{e1N|Yh|ryP NH74W|hUSU6JRWK=
K-562 MmfrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWrabW51UUN3ME21MlkxOzZizszN MWHTRW5ITVJ?
CAL-33 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWPIdXhkUUN3ME22MlMyOzV7IN88US=> M3PIcXNCVkeHUh?=
MDA-MB-361 NH3FTmdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVTJR|UxRTZwM{O2PVkh|ryP NEjoeVJUSU6JRWK=
IGROV-1 NG\VXIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWrJZYx1UUN3ME22MlQ4OTlzIN88US=> NULzPJQzW0GQR1XS
NY MoDGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUHJR|UxRTZwNUO1PVkh|ryP MWLTRW5ITVJ?
Ramos-2G6-4C10 MnHSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIDhR3VKSzVyPU[uOlY6OzFizszN M{TMcnNCVkeHUh?=
HuO9 NXHR[HBVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlSzTWM2OD14LkezPVY1KM7:TR?= MYXTRW5ITVJ?
MS-1 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXjJR|UxRTdwMUG5OVMh|ryP NVO0R4VWW0GQR1XS
RPMI-8226 M1;aUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX3JR|UxRTdwMkiyPFch|ryP NXvmUmg1W0GQR1XS
HDLM-2 NX[3NHJ{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVfiSJhGUUN3ME23MlQxOTR7IN88US=> M4\RenNCVkeHUh?=
D-566MG MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVz6SYdJUUN3ME23MlQ4OTV3IN88US=> NInPTJdUSU6JRWK=
SK-MEL-24 M4PDS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXnJR|UxRTdwNkOzPVIh|ryP NV;VfW57W0GQR1XS
COLO-679 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVPSbVZ7UUN3ME23Mlk5PjdzIN88US=> M3zWb3NCVkeHUh?=
EW-13 NH7hb|JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2HjfGlEPTB;OD6zNlA2PCEQvF2= MVPTRW5ITVJ?
A388 NIX5fXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmPDTWM2OD16LkO4OFgyKM7:TR?= M4DObXNCVkeHUh?=
UM-UC-3 NH3wfJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnnuTWM2OD16LkSzPVU3KM7:TR?= NV76VJpFW0GQR1XS
NUGC-3 NVPjSolHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mmi2TWM2OD16LkWzOVgzKM7:TR?= MUPTRW5ITVJ?
COLO-668 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVG3OmJwUUN3ME24MlU6PDlzIN88US=> NHHXW4VUSU6JRWK=
MOLT-4 Mlr4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{n2cmlEPTB;OD62NlM2OyEQvF2= NYnTd2YxW0GQR1XS
D-423MG MoDRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4jWNWlEPTB;OD64N|c2PiEQvF2= MW\TRW5ITVJ?
CTB-1 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1jwXWlEPTB;OD64O|EzQCEQvF2= NIfaRWtUSU6JRWK=
BCPAP MlHhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYPJR|UxRTlwMEK1OlIh|ryP NVzCZZp6W0GQR1XS
GCT MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX\JR|UxRTlwMEm4N|Eh|ryP NXHXWWdNW0GQR1XS
ACHN NUf1SIJ7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4H3eGlEPTB;OT6yN|Y{OiEQvF2= M2PDcnNCVkeHUh?=
KYSE-520 MljxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV\6RlNuUUN3ME25MlM{PDh{IN88US=> NVy2WHc3W0GQR1XS
LB771-HNC MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXTJR|UxRTlwN{[0PVch|ryP MkXaV2FPT0WU
MLMA NWnpcVZkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{\V[WlEPTB;MUCuNFE{OiEQvF2= MX;TRW5ITVJ?
HEC-1 MnznS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWjFdplKUUN3ME2xNE4zQDB2IN88US=> M4HRfnNCVkeHUh?=
HL-60 NH;1d2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M176bmlEPTB;MUCuOlg2OyEQvF2= MkjWV2FPT0WU
A101D NXv3e5g2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYHJR|UxRTFyLki5NlMh|ryP MnPVV2FPT0WU
A2058 NV\SemVYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGXBSG1KSzVyPUGwMlkzPDVizszN NUjHW4RvW0GQR1XS
KARPAS-45 NHmz[GtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml[xTWM2OD1zMT6wOlM2KM7:TR?= NXH2cZk6W0GQR1XS
697 NIi1OVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2TXb2lEPTB;MUGuNlExOSEQvF2= NFX2NFBUSU6JRWK=
NCI-N87 M1jZRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX:yU4RKUUN3ME2xNU44PzNzIN88US=> NYj5THE5W0GQR1XS
DSH1 MlfOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWPJR|UxRTFzLke5OVMh|ryP MUPTRW5ITVJ?
HLE MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUHJR|UxRTFzLki4N|kh|ryP M2DlRnNCVkeHUh?=
NCI-H720 NV\SV2RTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV7QR4g{UUN3ME2xNk43QDBzIN88US=> MmXqV2FPT0WU
EW-3 NX76cmx[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4PhSWlEPTB;MUKuPVMxPyEQvF2= NHqwXWlUSU6JRWK=
AGS NEDxOlFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYXJR|UxRTF|LkCzOVEh|ryP MYfTRW5ITVJ?
ES5 M1vsWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmexTWM2OD1zMz6wOVEzKM7:TR?= NWHDOWNRW0GQR1XS
DB M2Hldmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGDYO5hKSzVyPUGzMlMzPTZizszN NHniW3JUSU6JRWK=
A4-Fuk NF:1eGJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4C2XGlEPTB;MUOuOFExOiEQvF2= MlvlV2FPT0WU
A427 NVTacYg4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXHJR|UxRTF|LkS5O|Ih|ryP Mn71V2FPT0WU
MN-60 Mn\BS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHPyPHZKSzVyPUGzMlU5PDNizszN M3\aU3NCVkeHUh?=
HCC2218 NHPCe4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M12yRWlEPTB;MUOuOVg2PiEQvF2= NI\kblJUSU6JRWK=
MV-4-11 Mk[2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MojRTWM2OD1zMz64NVM4KM7:TR?= NELudlJUSU6JRWK=
GI-1 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIjSOGdKSzVyPUG0MlEyQDRizszN M1HGe3NCVkeHUh?=
JVM-3 MkTCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{LWeGlEPTB;MUSuNlY2PiEQvF2= M4\4TnNCVkeHUh?=
NCI-H2029 MoC0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYnCRY5iUUN3ME2xOE4zPzJ5IN88US=> Mm\sV2FPT0WU
TE-12 MnjiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGjCVYtKSzVyPUG0MlYxPDZizszN NGLzdHFUSU6JRWK=
WM-115 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHrlV45KSzVyPUG1MlU3QDNizszN Mnm2V2FPT0WU
BB65-RCC M1PyXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWHJR|UxRTF4LkCyOFEh|ryP NYXWRmhtW0GQR1XS
NCI-H1693 NETj[WxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXnJR|UxRTF4LkO4NFIh|ryP NWWzeZVyW0GQR1XS
KARPAS-299 NXzrc2NFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWLJR|UxRTF4Lk[yNFMh|ryP MUDTRW5ITVJ?
UACC-257 NFfCZlVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUi5[4dPUUN3ME2xO{4xPTh{IN88US=> M1T6bHNCVkeHUh?=
RKO NYTqbHY{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MonlTWM2OD1zNz62OFM{KM7:TR?= NEHmcGxUSU6JRWK=
HT-29 NH7GZ|ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3vFSmlEPTB;MUeuO|g5QSEQvF2= MVXTRW5ITVJ?
ES7 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{P3[WlEPTB;MUiuNVEzOiEQvF2= NHzpOpRUSU6JRWK=
DEL M{Wwbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHz2do5KSzVyPUG4MlMyPzJizszN MWDTRW5ITVJ?
BT-549 M2DydGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWjYS4NuUUN3ME2xPE41ODl{IN88US=> Ml\KV2FPT0WU
NCI-H1755 NGn0c5pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXPROm9CUUN3ME2xPE42PzJ|IN88US=> NGHxWnVUSU6JRWK=
HCE-T Mn;VS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1m3WGlEPTB;MUiuPFM1OSEQvF2= NXfydnpMW0GQR1XS
LU-139 MoTXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYHjcppuUUN3ME2xPU4xPDV6IN88US=> NXfJbmRFW0GQR1XS
ECC10 NFvwOolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFjRV|ZKSzVyPUG5MlI1PzVizszN NHG4bINUSU6JRWK=
769-P NWHUUVFmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYDJR|UxRTF7Lk[zN|Uh|ryP NUCyVVZVW0GQR1XS
BALL-1 MoDGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIHLPHdKSzVyPUG5MlY4PzVizszN NXiw[oY3W0GQR1XS
LXF-289 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkD2TWM2OD1zOT64PVc6KM7:TR?= NGDpW|lUSU6JRWK=
TYK-nu NFjtPGxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV7JR|UxRTF7LkmzNVUh|ryP MYXTRW5ITVJ?
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EW-18 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MULJR|UxRTJyLkO4NFIh|ryP MXTTRW5ITVJ?
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... Click to View More Cell Line Experimental Data

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]

Protocol

Cell Research:[4]
+ Expand
  • 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.
    (Only for Reference)
Animal Research:[6]
+ Expand
  • 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
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 27 mg/mL (50.98 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
4% DMSO+30% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.
3mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 529.52
Formula

C28H22F3N7O

CAS No. 641571-10-0
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03885830 Not yet recruiting CML Chronic Phase|CML (Chronic Myelogenous Leukemia|CML - Philadelphia Chromosome|Chronic Myeloid Leukemia|Chronic Myeloid Leukemia Chronic Phase UNC Lineberger Comprehensive Cancer Center May 2019 --
NCT03885830 Not yet recruiting CML Chronic Phase|CML (Chronic Myelogenous Leukemia|CML - Philadelphia Chromosome|Chronic Myeloid Leukemia|Chronic Myeloid Leukemia Chronic Phase UNC Lineberger Comprehensive Cancer Center May 2019 --
NCT03874858 Not yet recruiting Chronic Myeloid Leukemia Novartis Pharmaceuticals|Novartis April 1 2019 Phase 2
NCT03874858 Not yet recruiting Chronic Myeloid Leukemia Novartis Pharmaceuticals|Novartis April 1 2019 Phase 2
NCT03784014 Not yet recruiting Soft Tissue Sarcoma Institut National de la Santé Et de la Recherche Médicale France|Commissariat A L''energie Atomique|Institut Bergonié|Plateforme labellisée Inca – Institut Bergonié Bordeaux|Plateforme labellisée Inca – Hôpital Européen Georges Pompidou Paris|CIC-EC 1401/EUCLID March 2019 Phase 3
NCT03784014 Not yet recruiting Soft Tissue Sarcoma Institut National de la Santé Et de la Recherche Médicale France|Commissariat A L''energie Atomique|Institut Bergonié|Plateforme labellisée Inca – Institut Bergonié Bordeaux|Plateforme labellisée Inca – Hôpital Européen Georges Pompidou Paris|CIC-EC 1401/EUCLID March 2019 Phase 3

Tech Support

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

Tel: +1-832-582-8158 Ext:3

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Frequently Asked Questions

  • Question 1:

    I would like to use AMN-107 for in vivo studies in mice, can you give me some suggestions about the in vivo formulation?

  • Answer:

    For in vivo study, we recommend to use 4% DMSO+30% PEG 300+5% Tween 80+ddH2O up to 3mg/ml.

Bcr-Abl Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID