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 Ml7vS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmftTWM2OD1yLkCwNFE1PCEQvF2= MXTTRW5ITVJ?
KU812 MkL0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3[0SWlEPTB;MD6wNFI1QCEQvF2= M3zvV3NCVkeHUh?=
EM-2 NXj2XppST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEf3e2NKSzVyPUCuNFA1OSEQvF2= NXKy[G5iW0GQR1XS
LAMA-84 Moj1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NG\6WlhKSzVyPUCuNFA1QSEQvF2= MVHTRW5ITVJ?
MEG-01 M2\DWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1fxS2lEPTB;MD6wNFgzQCEQvF2= NXmycZVLW0GQR1XS
BV-173 NGjNbmdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYjuc4J{UUN3ME2wMlAyODh7IN88US=> MV3TRW5ITVJ?
KASUMI-1 MkGzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUXsWpdEUUN3ME2wMlAzPDF|IN88US=> NWHEOm4zW0GQR1XS
NB7 NWnxU2tqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEDOeI1KSzVyPUCuNVM1OzlizszN M{DCPHNCVkeHUh?=
BHT-101 NFXTZ5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHPnZmxKSzVyPUCuOlQzPjNizszN MorZV2FPT0WU
CGTH-W-1 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX33XFNrUUN3ME2wMlY1QDdizszN M{DD[3NCVkeHUh?=
HMV-II NWHYelFwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{TIV2lEPTB;MD63OFg4PCEQvF2= M2q2OHNCVkeHUh?=
NKM-1 NIfwcnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2juemlEPTB;MD65NFE2KM7:TR?= NIrneVVUSU6JRWK=
LB2241-RCC MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHLwfFBKSzVyPUGuNFIzOjhizszN M16zPXNCVkeHUh?=
NCI-H1703 NXPwcYZVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWfJR|UxRTFwMUi4O{DPxE1? MYTTRW5ITVJ?
BE-13 NHrFOZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYrJR|UxRTFwMke0NVYh|ryP NYftdXh6W0GQR1XS
ACN MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFTNWpZKSzVyPUGuOVUxPzdizszN MV3TRW5ITVJ?
A204 NVfHRWN4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3ruUGlEPTB;MT61O|IxPSEQvF2= NWfBS2FzW0GQR1XS
HOP-62 NGXtTZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX;JR|UxRTFwOEKwO|ch|ryP MlG3V2FPT0WU
H9 NFPDb5RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVXJR|UxRTJwN{O3PVMh|ryP NGDIeWdUSU6JRWK=
HCC1806 Mn3rS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlvKTWM2OD1{Lke0N|I4KM7:TR?= NGnTNWFUSU6JRWK=
NOS-1 MmS0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWrJR|UxRTJwOEexNFIh|ryP NVjkOnhKW0GQR1XS
RS4-11 M{DK[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX33V4FbUUN3ME2yMlkxPjJ|IN88US=> NGKwRmZUSU6JRWK=
JAR MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXjJR|UxRTJwOUKwPFQh|ryP NWnOOW5wW0GQR1XS
T98G MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NInnOXZKSzVyPUOuNFE{OTNizszN Mm\YV2FPT0WU
NCI-SNU-1 NWfSWVgxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXrCdnNzUUN3ME2zMlQxODl{IN88US=> M2C2TXNCVkeHUh?=
SK-MEL-1 MlXTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFLTemdKSzVyPUOuOFMxOjlizszN MoDDV2FPT0WU
L-363 MkLrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXvPPGZOUUN3ME2zMlYyOTB5IN88US=> NXLFS41pW0GQR1XS
SW982 M3y5[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1PkXGlEPTB;Mz62OFE3QSEQvF2= MWrTRW5ITVJ?
HT-1080 NHyz[IpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NImwdlZKSzVyPUOuPVE4PzVizszN M2rHT3NCVkeHUh?=
G-402 NUfMW3NET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX\JR|UxRTRwM{GyNFMh|ryP NHXpNGVUSU6JRWK=
HOS M{DVb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGjHbWhKSzVyPUSuPFAzQDJizszN Mke0V2FPT0WU
SK-NEP-1 MoD5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWr3PVhCUUN3ME20Mlg{OTlzIN88US=> NUC5WIZuW0GQR1XS
HAL-01 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUTZO5V1UUN3ME20Mlg5OjR{IN88US=> MUXTRW5ITVJ?
SBC-1 NH3IO4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoGxTWM2OD12LkmwPVA4KM7:TR?= NEH3eZRUSU6JRWK=
CTV-1 M{Hybmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4S5WGlEPTB;NT60PFk{QCEQvF2= NIHweXNUSU6JRWK=
LCLC-103H NGWzTWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVjJR|UxRTVwN{e0O|Eh|ryP NUjFNmNDW0GQR1XS
RVH-421 NFv6W49Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoC5TWM2OD13Lke3OVM3KM7:TR?= M4\RV3NCVkeHUh?=
K-562 MnvBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mki1TWM2OD13LkmwN|Yh|ryP NXy2OXlRW0GQR1XS
CAL-33 Mne4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUjJR|UxRTZwM{GzOVkh|ryP NHLkUFZUSU6JRWK=
MDA-MB-361 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWfWTFhNUUN3ME22MlM{Pjl7IN88US=> NUPUeWUyW0GQR1XS
IGROV-1 M{m1Zmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVTtWlBDUUN3ME22MlQ4OTlzIN88US=> MnvqV2FPT0WU
NY NILxNYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHfKbYZKSzVyPU[uOVM2QTlizszN NYOybm5VW0GQR1XS
Ramos-2G6-4C10 NULKVYdsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3LpO2lEPTB;Nj62Olk{OSEQvF2= M{nZUXNCVkeHUh?=
HuO9 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3jHPGlEPTB;Nj63N|k3PCEQvF2= NGTkUG5USU6JRWK=
MS-1 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIfZZ29KSzVyPUeuNVE6PTNizszN NID2eJlUSU6JRWK=
RPMI-8226 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWnpcItsUUN3ME23MlI5Ojh5IN88US=> M2jLVnNCVkeHUh?=
HDLM-2 MoHQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVWxc2JMUUN3ME23MlQxOTR7IN88US=> MoWyV2FPT0WU
D-566MG MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmfoTWM2OD15LkS3NVU2KM7:TR?= NFGzSmhUSU6JRWK=
SK-MEL-24 MlrZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYHJR|UxRTdwNkOzPVIh|ryP MXPTRW5ITVJ?
COLO-679 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHPnOVRKSzVyPUeuPVg3PzFizszN M1\iXHNCVkeHUh?=
EW-13 M{LJN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVXJR|UxRThwM{KwOVQh|ryP M{n4TnNCVkeHUh?=
A388 M1;OSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4L6TmlEPTB;OD6zPFQ5OSEQvF2= NFzyN5ZUSU6JRWK=
UM-UC-3 NHzGcYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUjr[2p4UUN3ME24MlQ{QTV4IN88US=> Moq5V2FPT0WU
NUGC-3 NYf2UGNDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYC4RlJDUUN3ME24MlU{PTh{IN88US=> NEe4UnBUSU6JRWK=
COLO-668 M1HoWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUHrNlB7UUN3ME24MlU6PDlzIN88US=> MU\TRW5ITVJ?
MOLT-4 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXzJR|UxRThwNkKzOVMh|ryP MV\TRW5ITVJ?
D-423MG M1;pWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1fKcGlEPTB;OD64N|c2PiEQvF2= M2G1VHNCVkeHUh?=
CTB-1 M3HW[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFK4XZZKSzVyPUiuPFcyOjhizszN Mo\lV2FPT0WU
BCPAP NEPrT3RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYrjW4JXUUN3ME25MlAzPTZ{IN88US=> M125VnNCVkeHUh?=
GCT NXfP[4FVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{\mOGlEPTB;OT6wPVg{OSEQvF2= M1z6cnNCVkeHUh?=
ACHN M{DIbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUPJR|UxRTlwMkO2N|Ih|ryP MnK5V2FPT0WU
KYSE-520 NVu5T|NkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIDGc21KSzVyPUmuN|M1QDJizszN MYfTRW5ITVJ?
LB771-HNC MmHJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{\LTWlEPTB;OT63OlQ6PyEQvF2= NXG2OZU6W0GQR1XS
MLMA MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEj3XpRKSzVyPUGwMlAyOzJizszN Ml;3V2FPT0WU
HEC-1 NIHIOHhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIfIcWhKSzVyPUGwMlI5ODRizszN NEXBSINUSU6JRWK=
HL-60 NEPCVXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWDHT|JXUUN3ME2xNE43QDV|IN88US=> MVzTRW5ITVJ?
A101D MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXv0T2pJUUN3ME2xNE45QTJ|IN88US=> MWnTRW5ITVJ?
A2058 Moq1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIj1NlNKSzVyPUGwMlkzPDVizszN M3\PZnNCVkeHUh?=
KARPAS-45 NHHWTVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWrJR|UxRTFzLkC2N|Uh|ryP M3qyU3NCVkeHUh?=
697 NXTuOY9jT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYLTcI5{UUN3ME2xNU4zOTBzIN88US=> NICzOmxUSU6JRWK=
NCI-N87 NEfSXmNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlLHTWM2OD1zMT63O|MyKM7:TR?= M2TU[3NCVkeHUh?=
DSH1 NEXUTWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1\HcmlEPTB;MUGuO|k2OyEQvF2= NELDclRUSU6JRWK=
HLE MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHnsWGtKSzVyPUGxMlg5OzlizszN NHzQbIlUSU6JRWK=
NCI-H720 MnzlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHr1XFlKSzVyPUGyMlY5ODFizszN NIrWbFdUSU6JRWK=
EW-3 NVLNcIhsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH[wVI5KSzVyPUGyMlk{ODdizszN M4j2SHNCVkeHUh?=
AGS MmHaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWjJR|UxRTF|LkCzOVEh|ryP MXXTRW5ITVJ?
ES5 NFTS[5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFjlXJBKSzVyPUGzMlA2OTJizszN NILxSZpUSU6JRWK=
DB NIKyWYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mk\0TWM2OD1zMz6zNlU3KM7:TR?= MWDTRW5ITVJ?
A4-Fuk MmW4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MY\JR|UxRTF|LkSxNFIh|ryP MV7TRW5ITVJ?
A427 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUTJR|UxRTF|LkS5O|Ih|ryP NXL6UXdxW0GQR1XS
MN-60 NXPYTW1NT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV\JR|UxRTF|LkW4OFMh|ryP M{H1enNCVkeHUh?=
HCC2218 M4DJTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkOxTWM2OD1zMz61PFU3KM7:TR?= M{LkVnNCVkeHUh?=
MV-4-11 NH;wS|lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2rkemlEPTB;MUOuPFE{PyEQvF2= NInETYxUSU6JRWK=
GI-1 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHjnc5JKSzVyPUG0MlEyQDRizszN MVPTRW5ITVJ?
JVM-3 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXjVTWdvUUN3ME2xOE4zPjV4IN88US=> NYHMWYpoW0GQR1XS
NCI-H2029 M3HQdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVGxcWo2UUN3ME2xOE4zPzJ5IN88US=> NYXiSHJyW0GQR1XS
TE-12 M4LqTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3v6R2lEPTB;MUSuOlA1PiEQvF2= NUW2T2FlW0GQR1XS
WM-115 NHXGepFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NG\odGhKSzVyPUG1MlU3QDNizszN NUizdGR[W0GQR1XS
BB65-RCC NH;a[XJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX3BUnh7UUN3ME2xOk4xOjRzIN88US=> MmXoV2FPT0WU
NCI-H1693 NIXkUXdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXK2[JJ6UUN3ME2xOk4{QDB{IN88US=> Mn7uV2FPT0WU
KARPAS-299 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWm1VW9rUUN3ME2xOk43OjB|IN88US=> NVXnW4R4W0GQR1XS
UACC-257 NGTPeI1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXLJR|UxRTF5LkC1PFIh|ryP MXPTRW5ITVJ?
RKO MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkPnTWM2OD1zNz62OFM{KM7:TR?= NEizbGZUSU6JRWK=
HT-29 NH\oT4hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWrRdVVlUUN3ME2xO{44QDh7IN88US=> M4Pw[3NCVkeHUh?=
ES7 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M33HXmlEPTB;MUiuNVEzOiEQvF2= M{DxdHNCVkeHUh?=
DEL NV7KUnJRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWnl[oluUUN3ME2xPE4{OTd{IN88US=> MUHTRW5ITVJ?
BT-549 NHn5WpVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M13LUGlEPTB;MUiuOFA6OiEQvF2= MlX4V2FPT0WU
NCI-H1755 NUftNYk3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX;PWpZLUUN3ME2xPE42PzJ|IN88US=> NViyZXlSW0GQR1XS
HCE-T MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXz2Wlg1UUN3ME2xPE45OzRzIN88US=> NGq3[2FUSU6JRWK=
LU-139 NW\HeHRqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVfJR|UxRTF7LkC0OVgh|ryP MXfTRW5ITVJ?
ECC10 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MULJR|UxRTF7LkK0O|Uh|ryP NFjaTG9USU6JRWK=
769-P MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXuwXJF[UUN3ME2xPU43OzN3IN88US=> NF\VclJUSU6JRWK=
BALL-1 MlPKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4LyPGlEPTB;MUmuOlc4PSEQvF2= M4fENHNCVkeHUh?=
LXF-289 NXn4Z|NJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWjJR|UxRTF7Lki5O|kh|ryP NHPoR|hUSU6JRWK=
TYK-nu M{\2[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4TjcmlEPTB;MUmuPVMyPSEQvF2= MYDTRW5ITVJ?
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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 slightly soluble or insoluble
Ethanol slightly soluble or insoluble
In vivo Add solvents individually and in order:
4% DMSO+30% PEG 300+5% Tween 80+ddH2O
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
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

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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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID