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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In DMSO USD 91 In stock
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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 NUfpNmg6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmLHTWM2OD1yLkCwNFE1PCEQvF2= NFPoZ4JUSU6JRWK=
KU812 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkfKTWM2OD1yLkCwNlQ5KM7:TR?= M2n6cnNCVkeHUh?=
EM-2 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGLVNGNKSzVyPUCuNFA1OSEQvF2= NHzi[IFUSU6JRWK=
LAMA-84 NVW5ZWxCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NISzbYNKSzVyPUCuNFA1QSEQvF2= MoD3V2FPT0WU
MEG-01 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn3YTWM2OD1yLkCwPFI5KM7:TR?= NYHnRWZ5W0GQR1XS
BV-173 NUTNTlMxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmLETWM2OD1yLkCxNFg6KM7:TR?= MnLsV2FPT0WU
KASUMI-1 MkDUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIHBXWlKSzVyPUCuNFI1OTNizszN MkjEV2FPT0WU
NB7 NXPDOog2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MonMTWM2OD1yLkGzOFM6KM7:TR?= NGDJ[GVUSU6JRWK=
BHT-101 MlTkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHXoe4hKSzVyPUCuOlQzPjNizszN MXTTRW5ITVJ?
CGTH-W-1 M4LUU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmTyTWM2OD1yLk[0PFch|ryP MoC0V2FPT0WU
HMV-II M1\lb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWLMT2NQUUN3ME2wMlc1QDd2IN88US=> M134bnNCVkeHUh?=
NKM-1 NY\zd4RPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH7LTIlKSzVyPUCuPVAyPSEQvF2= MmPRV2FPT0WU
LB2241-RCC MmfxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWnJR|UxRTFwMEKyNlgh|ryP MX\TRW5ITVJ?
NCI-H1703 NGTheHhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mli5TWM2OD1zLkG4PFch|ryP NEfLemhUSU6JRWK=
BE-13 MmnpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2LEUmlEPTB;MT6yO|QyPiEQvF2= MmHuV2FPT0WU
ACN MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NITHNYdKSzVyPUGuOVUxPzdizszN M2nvPXNCVkeHUh?=
A204 NFP1ZlBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGXsZ41KSzVyPUGuOVczODVizszN M2\mbHNCVkeHUh?=
HOP-62 M1XOe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmHKTWM2OD1zLkiyNFc4KM7:TR?= NVjG[JhrW0GQR1XS
H9 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NETxSXZKSzVyPUKuO|M4QTNizszN MnrNV2FPT0WU
HCC1806 NV;uUG54T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWPJR|UxRTJwN{SzNlch|ryP NVq0fYw5W0GQR1XS
NOS-1 NInaZndIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVjwPYdIUUN3ME2yMlg4OTB{IN88US=> NXToZXQyW0GQR1XS
RS4-11 NXu1O4p3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXXJR|UxRTJwOUC2NlMh|ryP M2TSbHNCVkeHUh?=
JAR NVXwWHhbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYPJR|UxRTJwOUKwPFQh|ryP NVPT[5c4W0GQR1XS
T98G MnLkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH32c2lKSzVyPUOuNFE{OTNizszN MVXTRW5ITVJ?
NCI-SNU-1 NILwNoRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEnyS4hKSzVyPUOuOFAxQTJizszN NWHBd3NWW0GQR1XS
SK-MEL-1 MmHKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmXGTWM2OD1|LkSzNFI6KM7:TR?= Mn;OV2FPT0WU
L-363 MnzVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1;oS2lEPTB;Mz62NVExPyEQvF2= Ml7BV2FPT0WU
SW982 MmL0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mln6TWM2OD1|Lk[0NVY6KM7:TR?= Mn;JV2FPT0WU
HT-1080 MmHxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3Lve2lEPTB;Mz65NVc4PSEQvF2= NXO4WFcxW0GQR1XS
G-402 NFHGPJJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUjSSFdEUUN3ME20MlMyOjB|IN88US=> NITxWo1USU6JRWK=
HOS MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWDGeWlXUUN3ME20MlgxOjh{IN88US=> NFHyeHZUSU6JRWK=
SK-NEP-1 MoqwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYHiNZdoUUN3ME20Mlg{OTlzIN88US=> MmmwV2FPT0WU
HAL-01 MkTpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3W1ZWlEPTB;ND64PFI1OiEQvF2= M3:3TXNCVkeHUh?=
SBC-1 M2rWcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn:yTWM2OD12LkmwPVA4KM7:TR?= MXXTRW5ITVJ?
CTV-1 NVTJcpFXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn3kTWM2OD13LkS4PVM5KM7:TR?= MmKzV2FPT0WU
LCLC-103H NWT1[ZpIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWPJR|UxRTVwN{e0O|Eh|ryP NEjsWHBUSU6JRWK=
RVH-421 NEXIcm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWDqdXdxUUN3ME21Mlc4PTN4IN88US=> M2iye3NCVkeHUh?=
K-562 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlW2TWM2OD13LkmwN|Yh|ryP NUjje3hvW0GQR1XS
CAL-33 MlPMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnT0TWM2OD14LkOxN|U6KM7:TR?= NYrNSIV4W0GQR1XS
MDA-MB-361 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3T3W2lEPTB;Nj6zN|Y6QSEQvF2= M4nrRXNCVkeHUh?=
IGROV-1 NV;PfpF4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUPJR|UxRTZwNEexPVEh|ryP NYLRWpZSW0GQR1XS
NY NVvNUIFGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NE\oUohKSzVyPU[uOVM2QTlizszN MljUV2FPT0WU
Ramos-2G6-4C10 NY\NcmlCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHLZdYFKSzVyPU[uOlY6OzFizszN MXfTRW5ITVJ?
HuO9 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIjq[VRKSzVyPU[uO|M6PjRizszN MmOzV2FPT0WU
MS-1 NVS4b2s5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{LaeGlEPTB;Nz6xNVk2OyEQvF2= NYP1Z|Y6W0GQR1XS
RPMI-8226 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUnpbFNsUUN3ME23MlI5Ojh5IN88US=> NV\wZ|RGW0GQR1XS
HDLM-2 NXroNpZGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEL3RW9KSzVyPUeuOFAyPDlizszN MVTTRW5ITVJ?
D-566MG MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2jW[2lEPTB;Nz60O|E2PSEQvF2= NV\MSnh5W0GQR1XS
SK-MEL-24 M2raO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUTJR|UxRTdwNkOzPVIh|ryP NVjVSotDW0GQR1XS
COLO-679 MmjUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml21TWM2OD15Lkm4OlcyKM7:TR?= NFnBcmpUSU6JRWK=
EW-13 M3ToPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3fsc2lEPTB;OD6zNlA2PCEQvF2= NEHFbXFUSU6JRWK=
A388 Mn75S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEPRNmxKSzVyPUiuN|g1QDFizszN MY\TRW5ITVJ?
UM-UC-3 NIPSPVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXro[VVMUUN3ME24MlQ{QTV4IN88US=> NHfjO|lUSU6JRWK=
NUGC-3 NFLlUY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXTJR|UxRThwNUO1PFIh|ryP MUjTRW5ITVJ?
COLO-668 NIjtS2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVrJR|UxRThwNUm0PVEh|ryP NXjMS3Q{W0GQR1XS
MOLT-4 NV;4V4tGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVrvPWlDUUN3ME24MlYzOzV|IN88US=> NHi5SnZUSU6JRWK=
D-423MG NIDoUHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4riV2lEPTB;OD64N|c2PiEQvF2= MlLYV2FPT0WU
CTB-1 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVPJR|UxRThwOEexNlgh|ryP M4X4[nNCVkeHUh?=
BCPAP MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV21XVlGUUN3ME25MlAzPTZ{IN88US=> M1HScnNCVkeHUh?=
GCT Mlz5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NI\ZdpJKSzVyPUmuNFk5OzFizszN M3XjR3NCVkeHUh?=
ACHN MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXHJR|UxRTlwMkO2N|Ih|ryP NIfldZlUSU6JRWK=
KYSE-520 NGDzRXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUXJR|UxRTlwM{O0PFIh|ryP MojiV2FPT0WU
LB771-HNC NGnwN3lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlLQTWM2OD17Lke2OFk4KM7:TR?= M3LyNXNCVkeHUh?=
MLMA MmLkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M37tdWlEPTB;MUCuNFE{OiEQvF2= M2DQcHNCVkeHUh?=
HEC-1 MkC1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH3KcVlKSzVyPUGwMlI5ODRizszN MVfTRW5ITVJ?
HL-60 M1H5OWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4fNS2lEPTB;MUCuOlg2OyEQvF2= MYDTRW5ITVJ?
A101D Mnj5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{XsOmlEPTB;MUCuPFkzOyEQvF2= M4L1V3NCVkeHUh?=
A2058 M4\Sdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUjJR|UxRTFyLkmyOFUh|ryP NI\xdZlUSU6JRWK=
KARPAS-45 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF\FWZJKSzVyPUGxMlA3OzVizszN MYHTRW5ITVJ?
697 M2W5UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmO1TWM2OD1zMT6yNVAyKM7:TR?= M4\1RnNCVkeHUh?=
NCI-N87 Mn\2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2flOWlEPTB;MUGuO|c{OSEQvF2= MW\TRW5ITVJ?
DSH1 MknqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkXQTWM2OD1zMT63PVU{KM7:TR?= NIfVWYxUSU6JRWK=
HLE MnrQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MonsTWM2OD1zMT64PFM6KM7:TR?= NFvZcnlUSU6JRWK=
NCI-H720 MmjYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{XVbGlEPTB;MUKuOlgxOSEQvF2= NXTLPIJNW0GQR1XS
EW-3 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnPjTWM2OD1zMj65N|A4KM7:TR?= Ml3UV2FPT0WU
AGS MoLPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVLJR|UxRTF|LkCzOVEh|ryP NUe4W3FWW0GQR1XS
ES5 M1TNcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mm[4TWM2OD1zMz6wOVEzKM7:TR?= MY\TRW5ITVJ?
DB MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVq4VGNOUUN3ME2xN{4{OjV4IN88US=> M4Pnc3NCVkeHUh?=
A4-Fuk NWW3c|NbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV3pb5R{UUN3ME2xN{41OTB{IN88US=> MYHTRW5ITVJ?
A427 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEfFSFZKSzVyPUGzMlQ6PzJizszN MYfTRW5ITVJ?
MN-60 M{PBdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkHqTWM2OD1zMz61PFQ{KM7:TR?= Mlm5V2FPT0WU
HCC2218 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnX4TWM2OD1zMz61PFU3KM7:TR?= NEK3VXdUSU6JRWK=
MV-4-11 NGeybYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{e4e2lEPTB;MUOuPFE{PyEQvF2= M4LsOnNCVkeHUh?=
GI-1 MonHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NY\sPVRHUUN3ME2xOE4yOTh2IN88US=> MWTTRW5ITVJ?
JVM-3 MoixS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH[0U|FKSzVyPUG0MlI3PTZizszN MkO4V2FPT0WU
NCI-H2029 M4W5dGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmXlTWM2OD1zND6yO|I4KM7:TR?= MXPTRW5ITVJ?
TE-12 NH7ENIFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M37qVWlEPTB;MUSuOlA1PiEQvF2= MUDTRW5ITVJ?
WM-115 NWK1S2hZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUPS[W5vUUN3ME2xOU42Pjh|IN88US=> M17adXNCVkeHUh?=
BB65-RCC MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFHS[|JKSzVyPUG2MlAzPDFizszN M2j1T3NCVkeHUh?=
NCI-H1693 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1TuXWlEPTB;MU[uN|gxOiEQvF2= MWTTRW5ITVJ?
KARPAS-299 NFvyelVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEjZboxKSzVyPUG2MlYzODNizszN MUHTRW5ITVJ?
UACC-257 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUPJR|UxRTF5LkC1PFIh|ryP M4[xbXNCVkeHUh?=
RKO NH\vW4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkLBTWM2OD1zNz62OFM{KM7:TR?= NXfNfYc5W0GQR1XS
HT-29 NFPoeZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYTLOZlLUUN3ME2xO{44QDh7IN88US=> M{e1fHNCVkeHUh?=
ES7 M2H0b2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4izRWlEPTB;MUiuNVEzOiEQvF2= M1q0R3NCVkeHUh?=
DEL MkjTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3P3UmlEPTB;MUiuN|E4OiEQvF2= MV;TRW5ITVJ?
BT-549 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mmj2TWM2OD1zOD60NFkzKM7:TR?= Mm\ZV2FPT0WU
NCI-H1755 NVe0RlByT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEPzS5hKSzVyPUG4MlU4OjNizszN MnXlV2FPT0WU
HCE-T NVXDd|lCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXjJR|UxRTF6LkizOFEh|ryP MVLTRW5ITVJ?
LU-139 MlvHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHW3T3ZKSzVyPUG5MlA1PThizszN MYjTRW5ITVJ?
ECC10 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGfWcHJKSzVyPUG5MlI1PzVizszN NG\ibVhUSU6JRWK=
769-P MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV;JR|UxRTF7Lk[zN|Uh|ryP MX7TRW5ITVJ?
BALL-1 NHLZPVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXfHV3V2UUN3ME2xPU43Pzd3IN88US=> M2XlfnNCVkeHUh?=
LXF-289 M4LIZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXXJR|UxRTF7Lki5O|kh|ryP MlvUV2FPT0WU
TYK-nu MorMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF;seJVKSzVyPUG5Mlk{OTVizszN NHvkfWhUSU6JRWK=
NCI-H630 M2[5S2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHLKPIhKSzVyPUG5Mlk{PzhizszN MlXqV2FPT0WU
EW-18 M3T2Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWC4cGFlUUN3ME2yNE4{QDB{IN88US=> Mlq3V2FPT0WU
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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:
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
Synonyms N/A

Bio Calculators

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Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02973711 Not yet recruiting Leukemia, Chronic Myeloid University of Michigan Cancer Center February 2017 Phase 1|Phase 2
NCT02954978 Recruiting Parkinson Disease|Parkinsons Disease With Dementia Georgetown University January 2017 Phase 2
NCT02947893 Recruiting Alzheimers Disease Georgetown University January 2017 Phase 2
NCT02602314 Not yet recruiting Chronyc Myeloid Leukemia Gruppo Italiano Malattie EMatologiche dellAdulto December 2016 Phase 4
NCT02709083 Recruiting Chronic Myelogenous Leukemia|Chronic Myeloid Leukemia|Leukemia Emory University October 2016 Phase 2
NCT02917720 Not yet recruiting Chronic Myeloid Leukemia European LeukemiaNet|Heidelberg University|Ludwig-Maximilians - University of Munich October 2016 Phase 2

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

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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