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 M{DSOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXrJR|UxRTBwMECwNVQ1KM7:TR?= M{PwOXNCVkeHUh?=
KU812 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUHJR|UxRTBwMECyOFgh|ryP NV65dYdDW0GQR1XS
EM-2 Mm\ZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWm5S4hsUUN3ME2wMlAxPDFizszN M124NHNCVkeHUh?=
LAMA-84 NIj2SoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUfJR|UxRTBwMEC0PUDPxE1? MkfrV2FPT0WU
MEG-01 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXHhboZDUUN3ME2wMlAxQDJ6IN88US=> M{jGdXNCVkeHUh?=
BV-173 MnPrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4\aPGlEPTB;MD6wNVA5QSEQvF2= MUjTRW5ITVJ?
KASUMI-1 NEDwT|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVf5OJBbUUN3ME2wMlAzPDF|IN88US=> Mn7lV2FPT0WU
NB7 NY\uTolWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mlu1TWM2OD1yLkGzOFM6KM7:TR?= Ml;EV2FPT0WU
BHT-101 M1H6Umdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWjJR|UxRTBwNkSyOlMh|ryP NVzwOXlHW0GQR1XS
CGTH-W-1 M1rT[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHO2UZVKSzVyPUCuOlQ5PyEQvF2= NF7ReY5USU6JRWK=
HMV-II M3XIZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NW\6e2NrUUN3ME2wMlc1QDd2IN88US=> NIP0boZUSU6JRWK=
NKM-1 NYrEXGFYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M363SGlEPTB;MD65NFE2KM7:TR?= MYLTRW5ITVJ?
LB2241-RCC M4TaW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFz3S4dKSzVyPUGuNFIzOjhizszN NWLuSo9PW0GQR1XS
NCI-H1703 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmTSTWM2OD1zLkG4PFch|ryP NV;1Z2l2W0GQR1XS
BE-13 MoqwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkLSTWM2OD1zLkK3OFE3KM7:TR?= MnHPV2FPT0WU
ACN MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX[2UZNsUUN3ME2xMlU2ODd5IN88US=> M1yxbnNCVkeHUh?=
A204 M3\0Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUXUWWFbUUN3ME2xMlU4OjB3IN88US=> MXXTRW5ITVJ?
HOP-62 NH\HZW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWfJR|UxRTFwOEKwO|ch|ryP NIDnUJlUSU6JRWK=
H9 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYDJR|UxRTJwN{O3PVMh|ryP NHnOOmVUSU6JRWK=
HCC1806 NF3mU45Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1rEc2lEPTB;Mj63OFMzPyEQvF2= NXvufllFW0GQR1XS
NOS-1 NYPMVpVST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M132bWlEPTB;Mj64O|ExOiEQvF2= M4fncXNCVkeHUh?=
RS4-11 M2jLUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEnzOJhKSzVyPUKuPVA3OjNizszN M2jzTXNCVkeHUh?=
JAR NFHsRXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnvZTWM2OD1{LkmyNFg1KM7:TR?= NWi3TGI2W0GQR1XS
T98G MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIHJbZlKSzVyPUOuNFE{OTNizszN MmiwV2FPT0WU
NCI-SNU-1 MkewS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHThWW1KSzVyPUOuOFAxQTJizszN M4fFVnNCVkeHUh?=
SK-MEL-1 M2eyRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3LtVGlEPTB;Mz60N|AzQSEQvF2= M1\xe3NCVkeHUh?=
L-363 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M37LR2lEPTB;Mz62NVExPyEQvF2= NXH2R41iW0GQR1XS
SW982 NHzkboVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4nCfWlEPTB;Mz62OFE3QSEQvF2= MWTTRW5ITVJ?
HT-1080 NYexZ5ZoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoL6TWM2OD1|LkmxO|c2KM7:TR?= MU\TRW5ITVJ?
G-402 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHWxR2JKSzVyPUSuN|EzODNizszN MV\TRW5ITVJ?
HOS M2Tj[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkDHTWM2OD12LkiwNlgzKM7:TR?= MXnTRW5ITVJ?
SK-NEP-1 NH33dINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVPw[m5sUUN3ME20Mlg{OTlzIN88US=> NHWxOnBUSU6JRWK=
HAL-01 NILke|lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mo\aTWM2OD12Lki4NlQzKM7:TR?= NF;5WnBUSU6JRWK=
SBC-1 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmDtTWM2OD12LkmwPVA4KM7:TR?= MYfTRW5ITVJ?
CTV-1 NHPJNnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHPadFNKSzVyPUWuOFg6OzhizszN M3\GeXNCVkeHUh?=
LCLC-103H NVPk[mR[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFW4R4NKSzVyPUWuO|c1PzFizszN M3r5fHNCVkeHUh?=
RVH-421 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4ezUmlEPTB;NT63O|U{PiEQvF2= M2PBSnNCVkeHUh?=
K-562 NFr3R4JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXrJR|UxRTVwOUCzOkDPxE1? MnToV2FPT0WU
CAL-33 MkTJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUPTb5RzUUN3ME22MlMyOzV7IN88US=> MnzGV2FPT0WU
MDA-MB-361 M1;xR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnSzTWM2OD14LkOzOlk6KM7:TR?= M{nWd3NCVkeHUh?=
IGROV-1 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{f3bmlEPTB;Nj60O|E6OSEQvF2= M2\hUXNCVkeHUh?=
NY MnzTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVTJR|UxRTZwNUO1PVkh|ryP NE\odGtUSU6JRWK=
Ramos-2G6-4C10 NIfTcGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXLJR|UxRTZwNk[5N|Eh|ryP MVzTRW5ITVJ?
HuO9 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUj1SWp3UUN3ME22Mlc{QTZ2IN88US=> MmHjV2FPT0WU
MS-1 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlPxTWM2OD15LkGxPVU{KM7:TR?= MWDTRW5ITVJ?
RPMI-8226 NXroV|lXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV3lflJnUUN3ME23MlI5Ojh5IN88US=> M4\scHNCVkeHUh?=
HDLM-2 NXq0OmQxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkT4TWM2OD15LkSwNVQ6KM7:TR?= MV7TRW5ITVJ?
D-566MG M3npdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmPuTWM2OD15LkS3NVU2KM7:TR?= M{\5OnNCVkeHUh?=
SK-MEL-24 MlvvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml;PTWM2OD15Lk[zN|kzKM7:TR?= Mlv1V2FPT0WU
COLO-679 M1[yUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYXiT2pkUUN3ME23Mlk5PjdzIN88US=> NWDlNm8xW0GQR1XS
EW-13 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHrucG1KSzVyPUiuN|IxPTRizszN MmDYV2FPT0WU
A388 NHTZfFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2TzTWlEPTB;OD6zPFQ5OSEQvF2= MUnTRW5ITVJ?
UM-UC-3 MkjxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWrJR|UxRThwNEO5OVYh|ryP MX7TRW5ITVJ?
NUGC-3 M2S3RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3XOV2lEPTB;OD61N|U5OiEQvF2= NVi2W5Z6W0GQR1XS
COLO-668 NV3xdpRjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlfGTWM2OD16LkW5OFkyKM7:TR?= M4T2WXNCVkeHUh?=
MOLT-4 NELSTnBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHnWS4dKSzVyPUiuOlI{PTNizszN M3S5VnNCVkeHUh?=
D-423MG NH3WO4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4\IS2lEPTB;OD64N|c2PiEQvF2= NH7OU5VUSU6JRWK=
CTB-1 NYGxeYZjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXvJR|UxRThwOEexNlgh|ryP M{fnN3NCVkeHUh?=
BCPAP NWLXOpJDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYLJR|UxRTlwMEK1OlIh|ryP NUfKSHZiW0GQR1XS
GCT NEixeHFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnTrTWM2OD17LkC5PFMyKM7:TR?= M1jiRXNCVkeHUh?=
ACHN MoGzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml7uTWM2OD17LkKzOlMzKM7:TR?= M2rsenNCVkeHUh?=
KYSE-520 M1HKd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGC4b3BKSzVyPUmuN|M1QDJizszN M2jKVXNCVkeHUh?=
LB771-HNC NXfFOXgzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MorsTWM2OD17Lke2OFk4KM7:TR?= MUjTRW5ITVJ?
MLMA NVLDOGczT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{WxfGlEPTB;MUCuNFE{OiEQvF2= MoSxV2FPT0WU
HEC-1 NFHqSFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{G1S2lEPTB;MUCuNlgxPCEQvF2= MnTjV2FPT0WU
HL-60 NXvXb4o5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV3sRZc{UUN3ME2xNE43QDV|IN88US=> M3rVbXNCVkeHUh?=
A101D M1L6dGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYPJR|UxRTFyLki5NlMh|ryP NGrHWIlUSU6JRWK=
A2058 NWPGdI5PT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHG2bFdKSzVyPUGwMlkzPDVizszN MVvTRW5ITVJ?
KARPAS-45 NWTib4FZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX\JR|UxRTFzLkC2N|Uh|ryP MonHV2FPT0WU
697 NV;JW2hFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlK2TWM2OD1zMT6yNVAyKM7:TR?= NF\I[4VUSU6JRWK=
NCI-N87 Mn;iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2W0XmlEPTB;MUGuO|c{OSEQvF2= NFvKSo5USU6JRWK=
DSH1 NWT1R3puT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2Xve2lEPTB;MUGuO|k2OyEQvF2= M4TLZXNCVkeHUh?=
HLE NIWxZ5JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4jJfmlEPTB;MUGuPFg{QSEQvF2= MWPTRW5ITVJ?
NCI-H720 NXX1cXpqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3\2SWlEPTB;MUKuOlgxOSEQvF2= M3\5PHNCVkeHUh?=
EW-3 NWH0OpdRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIfnXVRKSzVyPUGyMlk{ODdizszN M4W2UHNCVkeHUh?=
AGS M{jsZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFTIfYZKSzVyPUGzMlA{PTFizszN M1XyNHNCVkeHUh?=
ES5 NVP4SFBMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHv5TGRKSzVyPUGzMlA2OTJizszN MUPTRW5ITVJ?
DB NX;P[mE2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUfJR|UxRTF|LkOyOVYh|ryP NEXZZWJUSU6JRWK=
A4-Fuk MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXvJR|UxRTF|LkSxNFIh|ryP NFjCXWVUSU6JRWK=
A427 Mlv6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVXJR|UxRTF|LkS5O|Ih|ryP NHHFPIhUSU6JRWK=
MN-60 MlfhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml7RTWM2OD1zMz61PFQ{KM7:TR?= M4j0TnNCVkeHUh?=
HCC2218 NWLQWIJZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NY\le|BZUUN3ME2xN{42QDV4IN88US=> M3jPVnNCVkeHUh?=
MV-4-11 M1[3T2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEnBVpRKSzVyPUGzMlgyOzdizszN MmDBV2FPT0WU
GI-1 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUTJR|UxRTF2LkGxPFQh|ryP NEG2cYJUSU6JRWK=
JVM-3 M{fvSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NELJR4VKSzVyPUG0MlI3PTZizszN M122W3NCVkeHUh?=
NCI-H2029 NGLhUo5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3OzPWlEPTB;MUSuNlczPyEQvF2= Ml3JV2FPT0WU
TE-12 NHnTV|NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoPDTWM2OD1zND62NFQ3KM7:TR?= NIDOVohUSU6JRWK=
WM-115 NXzDNpY4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFLTdpFKSzVyPUG1MlU3QDNizszN NEX5b3BUSU6JRWK=
BB65-RCC NVWzNpc4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1;VXmlEPTB;MU[uNFI1OSEQvF2= Mn:3V2FPT0WU
NCI-H1693 MofuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4HVWGlEPTB;MU[uN|gxOiEQvF2= NWfp[ZkzW0GQR1XS
KARPAS-299 NHK5dWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX25c21PUUN3ME2xOk43OjB|IN88US=> NHPZUVhUSU6JRWK=
UACC-257 NEHRPJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoLjTWM2OD1zNz6wOVgzKM7:TR?= M{S0UHNCVkeHUh?=
RKO M4TGdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1HaRmlEPTB;MUeuOlQ{OyEQvF2= Mle0V2FPT0WU
HT-29 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYPJR|UxRTF5Lke4PFkh|ryP NVH5TGF5W0GQR1XS
ES7 M2rsU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEn1R4ZKSzVyPUG4MlEyOjJizszN MnPPV2FPT0WU
DEL Mn\ZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2rCUWlEPTB;MUiuN|E4OiEQvF2= NHzo[GZUSU6JRWK=
BT-549 NUjLZllHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFjCVnZKSzVyPUG4MlQxQTJizszN NFzr[Y5USU6JRWK=
NCI-H1755 Ml;rS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH;ycpZKSzVyPUG4MlU4OjNizszN NXW3V4xpW0GQR1XS
HCE-T M4\HOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2PGV2lEPTB;MUiuPFM1OSEQvF2= NG[3e|JUSU6JRWK=
LU-139 NFPvc2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYTVdZV7UUN3ME2xPU4xPDV6IN88US=> MlfXV2FPT0WU
ECC10 NWPKSWprT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoDpTWM2OD1zOT6yOFc2KM7:TR?= M17JOnNCVkeHUh?=
769-P MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWnJR|UxRTF7Lk[zN|Uh|ryP MnS2V2FPT0WU
BALL-1 NUezOVhoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4DMXmlEPTB;MUmuOlc4PSEQvF2= M3LwdXNCVkeHUh?=
LXF-289 NEDCcVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXHJR|UxRTF7Lki5O|kh|ryP NGTTOodUSU6JRWK=
TYK-nu NGfSTVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmLQTWM2OD1zOT65N|E2KM7:TR?= NFPieppUSU6JRWK=
NCI-H630 NEHEV5pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV;FXlNOUUN3ME2xPU46Ozd6IN88US=> MkX4V2FPT0WU
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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 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
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