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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  • 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 M1zVeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M175VmlEPTB;MD6wNFAyPDRizszN MWHTRW5ITVJ?
KU812 M1XSZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NE\Se|lKSzVyPUCuNFAzPDhizszN M{\zb3NCVkeHUh?=
EM-2 M{jlc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUnJR|UxRTBwMEC0NUDPxE1? M2ezVnNCVkeHUh?=
LAMA-84 MoG2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlvzTWM2OD1yLkCwOFkh|ryP MWXTRW5ITVJ?
MEG-01 M1X2d2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVrES3BNUUN3ME2wMlAxQDJ6IN88US=> MojOV2FPT0WU
BV-173 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH3HN3hKSzVyPUCuNFExQDlizszN M4jlRnNCVkeHUh?=
KASUMI-1 Mn72S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{mxPWlEPTB;MD6wNlQyOyEQvF2= MVfTRW5ITVJ?
NB7 NWT3SnpET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M33wWGlEPTB;MD6xN|Q{QSEQvF2= M33LeXNCVkeHUh?=
BHT-101 M2i4bGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVnJR|UxRTBwNkSyOlMh|ryP NHK2[2hUSU6JRWK=
CGTH-W-1 M2LldGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVzBUohVUUN3ME2wMlY1QDdizszN NUnNNXN[W0GQR1XS
HMV-II M2q2b2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV\JR|UxRTBwN{S4O|Qh|ryP M3;VU3NCVkeHUh?=
NKM-1 M3jxUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEPENo5KSzVyPUCuPVAyPSEQvF2= NVHFVIc3W0GQR1XS
LB2241-RCC NWDPXI1ET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmDsTWM2OD1zLkCyNlI5KM7:TR?= MYLTRW5ITVJ?
NCI-H1703 MkPBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlLPTWM2OD1zLkG4PFch|ryP MmLEV2FPT0WU
BE-13 NVG1T|JLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmmzTWM2OD1zLkK3OFE3KM7:TR?= NUDEN45jW0GQR1XS
ACN NGLjPJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3PsdWlEPTB;MT61OVA4PyEQvF2= MomwV2FPT0WU
A204 NEDaZWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mlj0TWM2OD1zLkW3NlA2KM7:TR?= MmPxV2FPT0WU
HOP-62 NYLuTZJYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2HkdGlEPTB;MT64NlA4PyEQvF2= Mn\hV2FPT0WU
H9 MoG1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEXlXZBKSzVyPUKuO|M4QTNizszN NEm4XYNUSU6JRWK=
HCC1806 NV;POWdLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV\JR|UxRTJwN{SzNlch|ryP M2HFdnNCVkeHUh?=
NOS-1 MknvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIrSRWRKSzVyPUKuPFcyODJizszN MYXTRW5ITVJ?
RS4-11 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIHnSIJKSzVyPUKuPVA3OjNizszN MYLTRW5ITVJ?
JAR NXnCWpFJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoXwTWM2OD1{LkmyNFg1KM7:TR?= NWTtfFhSW0GQR1XS
T98G M2rOPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmrGTWM2OD1|LkCxN|E{KM7:TR?= M4HxR3NCVkeHUh?=
NCI-SNU-1 NVXrSVdWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4HPPGlEPTB;Mz60NFA6OiEQvF2= MUfTRW5ITVJ?
SK-MEL-1 MlPiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmrCTWM2OD1|LkSzNFI6KM7:TR?= Mn\rV2FPT0WU
L-363 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFzY[I5KSzVyPUOuOlEyODdizszN M3nNVnNCVkeHUh?=
SW982 NGHJOHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2PrVWlEPTB;Mz62OFE3QSEQvF2= MWPTRW5ITVJ?
HT-1080 M3i2eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYTo[JdmUUN3ME2zMlkyPzd3IN88US=> NFPh[2lUSU6JRWK=
G-402 M4G2OGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYHJR|UxRTRwM{GyNFMh|ryP NHnBcYlUSU6JRWK=
HOS NGS1VVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MknKTWM2OD12LkiwNlgzKM7:TR?= M2nQfXNCVkeHUh?=
SK-NEP-1 M3[0TGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M37IcGlEPTB;ND64N|E6OSEQvF2= NGWzTmdUSU6JRWK=
HAL-01 M3vvbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWHzUHZ1UUN3ME20Mlg5OjR{IN88US=> MUfTRW5ITVJ?
SBC-1 MkX2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnX3TWM2OD12LkmwPVA4KM7:TR?= MXnTRW5ITVJ?
CTV-1 MkLUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoLSTWM2OD13LkS4PVM5KM7:TR?= NUi4PFZlW0GQR1XS
LCLC-103H NIi3N3FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVPJR|UxRTVwN{e0O|Eh|ryP NEf5NG1USU6JRWK=
RVH-421 NIrRcI5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXvJR|UxRTVwN{e1N|Yh|ryP NWC2XlU1W0GQR1XS
K-562 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2\1TWlEPTB;NT65NFM3KM7:TR?= M2qyTXNCVkeHUh?=
CAL-33 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFH6OmlKSzVyPU[uN|E{PTlizszN NHrYOHdUSU6JRWK=
MDA-MB-361 NHHibJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MljoTWM2OD14LkOzOlk6KM7:TR?= NFjKepJUSU6JRWK=
IGROV-1 MnrFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mny4TWM2OD14LkS3NVkyKM7:TR?= NEnBW4dUSU6JRWK=
NY NHrDRmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NY\teVVNUUN3ME22MlU{PTl7IN88US=> NG\aTIpUSU6JRWK=
Ramos-2G6-4C10 NEf3S2RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIX6Wm9KSzVyPU[uOlY6OzFizszN NFH1SpNUSU6JRWK=
HuO9 NWS1NXNDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{HJTWlEPTB;Nj63N|k3PCEQvF2= MW\TRW5ITVJ?
MS-1 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWnJR|UxRTdwMUG5OVMh|ryP MYTTRW5ITVJ?
RPMI-8226 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmKxTWM2OD15LkK4Nlg4KM7:TR?= NUiyOHNCW0GQR1XS
HDLM-2 NVrGUpZOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVrpSGd[UUN3ME23MlQxOTR7IN88US=> MYHTRW5ITVJ?
D-566MG NWqye|ZqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnvPTWM2OD15LkS3NVU2KM7:TR?= MWrTRW5ITVJ?
SK-MEL-24 NYT1NmFNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1SzTmlEPTB;Nz62N|M6OiEQvF2= Mm\OV2FPT0WU
COLO-679 NFTKNoRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVL5UFZmUUN3ME23Mlk5PjdzIN88US=> M1XL[3NCVkeHUh?=
EW-13 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXnJR|UxRThwM{KwOVQh|ryP MlL4V2FPT0WU
A388 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUX1N2s5UUN3ME24MlM5PDhzIN88US=> MU\TRW5ITVJ?
UM-UC-3 M2K0Zmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH:3cnJKSzVyPUiuOFM6PTZizszN MljzV2FPT0WU
NUGC-3 M3vxW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NU\QZlNKUUN3ME24MlU{PTh{IN88US=> M{PWVXNCVkeHUh?=
COLO-668 M4OzNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH\VfZBKSzVyPUiuOVk1QTFizszN NHK5fnFUSU6JRWK=
MOLT-4 Mn2wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWfnUHVUUUN3ME24MlYzOzV|IN88US=> M3LsZnNCVkeHUh?=
D-423MG MlO0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4KxbmlEPTB;OD64N|c2PiEQvF2= Mm\xV2FPT0WU
CTB-1 M1vIOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{HUOWlEPTB;OD64O|EzQCEQvF2= MXLTRW5ITVJ?
BCPAP MnTiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVHOe4JLUUN3ME25MlAzPTZ{IN88US=> M{LH[XNCVkeHUh?=
GCT M1Lnb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NInNeHRKSzVyPUmuNFk5OzFizszN M2fwS3NCVkeHUh?=
ACHN MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnrNTWM2OD17LkKzOlMzKM7:TR?= M1S5dHNCVkeHUh?=
KYSE-520 NGrVOYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIjWWYFKSzVyPUmuN|M1QDJizszN M2fwfnNCVkeHUh?=
LB771-HNC MlXRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXzJR|UxRTlwN{[0PVch|ryP NE\NbYJUSU6JRWK=
MLMA NVm4UpY5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVTJR|UxRTFyLkCxN|Ih|ryP M4rrOnNCVkeHUh?=
HEC-1 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXfJR|UxRTFyLkK4NFQh|ryP M1H1bHNCVkeHUh?=
HL-60 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF\vN2NKSzVyPUGwMlY5PTNizszN NVGzUYRCW0GQR1XS
A101D MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmDETWM2OD1zMD64PVI{KM7:TR?= NF;WcGFUSU6JRWK=
A2058 NWrGS2RyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlfhTWM2OD1zMD65NlQ2KM7:TR?= NYnMeZZYW0GQR1XS
KARPAS-45 MmfIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4DUTGlEPTB;MUGuNFY{PSEQvF2= MnvuV2FPT0WU
697 Mn\PS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3XFTWlEPTB;MUGuNlExOSEQvF2= MmDiV2FPT0WU
NCI-N87 M1\zOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{X1cGlEPTB;MUGuO|c{OSEQvF2= M4DPe3NCVkeHUh?=
DSH1 M1z4V2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NELUfWFKSzVyPUGxMlc6PTNizszN NX\pUI1YW0GQR1XS
HLE MljuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3HTOWlEPTB;MUGuPFg{QSEQvF2= M1OzU3NCVkeHUh?=
NCI-H720 NYDoNlI{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnfoTWM2OD1zMj62PFAyKM7:TR?= NV\RT3JGW0GQR1XS
EW-3 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{[yTGlEPTB;MUKuPVMxPyEQvF2= M2\6OHNCVkeHUh?=
AGS M4HtOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWLJR|UxRTF|LkCzOVEh|ryP NHfEVWlUSU6JRWK=
ES5 MmTaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4HEOGlEPTB;MUOuNFUyOiEQvF2= NUTReoVwW0GQR1XS
DB NET3XYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXzOcHJ2UUN3ME2xN{4{OjV4IN88US=> NWm0dnlrW0GQR1XS
A4-Fuk NFLQ[3FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{XPdWlEPTB;MUOuOFExOiEQvF2= NFvxNmhUSU6JRWK=
A427 NUP4R2pGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MknHTWM2OD1zMz60PVczKM7:TR?= Mme5V2FPT0WU
MN-60 NHriW25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3\DWmlEPTB;MUOuOVg1OyEQvF2= MUjTRW5ITVJ?
HCC2218 NF;PWHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkLHTWM2OD1zMz61PFU3KM7:TR?= NF;EUGFUSU6JRWK=
MV-4-11 NE\NT|RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mk\JTWM2OD1zMz64NVM4KM7:TR?= NYTFb5hlW0GQR1XS
GI-1 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MleyTWM2OD1zND6xNVg1KM7:TR?= MWTTRW5ITVJ?
JVM-3 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV;iPFQyUUN3ME2xOE4zPjV4IN88US=> MUnTRW5ITVJ?
NCI-H2029 M4XvUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHfBZ2pKSzVyPUG0MlI4OjdizszN NEH6O49USU6JRWK=
TE-12 NV;zS4hKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXHJR|UxRTF2Lk[wOFYh|ryP NHHPdnVUSU6JRWK=
WM-115 NUnocJR2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUXOdI57UUN3ME2xOU42Pjh|IN88US=> NWTo[GJ7W0GQR1XS
BB65-RCC NWrifG1HT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWq2Ums6UUN3ME2xOk4xOjRzIN88US=> MYjTRW5ITVJ?
NCI-H1693 MmHRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2DtNWlEPTB;MU[uN|gxOiEQvF2= NVHOXHNNW0GQR1XS
KARPAS-299 NVv4No9oT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1vwZ2lEPTB;MU[uOlIxOyEQvF2= M1vaXHNCVkeHUh?=
UACC-257 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlzZTWM2OD1zNz6wOVgzKM7:TR?= NInlUYtUSU6JRWK=
RKO Mm[0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4HWb2lEPTB;MUeuOlQ{OyEQvF2= M{LIdXNCVkeHUh?=
HT-29 M4m3O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mnf1TWM2OD1zNz63PFg6KM7:TR?= MYLTRW5ITVJ?
ES7 NUTweGRtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUnxdmU1UUN3ME2xPE4yOTJ{IN88US=> NVnHS3pIW0GQR1XS
DEL MonIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NELI[VdKSzVyPUG4MlMyPzJizszN M{XKSHNCVkeHUh?=
BT-549 M{XXXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFj2O2ZKSzVyPUG4MlQxQTJizszN M2HIeHNCVkeHUh?=
NCI-H1755 NISwXJVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHXF[IFKSzVyPUG4MlU4OjNizszN M2nQe3NCVkeHUh?=
HCE-T NHLhWlNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mk\GTWM2OD1zOD64N|QyKM7:TR?= MYPTRW5ITVJ?
LU-139 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHPPZo9KSzVyPUG5MlA1PThizszN M2PiRXNCVkeHUh?=
ECC10 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M131OmlEPTB;MUmuNlQ4PSEQvF2= MVrTRW5ITVJ?
769-P MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIXRW2JKSzVyPUG5MlY{OzVizszN NEfhOnpUSU6JRWK=
BALL-1 NFfiRlVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWPJR|UxRTF7Lk[3O|Uh|ryP Ml;rV2FPT0WU
LXF-289 Mn;5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MofsTWM2OD1zOT64PVc6KM7:TR?= Mo\xV2FPT0WU
TYK-nu NWDhb3l3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYjJR|UxRTF7LkmzNVUh|ryP MYPTRW5ITVJ?
NCI-H630 NWP4UVN{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWrDRXg4UUN3ME2xPU46Ozd6IN88US=> MYPTRW5ITVJ?
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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
NCT02108951 Terminated Philidelphia Positive Chronic Myeloid Leukaemia Novartis Pharmaceuticals|Novartis July 7 2014 Phase 3
NCT03332511 Completed Chronic Myeloid Leukemia Chronic Phase Seoul National University Hospital|Novartis Pharmaceuticals May 6 2013 Phase 4
NCT02627677 Active not recruiting Chronic Phase Chronic Myeloid Leukemia Ariad Pharmaceuticals|Takeda December 31 2015 Phase 3
NCT00471497 Active not recruiting Myelogenous Leukemia Chronic Novartis Pharmaceuticals|Novartis July 31 2007 Phase 3
NCT03079505 Recruiting Chronic Myeloid Leukemia - Chronic Phase Hamad Medical Corporation August 3 2017 Phase 3
NCT01735955 Recruiting GIST and CML Novartis Pharmaceuticals|Novartis March 29 2013 Phase 4

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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID