Nilotinib (AMN-107)

Catalog No.S1033

Nilotinib (AMN-107) Chemical Structure

Molecular Weight(MW): 529.52

Nilotinib (AMN-107) is a Bcr-Abl inhibitor with IC50 less than 30 nM in Murine myeloid progenitor cells.

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In DMSO USD 91 In stock
USD 70 In stock
USD 210 In stock
USD 470 In stock

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5 Customer Reviews

  • 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

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Biological Activity

Description Nilotinib (AMN-107) is a 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 M3XWPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4DmU2lEPTB;MD6wNFAyPDRizszN NHraPWdUSU6JRWK=
KU812 NVLHUW57T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M13vdmlEPTB;MD6wNFI1QCEQvF2= M{D4VHNCVkeHUh?=
EM-2 MoWwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXzvSYwyUUN3ME2wMlAxPDFizszN MoPhV2FPT0WU
LAMA-84 NGm3N|NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3\IUWlEPTB;MD6wNFQ6KM7:TR?= NFvLTWtUSU6JRWK=
MEG-01 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHfnOHNKSzVyPUCuNFA5OjhizszN NFrJW4lUSU6JRWK=
BV-173 MkPvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnXQTWM2OD1yLkCxNFg6KM7:TR?= M1joSHNCVkeHUh?=
KASUMI-1 M4rqPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV;JR|UxRTBwMEK0NVMh|ryP MlPMV2FPT0WU
NB7 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnPKTWM2OD1yLkGzOFM6KM7:TR?= MXjTRW5ITVJ?
BHT-101 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFjYWGxKSzVyPUCuOlQzPjNizszN M4fXSnNCVkeHUh?=
CGTH-W-1 NELIbFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M13FSmlEPTB;MD62OFg4KM7:TR?= NYHTPJY5W0GQR1XS
HMV-II M2TlZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlnZTWM2OD1yLke0PFc1KM7:TR?= Mn\6V2FPT0WU
NKM-1 NFywcXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEHkN3lKSzVyPUCuPVAyPSEQvF2= MYrTRW5ITVJ?
LB2241-RCC NWLxNmE5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIHW[ppKSzVyPUGuNFIzOjhizszN NVrJNVFSW0GQR1XS
NCI-H1703 NEDXT41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmjNTWM2OD1zLkG4PFch|ryP MmDXV2FPT0WU
BE-13 MnnYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUHaNmZ{UUN3ME2xMlI4PDF4IN88US=> M1nvRnNCVkeHUh?=
ACN NH21PHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWfJR|UxRTFwNUWwO|ch|ryP NVHnV4VNW0GQR1XS
A204 NIXBfHdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mk\YTWM2OD1zLkW3NlA2KM7:TR?= MmHRV2FPT0WU
HOP-62 MkDzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1P4ZWlEPTB;MT64NlA4PyEQvF2= MXfTRW5ITVJ?
H9 M{TUcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml7ZTWM2OD1{LkezO|k{KM7:TR?= NFLxPY9USU6JRWK=
HCC1806 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4DZbGlEPTB;Mj63OFMzPyEQvF2= NIPIVVhUSU6JRWK=
NOS-1 NVL6[4U4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYmybplPUUN3ME2yMlg4OTB{IN88US=> NU\hTY01W0GQR1XS
RS4-11 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXXJR|UxRTJwOUC2NlMh|ryP NGTwfYNUSU6JRWK=
JAR M321cWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn;TTWM2OD1{LkmyNFg1KM7:TR?= M3e3bXNCVkeHUh?=
T98G M13yVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXr2[YF6UUN3ME2zMlAyOzF|IN88US=> MojUV2FPT0WU
NCI-SNU-1 NV3x[49XT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX\JR|UxRTNwNECwPVIh|ryP MWDTRW5ITVJ?
SK-MEL-1 M1e1Omdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHX1R|RKSzVyPUOuOFMxOjlizszN NGfBVWlUSU6JRWK=
L-363 NUnjOo5JT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXfJR|UxRTNwNkGxNFch|ryP Mkm3V2FPT0WU
SW982 NU\Kcm5nT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHq0Nm9KSzVyPUOuOlQyPjlizszN NED1XGFUSU6JRWK=
HT-1080 NH\1TGRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3i2b2lEPTB;Mz65NVc4PSEQvF2= M{LlVXNCVkeHUh?=
G-402 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVfJR|UxRTRwM{GyNFMh|ryP MkG5V2FPT0WU
HOS MlvWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIjHeGtKSzVyPUSuPFAzQDJizszN MnXCV2FPT0WU
SK-NEP-1 NGewe2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MY\JR|UxRTRwOEOxPVEh|ryP NF3NUVRUSU6JRWK=
HAL-01 NUO5ZVJkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWfCOIJwUUN3ME20Mlg5OjR{IN88US=> MWnTRW5ITVJ?
SBC-1 NHW4co1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUjqNWV1UUN3ME20MlkxQTB5IN88US=> M2HETXNCVkeHUh?=
CTV-1 MlL6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF;1SXVKSzVyPUWuOFg6OzhizszN NXi4XJBFW0GQR1XS
LCLC-103H NUi1V3hxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHHIOIFKSzVyPUWuO|c1PzFizszN M3TGfHNCVkeHUh?=
RVH-421 NGrnTY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3u1bWlEPTB;NT63O|U{PiEQvF2= MVfTRW5ITVJ?
K-562 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4f6cWlEPTB;NT65NFM3KM7:TR?= MWrTRW5ITVJ?
CAL-33 NYXhZpZ7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M331PGlEPTB;Nj6zNVM2QSEQvF2= Ml7EV2FPT0WU
MDA-MB-361 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MofFTWM2OD14LkOzOlk6KM7:TR?= MUDTRW5ITVJ?
IGROV-1 M2X2cGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX3IeWVEUUN3ME22MlQ4OTlzIN88US=> MWXTRW5ITVJ?
NY M1XQWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWPJR|UxRTZwNUO1PVkh|ryP NUfrUJRTW0GQR1XS
Ramos-2G6-4C10 NGK2SYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2P3PGlEPTB;Nj62Olk{OSEQvF2= M1PkeXNCVkeHUh?=
HuO9 NUPzenl6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFvv[3hKSzVyPU[uO|M6PjRizszN NX\rfJNxW0GQR1XS
MS-1 Mke0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3vVRWlEPTB;Nz6xNVk2OyEQvF2= NVz3O2ROW0GQR1XS
RPMI-8226 NILi[5pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVjIfpVuUUN3ME23MlI5Ojh5IN88US=> NGjxS2JUSU6JRWK=
HDLM-2 NGLSPYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXLJR|UxRTdwNECxOFkh|ryP MUXTRW5ITVJ?
D-566MG NE\oeVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYX5b5V{UUN3ME23MlQ4OTV3IN88US=> MlzEV2FPT0WU
SK-MEL-24 M{eyOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mm\yTWM2OD15Lk[zN|kzKM7:TR?= M37rcXNCVkeHUh?=
COLO-679 M3HFbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVfncWZrUUN3ME23Mlk5PjdzIN88US=> Mnj0V2FPT0WU
EW-13 M3\hW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVzJR|UxRThwM{KwOVQh|ryP MWLTRW5ITVJ?
A388 MlvzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M13ofWlEPTB;OD6zPFQ5OSEQvF2= M331Z3NCVkeHUh?=
UM-UC-3 M1nYTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NE\LTHhKSzVyPUiuOFM6PTZizszN MmS2V2FPT0WU
NUGC-3 M4jFW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoHDTWM2OD16LkWzOVgzKM7:TR?= NFXLT4RUSU6JRWK=
COLO-668 NEHvS3FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoOyTWM2OD16LkW5OFkyKM7:TR?= M37r[3NCVkeHUh?=
MOLT-4 NU\Tclc2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3PNVWlEPTB;OD62NlM2OyEQvF2= M37UcXNCVkeHUh?=
D-423MG MlT3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWO4UHJIUUN3ME24Mlg{PzV4IN88US=> M37vOnNCVkeHUh?=
CTB-1 MmfQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M33JRmlEPTB;OD64O|EzQCEQvF2= NVfKcVhtW0GQR1XS
BCPAP MoHkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MneyTWM2OD17LkCyOVYzKM7:TR?= NEHhb5FUSU6JRWK=
GCT NH\sWYhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MojmTWM2OD17LkC5PFMyKM7:TR?= MWrTRW5ITVJ?
ACHN NVXzU2hPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn7tTWM2OD17LkKzOlMzKM7:TR?= M3:ydnNCVkeHUh?=
KYSE-520 MnzvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHPY[mxKSzVyPUmuN|M1QDJizszN MXvTRW5ITVJ?
LB771-HNC NWX3VohzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{\0eGlEPTB;OT63OlQ6PyEQvF2= NXHwO|VCW0GQR1XS
MLMA MofaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVPJR|UxRTFyLkCxN|Ih|ryP MkfGV2FPT0WU
HEC-1 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmC0TWM2OD1zMD6yPFA1KM7:TR?= MWLTRW5ITVJ?
HL-60 M13sR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUTZS5JVUUN3ME2xNE43QDV|IN88US=> NWHJXWxbW0GQR1XS
A101D M1Lycmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NImye|JKSzVyPUGwMlg6OjNizszN MX7TRW5ITVJ?
A2058 Ml3qS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4TIZ2lEPTB;MUCuPVI1PSEQvF2= M2HmdHNCVkeHUh?=
KARPAS-45 Mo\oS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkPOTWM2OD1zMT6wOlM2KM7:TR?= NGLUeolUSU6JRWK=
697 NEXlRpVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoPLTWM2OD1zMT6yNVAyKM7:TR?= MXrTRW5ITVJ?
NCI-N87 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGH3XnlKSzVyPUGxMlc4OzFizszN M3[3cnNCVkeHUh?=
DSH1 MnrFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4DIZWlEPTB;MUGuO|k2OyEQvF2= MmG4V2FPT0WU
HLE NVyyfZlFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX2wS2VDUUN3ME2xNU45QDN7IN88US=> MWjTRW5ITVJ?
NCI-H720 NEPQb|lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVTTXWtXUUN3ME2xNk43QDBzIN88US=> MmTDV2FPT0WU
EW-3 NGfEbmxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYLJR|UxRTF{LkmzNFch|ryP NHLHRWhUSU6JRWK=
AGS NGGzTnJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmT4TWM2OD1zMz6wN|UyKM7:TR?= MXzTRW5ITVJ?
ES5 MonBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{PD[2lEPTB;MUOuNFUyOiEQvF2= M1TUb3NCVkeHUh?=
DB NX[wSWM1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2Xjc2lEPTB;MUOuN|I2PiEQvF2= NGP3RY5USU6JRWK=
A4-Fuk M{PKNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NILEVHRKSzVyPUGzMlQyODJizszN M1;4TnNCVkeHUh?=
A427 NYXEdmxOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXf1[XQ4UUN3ME2xN{41QTd{IN88US=> NEnnU5pUSU6JRWK=
MN-60 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkfGTWM2OD1zMz61PFQ{KM7:TR?= M4nTWHNCVkeHUh?=
HCC2218 Mkj2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUfJR|UxRTF|LkW4OVYh|ryP MULTRW5ITVJ?
MV-4-11 MmezS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYnJR|UxRTF|LkixN|ch|ryP M3fD[nNCVkeHUh?=
GI-1 MmHnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmLOTWM2OD1zND6xNVg1KM7:TR?= M4DsNHNCVkeHUh?=
JVM-3 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1vRcWlEPTB;MUSuNlY2PiEQvF2= Mk\aV2FPT0WU
NCI-H2029 NHrQOWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NU\6TZFYUUN3ME2xOE4zPzJ5IN88US=> M3\5ZnNCVkeHUh?=
TE-12 MoLaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVjseXNWUUN3ME2xOE43ODR4IN88US=> NVntdmxPW0GQR1XS
WM-115 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NITUNnhKSzVyPUG1MlU3QDNizszN MX;TRW5ITVJ?
BB65-RCC MlLuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWfCRWR3UUN3ME2xOk4xOjRzIN88US=> MorBV2FPT0WU
NCI-H1693 NXfMWpZuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX\JR|UxRTF4LkO4NFIh|ryP MUHTRW5ITVJ?
KARPAS-299 M3nCcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXG1eVNxUUN3ME2xOk43OjB|IN88US=> NYTFemN1W0GQR1XS
UACC-257 M1zTTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{G5ZmlEPTB;MUeuNFU5OiEQvF2= MkHKV2FPT0WU
RKO M4PXSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M37pRmlEPTB;MUeuOlQ{OyEQvF2= MWLTRW5ITVJ?
HT-29 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkG3TWM2OD1zNz63PFg6KM7:TR?= MUTTRW5ITVJ?
ES7 Mlr1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NG\0SVBKSzVyPUG4MlEyOjJizszN MXPTRW5ITVJ?
DEL MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVH6Oo5TUUN3ME2xPE4{OTd{IN88US=> M{TWeXNCVkeHUh?=
BT-549 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlHVTWM2OD1zOD60NFkzKM7:TR?= NIDzOYdUSU6JRWK=
NCI-H1755 M3vvd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUPJR|UxRTF6LkW3NlMh|ryP NH7C[HlUSU6JRWK=
HCE-T NX3GcXp1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGfsbppKSzVyPUG4Mlg{PDFizszN NHTBOXhUSU6JRWK=
LU-139 NHrweo9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEjX[WpKSzVyPUG5MlA1PThizszN MWDTRW5ITVJ?
ECC10 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFn2XFVKSzVyPUG5MlI1PzVizszN M17zbXNCVkeHUh?=
769-P MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIDFZodKSzVyPUG5MlY{OzVizszN MWDTRW5ITVJ?
BALL-1 NE\UVFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NI\ZeYpKSzVyPUG5MlY4PzVizszN NHO4cG5USU6JRWK=
LXF-289 NEe0ZXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkL0TWM2OD1zOT64PVc6KM7:TR?= NF24NJdUSU6JRWK=
TYK-nu MkTyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVrJR|UxRTF7LkmzNVUh|ryP NHW5c2NUSU6JRWK=
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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
+ 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
+ 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 <1 mg/mL
Ethanol <1 mg/mL
In vivo 4% DMSO+30% PEG 300+5% Tween 80+ddH2O 3mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* 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
NCT02709083 Not yet recruiting Chronic Myelogenous Leukemia|Chronic Myeloid Leukemia|Leukemia Emory University December 2016 Phase 2
NCT01887522 Recruiting Refractory Low-grade Gliomas|Recurrent Low-grade Gliomas Gustave Roussy, Cancer Campus, Grand Paris|Innovative Therapies For Children with Cancer Consortium June 2016 Phase 2
NCT02774512 Not yet recruiting Colon Cancer Institut Bergonié|Novartis Pharmaceuticals May 2016 Phase 0
NCT02611492 Recruiting Philadelphia Chromosome Positive Adult Acute Lymphoblastic Leukemia Assistance Publique - Hôpitaux de Paris April 2016 Phase 3
NCT02602314 Not yet recruiting Chronyc Myeloid Leukemia Gruppo Italiano Malattie EMatologiche dellAdulto March 2016 Phase 4
NCT02546674 Recruiting Chronic Myeloid Leukemia Novartis Pharmaceuticals|Novartis February 2016 Phase 4

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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID