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 NWDoUJRvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml3ITWM2OD1yLkCwNFE1PCEQvF2= NFqwclhUSU6JRWK=
KU812 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWPJXJZxUUN3ME2wMlAxOjR6IN88US=> NFXtVINUSU6JRWK=
EM-2 M2O0OWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1r5UmlEPTB;MD6wNFQyKM7:TR?= M1\uRXNCVkeHUh?=
LAMA-84 M1T2cWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXfJR|UxRTBwMEC0PUDPxE1? MkL1V2FPT0WU
MEG-01 Mo\0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVnkOJZiUUN3ME2wMlAxQDJ6IN88US=> NV62d3d3W0GQR1XS
BV-173 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlrHTWM2OD1yLkCxNFg6KM7:TR?= MUDTRW5ITVJ?
KASUMI-1 M2HpXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF\yNXdKSzVyPUCuNFI1OTNizszN NES5e2xUSU6JRWK=
NB7 MmSyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MonnTWM2OD1yLkGzOFM6KM7:TR?= NXfGO4tRW0GQR1XS
BHT-101 MlzpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3zRXmlEPTB;MD62OFI3OyEQvF2= M1u1cnNCVkeHUh?=
CGTH-W-1 NGPtWXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2TERWlEPTB;MD62OFg4KM7:TR?= M1G4W3NCVkeHUh?=
HMV-II M2ry[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIrXfXlKSzVyPUCuO|Q5PzRizszN MXjTRW5ITVJ?
NKM-1 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGfSW5hKSzVyPUCuPVAyPSEQvF2= MmPpV2FPT0WU
LB2241-RCC MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4XIdWlEPTB;MT6wNlIzQCEQvF2= NGL2RXBUSU6JRWK=
NCI-H1703 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWXJR|UxRTFwMUi4O{DPxE1? NFqzOZFUSU6JRWK=
BE-13 NGDtNXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3j0OmlEPTB;MT6yO|QyPiEQvF2= Mlz4V2FPT0WU
ACN M1TqNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIjCXphKSzVyPUGuOVUxPzdizszN MoDnV2FPT0WU
A204 NYTjOnpOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2Dm[WlEPTB;MT61O|IxPSEQvF2= M{LxRnNCVkeHUh?=
HOP-62 MnTlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2XKcWlEPTB;MT64NlA4PyEQvF2= NYjVVJF4W0GQR1XS
H9 NGLyS3BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWLqRVFYUUN3ME2yMlc{Pzl|IN88US=> NWHkNmFSW0GQR1XS
HCC1806 NGnrR5pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4qxT2lEPTB;Mj63OFMzPyEQvF2= NHHGeG1USU6JRWK=
NOS-1 NGPHeYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1fYPWlEPTB;Mj64O|ExOiEQvF2= MVzTRW5ITVJ?
RS4-11 MnL3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXrJR|UxRTJwOUC2NlMh|ryP MkjLV2FPT0WU
JAR NHLKN5JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEXaOJJKSzVyPUKuPVIxQDRizszN NYXqcWpEW0GQR1XS
T98G NVjwcYhST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVPJR|UxRTNwMEGzNVMh|ryP MVfTRW5ITVJ?
NCI-SNU-1 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVXJR|UxRTNwNECwPVIh|ryP MmHiV2FPT0WU
SK-MEL-1 M13u[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3;NSWlEPTB;Mz60N|AzQSEQvF2= NH7NcG9USU6JRWK=
L-363 NFLlRlJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUTqbWY3UUN3ME2zMlYyOTB5IN88US=> NVvGOXBpW0GQR1XS
SW982 M3;USGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV\6SmZvUUN3ME2zMlY1OTZ7IN88US=> NXm5dopVW0GQR1XS
HT-1080 NYLTO4N2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml3JTWM2OD1|LkmxO|c2KM7:TR?= NVrWVms6W0GQR1XS
G-402 NVq1TY5OT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWXJR|UxRTRwM{GyNFMh|ryP M2nPTnNCVkeHUh?=
HOS M4HLOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlrhTWM2OD12LkiwNlgzKM7:TR?= NE\HR3ZUSU6JRWK=
SK-NEP-1 NXX2bmp[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWrEZ4I2UUN3ME20Mlg{OTlzIN88US=> MXTTRW5ITVJ?
HAL-01 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2nV[GlEPTB;ND64PFI1OiEQvF2= MofUV2FPT0WU
SBC-1 MoPQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoHCTWM2OD12LkmwPVA4KM7:TR?= M2Pab3NCVkeHUh?=
CTV-1 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NILte|dKSzVyPUWuOFg6OzhizszN NFTGRo9USU6JRWK=
LCLC-103H MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1n1TmlEPTB;NT63O|Q4OSEQvF2= MWnTRW5ITVJ?
RVH-421 MnPES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M173VGlEPTB;NT63O|U{PiEQvF2= M1jxenNCVkeHUh?=
K-562 NF7GN|lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYjJR|UxRTVwOUCzOkDPxE1? NYXSV4w2W0GQR1XS
CAL-33 NW[xfXU6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFLDdnZKSzVyPU[uN|E{PTlizszN NX;1b3Y5W0GQR1XS
MDA-MB-361 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoixTWM2OD14LkOzOlk6KM7:TR?= MWPTRW5ITVJ?
IGROV-1 NYTRNI1XT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF;Z[o1KSzVyPU[uOFcyQTFizszN MXHTRW5ITVJ?
NY NFTnOGRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4LhSWlEPTB;Nj61N|U6QSEQvF2= MknPV2FPT0WU
Ramos-2G6-4C10 MnXRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4TtTmlEPTB;Nj62Olk{OSEQvF2= M2LF[nNCVkeHUh?=
HuO9 NXi3fmM6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1fTPGlEPTB;Nj63N|k3PCEQvF2= NVmyVFdsW0GQR1XS
MS-1 NVLNN3Y3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUnJR|UxRTdwMUG5OVMh|ryP M{HIWHNCVkeHUh?=
RPMI-8226 M4\VTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkfITWM2OD15LkK4Nlg4KM7:TR?= M{nwUHNCVkeHUh?=
HDLM-2 NWT4XG5rT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHjBNIVKSzVyPUeuOFAyPDlizszN MULTRW5ITVJ?
D-566MG M2LP[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVLJR|UxRTdwNEexOVUh|ryP MWPTRW5ITVJ?
SK-MEL-24 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXrJR|UxRTdwNkOzPVIh|ryP NHHQTmNUSU6JRWK=
COLO-679 MlPjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVXJR|UxRTdwOUi2O|Eh|ryP MkX2V2FPT0WU
EW-13 NGTUfZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkXKTWM2OD16LkOyNFU1KM7:TR?= M3PLNHNCVkeHUh?=
A388 NHPFOHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnjtTWM2OD16LkO4OFgyKM7:TR?= M2niZnNCVkeHUh?=
UM-UC-3 NHzmZotIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlvWTWM2OD16LkSzPVU3KM7:TR?= NHHL[VNUSU6JRWK=
NUGC-3 Mnj2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIDxc5BKSzVyPUiuOVM2QDJizszN NIrUe|dUSU6JRWK=
COLO-668 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYnxS|JiUUN3ME24MlU6PDlzIN88US=> M2Xs[HNCVkeHUh?=
MOLT-4 NIfSSWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWTJR|UxRThwNkKzOVMh|ryP Ml;zV2FPT0WU
D-423MG MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkHjTWM2OD16LkizO|U3KM7:TR?= M3i2c3NCVkeHUh?=
CTB-1 NXL5epRYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXzJR|UxRThwOEexNlgh|ryP NEDQN25USU6JRWK=
BCPAP MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnjoTWM2OD17LkCyOVYzKM7:TR?= NX3JZYE6W0GQR1XS
GCT MljsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3v0cWlEPTB;OT6wPVg{OSEQvF2= NVHkOFdIW0GQR1XS
ACHN MoXLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWfrdYc4UUN3ME25MlI{PjN{IN88US=> NYi1UnI5W0GQR1XS
KYSE-520 NH72[IJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M33YRWlEPTB;OT6zN|Q5OiEQvF2= NX60NYRbW0GQR1XS
LB771-HNC NUTlUoY4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4jRXWlEPTB;OT63OlQ6PyEQvF2= NVHne5dWW0GQR1XS
MLMA MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkLuTWM2OD1zMD6wNVMzKM7:TR?= MYXTRW5ITVJ?
HEC-1 NXnwNmtnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NETVfGxKSzVyPUGwMlI5ODRizszN MXfTRW5ITVJ?
HL-60 Ml3BS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUXDO20zUUN3ME2xNE43QDV|IN88US=> M2DBSnNCVkeHUh?=
A101D MlXjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEPUR3JKSzVyPUGwMlg6OjNizszN NVqwdFRIW0GQR1XS
A2058 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmPnTWM2OD1zMD65NlQ2KM7:TR?= NIiyZWJUSU6JRWK=
KARPAS-45 M4DjeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlfxTWM2OD1zMT6wOlM2KM7:TR?= M1n1cnNCVkeHUh?=
697 M3vZZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEj1O5NKSzVyPUGxMlIyODFizszN M3m1PHNCVkeHUh?=
NCI-N87 MkPsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXyxT3pCUUN3ME2xNU44PzNzIN88US=> MmfUV2FPT0WU
DSH1 NX3BfJFPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYDGWXFZUUN3ME2xNU44QTV|IN88US=> MofIV2FPT0WU
HLE M3PxdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MojMTWM2OD1zMT64PFM6KM7:TR?= M2TnWXNCVkeHUh?=
NCI-H720 NWrQeFJOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXXJR|UxRTF{Lk[4NFEh|ryP MlfPV2FPT0WU
EW-3 NFfSUJdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHP3S25KSzVyPUGyMlk{ODdizszN NYjh[oZIW0GQR1XS
AGS M2HiW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NICwZpJKSzVyPUGzMlA{PTFizszN MXPTRW5ITVJ?
ES5 NUTEUlgxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYfJR|UxRTF|LkC1NVIh|ryP NWnH[plwW0GQR1XS
DB M4jQOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3n0WWlEPTB;MUOuN|I2PiEQvF2= NUTs[ZNCW0GQR1XS
A4-Fuk NXOyW4VKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVLoNmZEUUN3ME2xN{41OTB{IN88US=> M4Tu[HNCVkeHUh?=
A427 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIrVRWJKSzVyPUGzMlQ6PzJizszN M4jh[nNCVkeHUh?=
MN-60 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1rlUmlEPTB;MUOuOVg1OyEQvF2= NVjEWHVlW0GQR1XS
HCC2218 NHziVXBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4XPbmlEPTB;MUOuOVg2PiEQvF2= MmX1V2FPT0WU
MV-4-11 MkLWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MojsTWM2OD1zMz64NVM4KM7:TR?= M3i3PXNCVkeHUh?=
GI-1 NWTrXG9JT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVjJR|UxRTF2LkGxPFQh|ryP MWrTRW5ITVJ?
JVM-3 NW\ueHdCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUHrdpZ6UUN3ME2xOE4zPjV4IN88US=> MlLSV2FPT0WU
NCI-H2029 MmTWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH\C[XpKSzVyPUG0MlI4OjdizszN NFmwPFJUSU6JRWK=
TE-12 M1TzO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWTmZpNOUUN3ME2xOE43ODR4IN88US=> NIH4SFZUSU6JRWK=
WM-115 NEjheYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWXJR|UxRTF3LkW2PFMh|ryP NETERW1USU6JRWK=
BB65-RCC MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFnQbXVKSzVyPUG2MlAzPDFizszN MlW0V2FPT0WU
NCI-H1693 M{HPcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M12zS2lEPTB;MU[uN|gxOiEQvF2= MVrTRW5ITVJ?
KARPAS-299 M{fZNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{fTVGlEPTB;MU[uOlIxOyEQvF2= NHHtO4RUSU6JRWK=
UACC-257 M17FWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2r2fmlEPTB;MUeuNFU5OiEQvF2= NGj2UFdUSU6JRWK=
RKO M3zX[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFmwRYFKSzVyPUG3MlY1OzNizszN MlK2V2FPT0WU
HT-29 M3npdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4D1UWlEPTB;MUeuO|g5QSEQvF2= MUfTRW5ITVJ?
ES7 NIrYVY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWDTSnFsUUN3ME2xPE4yOTJ{IN88US=> MWPTRW5ITVJ?
DEL M1;oV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVOx[HJ6UUN3ME2xPE4{OTd{IN88US=> NUOxPHNmW0GQR1XS
BT-549 MlXUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnT2TWM2OD1zOD60NFkzKM7:TR?= MY\TRW5ITVJ?
NCI-H1755 M4DzUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEPHdmFKSzVyPUG4MlU4OjNizszN Mor1V2FPT0WU
HCE-T NV;q[JhuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWXJR|UxRTF6LkizOFEh|ryP NVXM[45ZW0GQR1XS
LU-139 NHX6UXdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2iyRWlEPTB;MUmuNFQ2QCEQvF2= NU\HNop[W0GQR1XS
ECC10 M1HmOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3HYU2lEPTB;MUmuNlQ4PSEQvF2= NVrVN5hSW0GQR1XS
769-P MoHPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1fLbmlEPTB;MUmuOlM{PSEQvF2= NInBO|hUSU6JRWK=
BALL-1 NUD1bVRwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4\BNWlEPTB;MUmuOlc4PSEQvF2= M{j6e3NCVkeHUh?=
LXF-289 NInlUllIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NULuS3BmUUN3ME2xPU45QTd7IN88US=> MUXTRW5ITVJ?
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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

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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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID