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 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFWyO5ZKSzVyPUCuNFAxOTR2IN88US=> NGna[VhUSU6JRWK=
KU812 NHiwUm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MU\JR|UxRTBwMECyOFgh|ryP Ml\vV2FPT0WU
EM-2 M1XYeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mo\nTWM2OD1yLkCwOFEh|ryP NVqybm1CW0GQR1XS
LAMA-84 M3XFUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoLBTWM2OD1yLkCwOFkh|ryP M2LJTHNCVkeHUh?=
MEG-01 MmrNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV;4eIVHUUN3ME2wMlAxQDJ6IN88US=> NG[ycGNUSU6JRWK=
BV-173 MnrBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWXJR|UxRTBwMEGwPFkh|ryP NYXlV|dFW0GQR1XS
KASUMI-1 MlrvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHTwTJdKSzVyPUCuNFI1OTNizszN NYfRfIdNW0GQR1XS
NB7 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHfVfIhKSzVyPUCuNVM1OzlizszN M1Hi[XNCVkeHUh?=
BHT-101 NVj0SW4{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWK4ZoE6UUN3ME2wMlY1OjZ|IN88US=> NWfQTVdqW0GQR1XS
CGTH-W-1 NHfJSGNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmPoTWM2OD1yLk[0PFch|ryP MVPTRW5ITVJ?
HMV-II NHjUfopIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1fafmlEPTB;MD63OFg4PCEQvF2= NHPo[FlUSU6JRWK=
NKM-1 MlnoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2npWmlEPTB;MD65NFE2KM7:TR?= M{\Cd3NCVkeHUh?=
LB2241-RCC NGTlXVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWXJR|UxRTFwMEKyNlgh|ryP MX3TRW5ITVJ?
NCI-H1703 M3HtWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHXZVopKSzVyPUGuNVg5PyEQvF2= M2fTUXNCVkeHUh?=
BE-13 NFvhUHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NE\pPG9KSzVyPUGuNlc1OTZizszN NHjOOoxUSU6JRWK=
ACN NX23VoRHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX;QXJpGUUN3ME2xMlU2ODd5IN88US=> NXOyRWk5W0GQR1XS
A204 M3vjV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVjxRYc1UUN3ME2xMlU4OjB3IN88US=> MkfQV2FPT0WU
HOP-62 NIrkfZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4LwfGlEPTB;MT64NlA4PyEQvF2= MYXTRW5ITVJ?
H9 M2f5Wmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn73TWM2OD1{LkezO|k{KM7:TR?= Ml\pV2FPT0WU
HCC1806 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHrXPIpKSzVyPUKuO|Q{OjdizszN M2DPXnNCVkeHUh?=
NOS-1 M3nmOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mnm1TWM2OD1{Lki3NVAzKM7:TR?= MnPXV2FPT0WU
RS4-11 M3nwT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NU\GWWVmUUN3ME2yMlkxPjJ|IN88US=> MnzFV2FPT0WU
JAR MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4TZdWlEPTB;Mj65NlA5PCEQvF2= MlqyV2FPT0WU
T98G NULqZWVpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml;FTWM2OD1|LkCxN|E{KM7:TR?= M3flTnNCVkeHUh?=
NCI-SNU-1 MmXRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmHYTWM2OD1|LkSwNFkzKM7:TR?= M4XWcXNCVkeHUh?=
SK-MEL-1 M4\2fGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVTJR|UxRTNwNEOwNlkh|ryP M1PCXHNCVkeHUh?=
L-363 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml;ZTWM2OD1|Lk[xNVA4KM7:TR?= M33JXnNCVkeHUh?=
SW982 NEmyT4JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF:zcodKSzVyPUOuOlQyPjlizszN MXXTRW5ITVJ?
HT-1080 NFOzPWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2C5emlEPTB;Mz65NVc4PSEQvF2= M3;zOHNCVkeHUh?=
G-402 MoXUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWrJR|UxRTRwM{GyNFMh|ryP NV74bHNSW0GQR1XS
HOS NF:wcXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWHJR|UxRTRwOECyPFIh|ryP NIr1[5dUSU6JRWK=
SK-NEP-1 M1rsNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmrlTWM2OD12LkizNVkyKM7:TR?= MXjTRW5ITVJ?
HAL-01 NUXVNGhoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1;4TmlEPTB;ND64PFI1OiEQvF2= NETk[|ZUSU6JRWK=
SBC-1 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MojwTWM2OD12LkmwPVA4KM7:TR?= NVWz[XFLW0GQR1XS
CTV-1 NXuwNGVCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH3xcWhKSzVyPUWuOFg6OzhizszN MmfCV2FPT0WU
LCLC-103H M{j6WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFvYfVFKSzVyPUWuO|c1PzFizszN Ml\1V2FPT0WU
RVH-421 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUTrSIRSUUN3ME21Mlc4PTN4IN88US=> M4LWOHNCVkeHUh?=
K-562 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{L5ZmlEPTB;NT65NFM3KM7:TR?= MVPTRW5ITVJ?
CAL-33 M3\F[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlnBTWM2OD14LkOxN|U6KM7:TR?= NHrLNWlUSU6JRWK=
MDA-MB-361 NHPBRo5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWjzVJc{UUN3ME22MlM{Pjl7IN88US=> M1;N[XNCVkeHUh?=
IGROV-1 MlrpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIW3PZpKSzVyPU[uOFcyQTFizszN NYH1No14W0GQR1XS
NY NYnhZpNvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVnK[Gp6UUN3ME22MlU{PTl7IN88US=> NX7HbWxTW0GQR1XS
Ramos-2G6-4C10 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1W4V2lEPTB;Nj62Olk{OSEQvF2= MXLTRW5ITVJ?
HuO9 M2LFV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXnBNYRDUUN3ME22Mlc{QTZ2IN88US=> MUHTRW5ITVJ?
MS-1 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWTJR|UxRTdwMUG5OVMh|ryP Mk[wV2FPT0WU
RPMI-8226 M3iwVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmHVTWM2OD15LkK4Nlg4KM7:TR?= MY\TRW5ITVJ?
HDLM-2 Mn3vS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUTiRpc4UUN3ME23MlQxOTR7IN88US=> MnjFV2FPT0WU
D-566MG M3XDT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mo\CTWM2OD15LkS3NVU2KM7:TR?= MW\TRW5ITVJ?
SK-MEL-24 NVLUXHltT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXPJR|UxRTdwNkOzPVIh|ryP M1zRZXNCVkeHUh?=
COLO-679 MlftS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3i2NWlEPTB;Nz65PFY4OSEQvF2= MUPTRW5ITVJ?
EW-13 NXOydHJvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGXWZ4ZKSzVyPUiuN|IxPTRizszN NEnxTYFUSU6JRWK=
A388 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV;mR2ZEUUN3ME24MlM5PDhzIN88US=> MXLTRW5ITVJ?
UM-UC-3 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2rvWmlEPTB;OD60N|k2PiEQvF2= NWHaTJlQW0GQR1XS
NUGC-3 MoDhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkLiTWM2OD16LkWzOVgzKM7:TR?= NYTlZmxUW0GQR1XS
COLO-668 NWDHWGNLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{S4NmlEPTB;OD61PVQ6OSEQvF2= NHLWcZFUSU6JRWK=
MOLT-4 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{Sxd2lEPTB;OD62NlM2OyEQvF2= Mmr5V2FPT0WU
D-423MG MnfOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYXJR|UxRThwOEO3OVYh|ryP MYrTRW5ITVJ?
CTB-1 NILB[m9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnzCTWM2OD16Lki3NVI5KM7:TR?= MnfiV2FPT0WU
BCPAP NEO4WI9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NY\qN3VPUUN3ME25MlAzPTZ{IN88US=> NIPuZ25USU6JRWK=
GCT M2LE[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MorsTWM2OD17LkC5PFMyKM7:TR?= M1PEW3NCVkeHUh?=
ACHN NY\TWIFHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGnEUHhKSzVyPUmuNlM3OzJizszN MYrTRW5ITVJ?
KYSE-520 NHH5[mhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYXJR|UxRTlwM{O0PFIh|ryP MWnTRW5ITVJ?
LB771-HNC NGnmcpRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3vEUWlEPTB;OT63OlQ6PyEQvF2= M2POcnNCVkeHUh?=
MLMA MlPwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NULl[o9uUUN3ME2xNE4xOTN{IN88US=> NX3O[JFiW0GQR1XS
HEC-1 MnP0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWjJR|UxRTFyLkK4NFQh|ryP MVjTRW5ITVJ?
HL-60 NE\od5VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIPDbVRKSzVyPUGwMlY5PTNizszN M3\TOXNCVkeHUh?=
A101D MnXYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIXUdpRKSzVyPUGwMlg6OjNizszN NWfkTZpkW0GQR1XS
A2058 MnXVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVHjbXNwUUN3ME2xNE46OjR3IN88US=> NHq4fW5USU6JRWK=
KARPAS-45 Mo\KS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MorwTWM2OD1zMT6wOlM2KM7:TR?= NF;6SoFUSU6JRWK=
697 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXzJR|UxRTFzLkKxNFEh|ryP MoTJV2FPT0WU
NCI-N87 Mlq0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFm4enpKSzVyPUGxMlc4OzFizszN M4LXenNCVkeHUh?=
DSH1 NUX2fIFbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYTDbppLUUN3ME2xNU44QTV|IN88US=> Mnu2V2FPT0WU
HLE NFfYTWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Moq4TWM2OD1zMT64PFM6KM7:TR?= M1fuTXNCVkeHUh?=
NCI-H720 NVjDWo9lT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWfZUFZbUUN3ME2xNk43QDBzIN88US=> NH;lXnlUSU6JRWK=
EW-3 M2nJN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIjVXIpKSzVyPUGyMlk{ODdizszN NVXVW5R5W0GQR1XS
AGS NYi4OHFqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn7WTWM2OD1zMz6wN|UyKM7:TR?= NULtVWpsW0GQR1XS
ES5 M4fYcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1ft[GlEPTB;MUOuNFUyOiEQvF2= MlfWV2FPT0WU
DB MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHPlbIRKSzVyPUGzMlMzPTZizszN NXGxZ3l7W0GQR1XS
A4-Fuk NV3m[nh7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVzJR|UxRTF|LkSxNFIh|ryP MVvTRW5ITVJ?
A427 M363Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mnr0TWM2OD1zMz60PVczKM7:TR?= NYHFTGJHW0GQR1XS
MN-60 NF;2VpRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1LpdWlEPTB;MUOuOVg1OyEQvF2= NET2VWVUSU6JRWK=
HCC2218 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3nmdmlEPTB;MUOuOVg2PiEQvF2= Mn71V2FPT0WU
MV-4-11 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHftTWJKSzVyPUGzMlgyOzdizszN NXjUfHpFW0GQR1XS
GI-1 Mnn3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV7JR|UxRTF2LkGxPFQh|ryP M3fVUXNCVkeHUh?=
JVM-3 M{jRNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYDJR|UxRTF2LkK2OVYh|ryP MlvIV2FPT0WU
NCI-H2029 M1vFTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlrrTWM2OD1zND6yO|I4KM7:TR?= MVnTRW5ITVJ?
TE-12 M17sRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXKyWpRSUUN3ME2xOE43ODR4IN88US=> M1LJT3NCVkeHUh?=
WM-115 M2[xXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHzsd25KSzVyPUG1MlU3QDNizszN MlHJV2FPT0WU
BB65-RCC M4CxVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4PL[GlEPTB;MU[uNFI1OSEQvF2= Mnv6V2FPT0WU
NCI-H1693 NFvPPVdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYnJR|UxRTF4LkO4NFIh|ryP NUjpZ2lQW0GQR1XS
KARPAS-299 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEK5NZpKSzVyPUG2MlYzODNizszN Mn7FV2FPT0WU
UACC-257 NH;XfItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1LYR2lEPTB;MUeuNFU5OiEQvF2= MYjTRW5ITVJ?
RKO M{f4VGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX;kSYo4UUN3ME2xO{43PDN|IN88US=> MXvTRW5ITVJ?
HT-29 M2fkR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX\JR|UxRTF5Lke4PFkh|ryP M2fHOXNCVkeHUh?=
ES7 NWDjV3VvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4Xhc2lEPTB;MUiuNVEzOiEQvF2= NUHDfVRFW0GQR1XS
DEL NGXVNWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M36yUWlEPTB;MUiuN|E4OiEQvF2= M1XKeHNCVkeHUh?=
BT-549 MlriS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFjTTlRKSzVyPUG4MlQxQTJizszN NYjXOZdLW0GQR1XS
NCI-H1755 NWfsOWR7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF7PWm9KSzVyPUG4MlU4OjNizszN M3O5c3NCVkeHUh?=
HCE-T MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1rNOGlEPTB;MUiuPFM1OSEQvF2= MnO5V2FPT0WU
LU-139 NYfGfVM2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlL3TWM2OD1zOT6wOFU5KM7:TR?= NXH4WlJ4W0GQR1XS
ECC10 MlfwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYfzVGRWUUN3ME2xPU4zPDd3IN88US=> MmDGV2FPT0WU
769-P MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWDJR|UxRTF7Lk[zN|Uh|ryP MXnTRW5ITVJ?
BALL-1 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX7JR|UxRTF7Lk[3O|Uh|ryP MlrjV2FPT0WU
LXF-289 M1;6[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWq4fIpvUUN3ME2xPU45QTd7IN88US=> MYHTRW5ITVJ?
TYK-nu MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUnJR|UxRTF7LkmzNVUh|ryP MkfWV2FPT0WU
NCI-H630 Mn;WS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWPObYlYUUN3ME2xPU46Ozd6IN88US=> NXP3ZnoxW0GQR1XS
EW-18 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVvJR|UxRTJyLkO4NFIh|ryP 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 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

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

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Molecular Weight Calculator

Molecular Weight Calculator

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Mass Concentration Volume Molecular Weight

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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID