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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USD 210 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 NXvOSZdiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXWwUGZxUUN3ME2wMlAxODF2NDFOwG0> MmnHV2FPT0WU
KU812 M4HY[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH[yOYVKSzVyPUCuNFAzPDhizszN M2[xXHNCVkeHUh?=
EM-2 NXq4VHNlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHrrO4FKSzVyPUCuNFA1OSEQvF2= MWnTRW5ITVJ?
LAMA-84 MmnhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVnJR|UxRTBwMEC0PUDPxE1? MXvTRW5ITVJ?
MEG-01 MlLoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUXJR|UxRTBwMEC4Nlgh|ryP NE\UNIdUSU6JRWK=
BV-173 NED0RXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4DudGlEPTB;MD6wNVA5QSEQvF2= NHLpVoxUSU6JRWK=
KASUMI-1 NFzLd41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWLJR|UxRTBwMEK0NVMh|ryP NWnv[GVWW0GQR1XS
NB7 NX;oV4FtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MU\JR|UxRTBwMUO0N|kh|ryP MUfTRW5ITVJ?
BHT-101 Mlm5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYnJR|UxRTBwNkSyOlMh|ryP NYTac4ViW0GQR1XS
CGTH-W-1 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2TGOWlEPTB;MD62OFg4KM7:TR?= M1eybXNCVkeHUh?=
HMV-II MnvJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlfRTWM2OD1yLke0PFc1KM7:TR?= NHjJTIJUSU6JRWK=
NKM-1 NXrzZXFwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEPKdY9KSzVyPUCuPVAyPSEQvF2= MlvIV2FPT0WU
LB2241-RCC MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUnCN21kUUN3ME2xMlAzOjJ6IN88US=> M2Dl[nNCVkeHUh?=
NCI-H1703 NWCzPIo6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NE\CfVdKSzVyPUGuNVg5PyEQvF2= MnTrV2FPT0WU
BE-13 MnyxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{TMeGlEPTB;MT6yO|QyPiEQvF2= MUfTRW5ITVJ?
ACN NVrRcGhNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVzpW|c{UUN3ME2xMlU2ODd5IN88US=> NHjtXWNUSU6JRWK=
A204 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVHoXVl{UUN3ME2xMlU4OjB3IN88US=> M4\mc3NCVkeHUh?=
HOP-62 M3TXfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEi3b5FKSzVyPUGuPFIxPzdizszN M4D3e3NCVkeHUh?=
H9 NWKyWWw1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{exdmlEPTB;Mj63N|c6OyEQvF2= M1LsVnNCVkeHUh?=
HCC1806 M3jvc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{nYUmlEPTB;Mj63OFMzPyEQvF2= MYnTRW5ITVJ?
NOS-1 MnrwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXjJR|UxRTJwOEexNFIh|ryP NV7tUY9XW0GQR1XS
RS4-11 NX3lR49[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmLzTWM2OD1{LkmwOlI{KM7:TR?= M{nISHNCVkeHUh?=
JAR MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV7j[GNDUUN3ME2yMlkzODh2IN88US=> MlHpV2FPT0WU
T98G NYjJcmNTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHXuNlFKSzVyPUOuNFE{OTNizszN NHnSWXpUSU6JRWK=
NCI-SNU-1 MnLVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHflR3VKSzVyPUOuOFAxQTJizszN NF;yU3dUSU6JRWK=
SK-MEL-1 NHu4[opIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVf0TJNJUUN3ME2zMlQ{ODJ7IN88US=> NYrFbIY6W0GQR1XS
L-363 NHLm[IxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYXUOI9VUUN3ME2zMlYyOTB5IN88US=> MmflV2FPT0WU
SW982 NVrXb5Z3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWSxOYtPUUN3ME2zMlY1OTZ7IN88US=> NUPtS2FyW0GQR1XS
HT-1080 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHPHflNKSzVyPUOuPVE4PzVizszN NH7aNoZUSU6JRWK=
G-402 NXntbVBGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MU\JR|UxRTRwM{GyNFMh|ryP NIDt[VNUSU6JRWK=
HOS M3vhWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYjEOJFZUUN3ME20MlgxOjh{IN88US=> MkGwV2FPT0WU
SK-NEP-1 NGO3b5RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYHJR|UxRTRwOEOxPVEh|ryP NHLmeIdUSU6JRWK=
HAL-01 NWHnclJWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX\3W|BYUUN3ME20Mlg5OjR{IN88US=> MWDTRW5ITVJ?
SBC-1 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3jmfGlEPTB;ND65NFkxPyEQvF2= NGLiWXdUSU6JRWK=
CTV-1 M3nBd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmHRTWM2OD13LkS4PVM5KM7:TR?= MoH6V2FPT0WU
LCLC-103H MojhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGfQcFFKSzVyPUWuO|c1PzFizszN MYDTRW5ITVJ?
RVH-421 M4PuPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3\V[mlEPTB;NT63O|U{PiEQvF2= NH3ETnVUSU6JRWK=
K-562 M{jkdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mo\DTWM2OD13LkmwN|Yh|ryP MXLTRW5ITVJ?
CAL-33 NGfZNHdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWjjVo9uUUN3ME22MlMyOzV7IN88US=> MVXTRW5ITVJ?
MDA-MB-361 NV36VlBbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV3JR|UxRTZwM{O2PVkh|ryP MYjTRW5ITVJ?
IGROV-1 MnzMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX7HUJJkUUN3ME22MlQ4OTlzIN88US=> MmfrV2FPT0WU
NY MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFThUYJKSzVyPU[uOVM2QTlizszN MXvTRW5ITVJ?
Ramos-2G6-4C10 MmraS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF6wU3hKSzVyPU[uOlY6OzFizszN NGnlfnhUSU6JRWK=
HuO9 NYrOOnFGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWLJR|UxRTZwN{O5OlQh|ryP M1LQR3NCVkeHUh?=
MS-1 MkfVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUHBRXlKUUN3ME23MlEyQTV|IN88US=> MmCxV2FPT0WU
RPMI-8226 NWfGZ5p3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlPoTWM2OD15LkK4Nlg4KM7:TR?= M1rOOXNCVkeHUh?=
HDLM-2 M2HoUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{nYfmlEPTB;Nz60NFE1QSEQvF2= NIDUWYRUSU6JRWK=
D-566MG MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX3JR|UxRTdwNEexOVUh|ryP Mk\aV2FPT0WU
SK-MEL-24 NYXlTlVuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml\aTWM2OD15Lk[zN|kzKM7:TR?= MVvTRW5ITVJ?
COLO-679 NIjKUWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1rsbWlEPTB;Nz65PFY4OSEQvF2= NH65dW5USU6JRWK=
EW-13 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFn5VoFKSzVyPUiuN|IxPTRizszN NHTHeZdUSU6JRWK=
A388 NYq3[pZtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFj3W5lKSzVyPUiuN|g1QDFizszN NIizbFRUSU6JRWK=
UM-UC-3 NEXuXFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mnz6TWM2OD16LkSzPVU3KM7:TR?= NILu[m1USU6JRWK=
NUGC-3 M4\UOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2n0d2lEPTB;OD61N|U5OiEQvF2= NXXQbHhLW0GQR1XS
COLO-668 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUXJR|UxRThwNUm0PVEh|ryP M3XUenNCVkeHUh?=
MOLT-4 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MojnTWM2OD16Lk[yN|U{KM7:TR?= MYjTRW5ITVJ?
D-423MG NVLiPJZRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVf6XoYxUUN3ME24Mlg{PzV4IN88US=> M3y0W3NCVkeHUh?=
CTB-1 M2rUPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MorFTWM2OD16Lki3NVI5KM7:TR?= NIP5c5JUSU6JRWK=
BCPAP NUfvU3ZHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYXJR|UxRTlwMEK1OlIh|ryP NH3EWHpUSU6JRWK=
GCT MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYfyb49qUUN3ME25MlA6QDNzIN88US=> NGnVUnFUSU6JRWK=
ACHN M3zVU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4\rSGlEPTB;OT6yN|Y{OiEQvF2= M3zLO3NCVkeHUh?=
KYSE-520 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoPoTWM2OD17LkOzOFgzKM7:TR?= M1vucXNCVkeHUh?=
LB771-HNC MlLrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWG1TFZlUUN3ME25Mlc3PDl5IN88US=> NHqxcmlUSU6JRWK=
MLMA MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVXJR|UxRTFyLkCxN|Ih|ryP MnPJV2FPT0WU
HEC-1 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{HSbmlEPTB;MUCuNlgxPCEQvF2= M4HWe3NCVkeHUh?=
HL-60 NEH6eFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUPJR|UxRTFyLk[4OVMh|ryP NGPVOVRUSU6JRWK=
A101D M1nzfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH3RZVFKSzVyPUGwMlg6OjNizszN MnjyV2FPT0WU
A2058 NUXlVphXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3TZWWlEPTB;MUCuPVI1PSEQvF2= M3XVZ3NCVkeHUh?=
KARPAS-45 NELkR3RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUGxfFFwUUN3ME2xNU4xPjN3IN88US=> MYTTRW5ITVJ?
697 NX7wWoE{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NY\DWI1VUUN3ME2xNU4zOTBzIN88US=> Mn3pV2FPT0WU
NCI-N87 NVPvcZR7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2TZdWlEPTB;MUGuO|c{OSEQvF2= MWnTRW5ITVJ?
DSH1 MlznS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHjYfphKSzVyPUGxMlc6PTNizszN M4T2Z3NCVkeHUh?=
HLE NYL0OWlGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHvaTJlKSzVyPUGxMlg5OzlizszN MWPTRW5ITVJ?
NCI-H720 MoXPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX7I[2FPUUN3ME2xNk43QDBzIN88US=> NXXGVY9vW0GQR1XS
EW-3 NEPXVWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUfJR|UxRTF{LkmzNFch|ryP NXfiOmYzW0GQR1XS
AGS MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYHJR|UxRTF|LkCzOVEh|ryP MmPUV2FPT0WU
ES5 NUXkdZNOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWfJR|UxRTF|LkC1NVIh|ryP M2noOnNCVkeHUh?=
DB NXHVTmY6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIfIOY5KSzVyPUGzMlMzPTZizszN M2L4SXNCVkeHUh?=
A4-Fuk MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX3MVlBXUUN3ME2xN{41OTB{IN88US=> MV;TRW5ITVJ?
A427 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIPDfXZKSzVyPUGzMlQ6PzJizszN NHLW[GNUSU6JRWK=
MN-60 M4P5eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MknVTWM2OD1zMz61PFQ{KM7:TR?= MmXRV2FPT0WU
HCC2218 MnnXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXrRU|QyUUN3ME2xN{42QDV4IN88US=> NUfCNG9iW0GQR1XS
MV-4-11 M3XNXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MofyTWM2OD1zMz64NVM4KM7:TR?= M17WNnNCVkeHUh?=
GI-1 NXi0flFJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXX3fopqUUN3ME2xOE4yOTh2IN88US=> MoHUV2FPT0WU
JVM-3 M{j5c2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXP4ZWs1UUN3ME2xOE4zPjV4IN88US=> MY\TRW5ITVJ?
NCI-H2029 NUPUdlJbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NY[wcGppUUN3ME2xOE4zPzJ5IN88US=> Mn\GV2FPT0WU
TE-12 MkTWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXXpfWhXUUN3ME2xOE43ODR4IN88US=> M4rXO3NCVkeHUh?=
WM-115 M1vsUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M13pNmlEPTB;MUWuOVY5OyEQvF2= MXnTRW5ITVJ?
BB65-RCC MkfBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHj3PGhKSzVyPUG2MlAzPDFizszN MWXTRW5ITVJ?
NCI-H1693 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NULFeIpvUUN3ME2xOk4{QDB{IN88US=> M1HO[3NCVkeHUh?=
KARPAS-299 NWrEcWROT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnLLTWM2OD1zNj62NlA{KM7:TR?= M4jZUHNCVkeHUh?=
UACC-257 NUf1WoJ4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{m2XWlEPTB;MUeuNFU5OiEQvF2= M2TpUnNCVkeHUh?=
RKO MoDBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV\JR|UxRTF5Lk[0N|Mh|ryP NW\PXW9XW0GQR1XS
HT-29 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWjJR|UxRTF5Lke4PFkh|ryP NF35cGVUSU6JRWK=
ES7 MlPoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHzjdnFKSzVyPUG4MlEyOjJizszN MmPMV2FPT0WU
DEL NV\hXlM3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmfrTWM2OD1zOD6zNVczKM7:TR?= NV7meVRRW0GQR1XS
BT-549 M2n1XGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmLZTWM2OD1zOD60NFkzKM7:TR?= NYfvbIg3W0GQR1XS
NCI-H1755 M{D6Omdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIHv[WtKSzVyPUG4MlU4OjNizszN MXHTRW5ITVJ?
HCE-T MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF7n[WxKSzVyPUG4Mlg{PDFizszN Mk[0V2FPT0WU
LU-139 NWLmdnE2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX;qZ3RyUUN3ME2xPU4xPDV6IN88US=> NWPrS|NKW0GQR1XS
ECC10 NFjzSo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmPxTWM2OD1zOT6yOFc2KM7:TR?= MVTTRW5ITVJ?
769-P NF;qSoNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkL1TWM2OD1zOT62N|M2KM7:TR?= MY\TRW5ITVJ?
BALL-1 NF\SdJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NELHPYtKSzVyPUG5MlY4PzVizszN NU\xS2dYW0GQR1XS
LXF-289 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV:0Uo5NUUN3ME2xPU45QTd7IN88US=> MXjTRW5ITVJ?
TYK-nu M2HqfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M125O2lEPTB;MUmuPVMyPSEQvF2= NUPhPXFQW0GQR1XS
NCI-H630 M1[4TGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYXJR|UxRTF7LkmzO|gh|ryP MXvTRW5ITVJ?
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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
NCT03578367 Recruiting CML|Chronic Myelogenous Leukemia|Leukemia Myeloid Chronic|Hematologic Diseases Novartis Pharmaceuticals|Novartis November 12 2018 Phase 2
NCT03516279 Not yet recruiting Chronic Phase Chronic Myelogenous Leukemia BCR-ABL1 Positive|Minimal Residual Disease ECOG-ACRIN Cancer Research Group|National Cancer Institute (NCI)|Eastern Cooperative Oncology Group August 12 2018 Phase 2
NCT03654768 Recruiting Chronic Phase Chronic Myelogenous Leukemia BCR-ABL1 Positive Southwest Oncology Group|National Cancer Institute (NCI) July 20 2018 Phase 2
NCT03228303 Not yet recruiting Chronic Myeloid Leukemia Assiut University December 1 2017 Early Phase 1
NCT03205488 Recruiting Parkinson Disease Northwestern University|University of Rochester|University of Iowa|Michael J. Fox Foundation for Parkinson''s Research October 16 2017 Phase 2
NCT03079505 Recruiting Chronic Myeloid Leukemia - Chronic Phase Hamad Medical Corporation August 3 2017 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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID