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 Mm\5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEixWmVKSzVyPUCuNFAxOTR2IN88US=> NIHrflFUSU6JRWK=
KU812 MlT5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIDFSY1KSzVyPUCuNFAzPDhizszN MVrTRW5ITVJ?
EM-2 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkXnTWM2OD1yLkCwOFEh|ryP M3S2RXNCVkeHUh?=
LAMA-84 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXnBTmN5UUN3ME2wMlAxPDlizszN NFn3NlVUSU6JRWK=
MEG-01 NILsOFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4rm[WlEPTB;MD6wNFgzQCEQvF2= NX;OSFhzW0GQR1XS
BV-173 NIDremVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWPJR|UxRTBwMEGwPFkh|ryP M{TEfXNCVkeHUh?=
KASUMI-1 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWX6TVBKUUN3ME2wMlAzPDF|IN88US=> NGjhcpBUSU6JRWK=
NB7 M2L3e2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH;6SZdKSzVyPUCuNVM1OzlizszN MoDGV2FPT0WU
BHT-101 NH7zTVdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2rHTWlEPTB;MD62OFI3OyEQvF2= M{HjU3NCVkeHUh?=
CGTH-W-1 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYrJR|UxRTBwNkS4O{DPxE1? M{TFfnNCVkeHUh?=
HMV-II Mn7qS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnLSTWM2OD1yLke0PFc1KM7:TR?= MVHTRW5ITVJ?
NKM-1 MmLaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3vRdGlEPTB;MD65NFE2KM7:TR?= NX73V4c6W0GQR1XS
LB2241-RCC NWPZOpl1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFTtVmJKSzVyPUGuNFIzOjhizszN MWrTRW5ITVJ?
NCI-H1703 MojtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH;udINKSzVyPUGuNVg5PyEQvF2= MYjTRW5ITVJ?
BE-13 Mn3CS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MofSTWM2OD1zLkK3OFE3KM7:TR?= M4HvRXNCVkeHUh?=
ACN M{LGT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mk\aTWM2OD1zLkW1NFc4KM7:TR?= M{ixbnNCVkeHUh?=
A204 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWH5R2hzUUN3ME2xMlU4OjB3IN88US=> M320WHNCVkeHUh?=
HOP-62 NI\aWGxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH3WdIdKSzVyPUGuPFIxPzdizszN M1zTe3NCVkeHUh?=
H9 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXnJR|UxRTJwN{O3PVMh|ryP NF\FbXJUSU6JRWK=
HCC1806 M3;4RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mmq1TWM2OD1{Lke0N|I4KM7:TR?= MkDvV2FPT0WU
NOS-1 NWC0[|JiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYPJR|UxRTJwOEexNFIh|ryP NHzDVWtUSU6JRWK=
RS4-11 NELYOZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWHJR|UxRTJwOUC2NlMh|ryP Mn7QV2FPT0WU
JAR MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIjnbY5KSzVyPUKuPVIxQDRizszN MV3TRW5ITVJ?
T98G M3P5SWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWLJR|UxRTNwMEGzNVMh|ryP M4W4O3NCVkeHUh?=
NCI-SNU-1 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYPJR|UxRTNwNECwPVIh|ryP Mn;EV2FPT0WU
SK-MEL-1 Mm\sS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUXsSXh3UUN3ME2zMlQ{ODJ7IN88US=> MYrTRW5ITVJ?
L-363 NWHh[oJzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYrJR|UxRTNwNkGxNFch|ryP NIq3fVNUSU6JRWK=
SW982 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NITvWFFKSzVyPUOuOlQyPjlizszN M3ixb3NCVkeHUh?=
HT-1080 NUG3XZlnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NG\kdHlKSzVyPUOuPVE4PzVizszN M4DIWHNCVkeHUh?=
G-402 NIG5ZmFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVPiZpBQUUN3ME20MlMyOjB|IN88US=> MoHqV2FPT0WU
HOS M3;Nfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFj2SXhKSzVyPUSuPFAzQDJizszN NWnYZlh{W0GQR1XS
SK-NEP-1 MnflS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoXzTWM2OD12LkizNVkyKM7:TR?= MWfTRW5ITVJ?
HAL-01 M{HYO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3nQWWlEPTB;ND64PFI1OiEQvF2= NFXL[W5USU6JRWK=
SBC-1 Mln5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV\JR|UxRTRwOUC5NFch|ryP MVLTRW5ITVJ?
CTV-1 NYLxVHlqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX3JR|UxRTVwNEi5N|gh|ryP NFnmd3BUSU6JRWK=
LCLC-103H MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnzmTWM2OD13Lke3OFcyKM7:TR?= NYfXdJZCW0GQR1XS
RVH-421 NGnUN3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXrP[4RzUUN3ME21Mlc4PTN4IN88US=> NInReGdUSU6JRWK=
K-562 MkTuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnryTWM2OD13LkmwN|Yh|ryP M3jmeHNCVkeHUh?=
CAL-33 NIjMO2lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1G5fWlEPTB;Nj6zNVM2QSEQvF2= M3\VOnNCVkeHUh?=
MDA-MB-361 M1T2O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlvyTWM2OD14LkOzOlk6KM7:TR?= NYTuVYxwW0GQR1XS
IGROV-1 MoLGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGDCZ5FKSzVyPU[uOFcyQTFizszN Mn;HV2FPT0WU
NY NYKy[G8{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWLJR|UxRTZwNUO1PVkh|ryP M4jCRXNCVkeHUh?=
Ramos-2G6-4C10 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{H0TGlEPTB;Nj62Olk{OSEQvF2= M4DGSHNCVkeHUh?=
HuO9 NVrWW2xTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkmwTWM2OD14LkezPVY1KM7:TR?= NEL4OYZUSU6JRWK=
MS-1 NGXRd4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnniTWM2OD15LkGxPVU{KM7:TR?= NEW5WWJUSU6JRWK=
RPMI-8226 M1;RT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUC5bZEyUUN3ME23MlI5Ojh5IN88US=> MkXNV2FPT0WU
HDLM-2 NXTuXIRNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGL0RodKSzVyPUeuOFAyPDlizszN MVrTRW5ITVJ?
D-566MG MkPrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGf4TGRKSzVyPUeuOFcyPTVizszN NEHNZmJUSU6JRWK=
SK-MEL-24 M3TBb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHvIVVZKSzVyPUeuOlM{QTJizszN MX3TRW5ITVJ?
COLO-679 NFTmVHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlTVTWM2OD15Lkm4OlcyKM7:TR?= NGDCUnNUSU6JRWK=
EW-13 NF7rUXlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFX4foVKSzVyPUiuN|IxPTRizszN NXzXNFJTW0GQR1XS
A388 MoPUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3jUNGlEPTB;OD6zPFQ5OSEQvF2= NGHXZoVUSU6JRWK=
UM-UC-3 NUO1cVU6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWTJR|UxRThwNEO5OVYh|ryP MYXTRW5ITVJ?
NUGC-3 NV\3SJdJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXfJR|UxRThwNUO1PFIh|ryP NHXubHRUSU6JRWK=
COLO-668 Mnf4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWiz[Y05UUN3ME24MlU6PDlzIN88US=> Ml7wV2FPT0WU
MOLT-4 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml;hTWM2OD16Lk[yN|U{KM7:TR?= NXnyO5lxW0GQR1XS
D-423MG MneyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXnJR|UxRThwOEO3OVYh|ryP NVfKc5BOW0GQR1XS
CTB-1 NWWzSVl{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1HXe2lEPTB;OD64O|EzQCEQvF2= NGO2UpJUSU6JRWK=
BCPAP MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mm\MTWM2OD17LkCyOVYzKM7:TR?= NYXXUZBoW0GQR1XS
GCT M{jy[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MknLTWM2OD17LkC5PFMyKM7:TR?= M4XnOnNCVkeHUh?=
ACHN MljmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWrJR|UxRTlwMkO2N|Ih|ryP NILPNI9USU6JRWK=
KYSE-520 NIDWVIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2PTdGlEPTB;OT6zN|Q5OiEQvF2= MXPTRW5ITVJ?
LB771-HNC M{DJRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MY\JR|UxRTlwN{[0PVch|ryP NIWzeXBUSU6JRWK=
MLMA NVfzdHBGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFXzPFFKSzVyPUGwMlAyOzJizszN M1TqcHNCVkeHUh?=
HEC-1 NWntdXozT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGPqS45KSzVyPUGwMlI5ODRizszN NEXme5pUSU6JRWK=
HL-60 M{LOXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnT1TWM2OD1zMD62PFU{KM7:TR?= MnXRV2FPT0WU
A101D NE\UPXpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3LQVWlEPTB;MUCuPFkzOyEQvF2= MXnTRW5ITVJ?
A2058 M33kRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{HnW2lEPTB;MUCuPVI1PSEQvF2= NYPxUpVVW0GQR1XS
KARPAS-45 MoruS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkLUTWM2OD1zMT6wOlM2KM7:TR?= MVzTRW5ITVJ?
697 NUjF[Fh2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGW0VHdKSzVyPUGxMlIyODFizszN M1faU3NCVkeHUh?=
NCI-N87 NUDlSZpNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{W1b2lEPTB;MUGuO|c{OSEQvF2= M2jBPXNCVkeHUh?=
DSH1 M4XwSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF3vPJNKSzVyPUGxMlc6PTNizszN MmPjV2FPT0WU
HLE MkLkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mnj6TWM2OD1zMT64PFM6KM7:TR?= MkjNV2FPT0WU
NCI-H720 NWO4O4RIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWHJR|UxRTF{Lk[4NFEh|ryP NVm4Z|hxW0GQR1XS
EW-3 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlfFTWM2OD1zMj65N|A4KM7:TR?= MoDJV2FPT0WU
AGS NXn5e281T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHHGNGdKSzVyPUGzMlA{PTFizszN MmXHV2FPT0WU
ES5 NWPiRZhzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmLGTWM2OD1zMz6wOVEzKM7:TR?= NIn4UW9USU6JRWK=
DB NULqfpZET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWHJR|UxRTF|LkOyOVYh|ryP NGPRO4xUSU6JRWK=
A4-Fuk NESzenNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVLJR|UxRTF|LkSxNFIh|ryP NH3ublNUSU6JRWK=
A427 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUDJR|UxRTF|LkS5O|Ih|ryP NVn6NnFwW0GQR1XS
MN-60 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYLJR|UxRTF|LkW4OFMh|ryP Ml[3V2FPT0WU
HCC2218 MmLRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWLXT2I6UUN3ME2xN{42QDV4IN88US=> NH34W|dUSU6JRWK=
MV-4-11 NYT3VVZCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV\sWZBnUUN3ME2xN{45OTN5IN88US=> M1vDW3NCVkeHUh?=
GI-1 Mk[4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2HMd2lEPTB;MUSuNVE5PCEQvF2= NXLJ[GdUW0GQR1XS
JVM-3 M4f3Omdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUnJR|UxRTF2LkK2OVYh|ryP MnruV2FPT0WU
NCI-H2029 M2DmcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYLJR|UxRTF2LkK3Nlch|ryP M2TjbXNCVkeHUh?=
TE-12 NXmyTFVyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHe4dVBKSzVyPUG0MlYxPDZizszN NFezSXFUSU6JRWK=
WM-115 MlzlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWXzS|NFUUN3ME2xOU42Pjh|IN88US=> NYTXW3pMW0GQR1XS
BB65-RCC NUnjU2d[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV3wdJREUUN3ME2xOk4xOjRzIN88US=> MkPHV2FPT0WU
NCI-H1693 M3S1N2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlLJTWM2OD1zNj6zPFAzKM7:TR?= NVzsUIJKW0GQR1XS
KARPAS-299 NFvjOpFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoLlTWM2OD1zNj62NlA{KM7:TR?= NYGw[3k2W0GQR1XS
UACC-257 NH\KUoxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXT2dIlRUUN3ME2xO{4xPTh{IN88US=> M2rVO3NCVkeHUh?=
RKO MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUPJR|UxRTF5Lk[0N|Mh|ryP MoDTV2FPT0WU
HT-29 NYTJeoZkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NI[4O2lKSzVyPUG3Mlc5QDlizszN NETTNnpUSU6JRWK=
ES7 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVjJR|UxRTF6LkGxNlIh|ryP MlrzV2FPT0WU
DEL NWLuS5R5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUnjUIczUUN3ME2xPE4{OTd{IN88US=> NUfCeYpuW0GQR1XS
BT-549 NYqxN2pKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkfoTWM2OD1zOD60NFkzKM7:TR?= NILsRpJUSU6JRWK=
NCI-H1755 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXTJR|UxRTF6LkW3NlMh|ryP M{nJbXNCVkeHUh?=
HCE-T MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4POR2lEPTB;MUiuPFM1OSEQvF2= MlXaV2FPT0WU
LU-139 MkDlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkTQTWM2OD1zOT6wOFU5KM7:TR?= M4X1T3NCVkeHUh?=
ECC10 NYPWTlNJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmXSTWM2OD1zOT6yOFc2KM7:TR?= NIDiR|dUSU6JRWK=
769-P NVj0em42T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIr4e2RKSzVyPUG5MlY{OzVizszN NF;LW3lUSU6JRWK=
BALL-1 NG[3Oo9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{HhcGlEPTB;MUmuOlc4PSEQvF2= M2rLWXNCVkeHUh?=
LXF-289 NYLhbo0zT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVjQWFZLUUN3ME2xPU45QTd7IN88US=> NF;QeZNUSU6JRWK=
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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