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 Mnf5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXjJR|UxRTBwMECwNVQ1KM7:TR?= NFjzTJhUSU6JRWK=
KU812 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MU\JR|UxRTBwMECyOFgh|ryP NXn4RlZXW0GQR1XS
EM-2 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWDNc4pzUUN3ME2wMlAxPDFizszN NHXKdWNUSU6JRWK=
LAMA-84 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXzJR|UxRTBwMEC0PUDPxE1? M1vnVHNCVkeHUh?=
MEG-01 M1Hwemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4\3PGlEPTB;MD6wNFgzQCEQvF2= MXTTRW5ITVJ?
BV-173 MoHWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYrJR|UxRTBwMEGwPFkh|ryP M4n1fXNCVkeHUh?=
KASUMI-1 NUD6d|FOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml7DTWM2OD1yLkCyOFE{KM7:TR?= M2fXdXNCVkeHUh?=
NB7 NWLtcHM6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3vKNmlEPTB;MD6xN|Q{QSEQvF2= M3PrVXNCVkeHUh?=
BHT-101 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NI\VXpNKSzVyPUCuOlQzPjNizszN NF7yR45USU6JRWK=
CGTH-W-1 MkHIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX;JR|UxRTBwNkS4O{DPxE1? NInoSXhUSU6JRWK=
HMV-II M1rpUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVHJR|UxRTBwN{S4O|Qh|ryP MWfTRW5ITVJ?
NKM-1 NWnwVXhmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHTycolKSzVyPUCuPVAyPSEQvF2= NGLDcJRUSU6JRWK=
LB2241-RCC NET1fIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWTsfZVJUUN3ME2xMlAzOjJ6IN88US=> NYLB[ZRTW0GQR1XS
NCI-H1703 M{CzOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{HhVGlEPTB;MT6xPFg4KM7:TR?= MmTLV2FPT0WU
BE-13 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFzXVFdKSzVyPUGuNlc1OTZizszN M4rYNHNCVkeHUh?=
ACN NW\Gclc5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoDHTWM2OD1zLkW1NFc4KM7:TR?= Mn6yV2FPT0WU
A204 NEfycVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX;VUIxYUUN3ME2xMlU4OjB3IN88US=> NUfueVdiW0GQR1XS
HOP-62 NHHKN5VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MY\JR|UxRTFwOEKwO|ch|ryP MWXTRW5ITVJ?
H9 MoDsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1u5NmlEPTB;Mj63N|c6OyEQvF2= M4HaTXNCVkeHUh?=
HCC1806 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV\JR|UxRTJwN{SzNlch|ryP Mn7VV2FPT0WU
NOS-1 NEHtPW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnuzTWM2OD1{Lki3NVAzKM7:TR?= MmKzV2FPT0WU
RS4-11 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVrJR|UxRTJwOUC2NlMh|ryP MXjTRW5ITVJ?
JAR MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVzZeHlwUUN3ME2yMlkzODh2IN88US=> NInw[FhUSU6JRWK=
T98G MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2XKfWlEPTB;Mz6wNVMyOyEQvF2= M{S0bnNCVkeHUh?=
NCI-SNU-1 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{HZTmlEPTB;Mz60NFA6OiEQvF2= MX;TRW5ITVJ?
SK-MEL-1 NGWyN5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NESyVpdKSzVyPUOuOFMxOjlizszN NYLaeG9iW0GQR1XS
L-363 M4\3cGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWi1W2JxUUN3ME2zMlYyOTB5IN88US=> M{fIOXNCVkeHUh?=
SW982 NI\aNnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEDHRVhKSzVyPUOuOlQyPjlizszN MYfTRW5ITVJ?
HT-1080 NFTscHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYHrc2RPUUN3ME2zMlkyPzd3IN88US=> NGLXXHVUSU6JRWK=
G-402 NVjMT2V2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGnKdW1KSzVyPUSuN|EzODNizszN NXnwSm9vW0GQR1XS
HOS MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWLJR|UxRTRwOECyPFIh|ryP MX3TRW5ITVJ?
SK-NEP-1 NWnEOYQ5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoLFTWM2OD12LkizNVkyKM7:TR?= MlLUV2FPT0WU
HAL-01 M2H2fGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIPhOo9KSzVyPUSuPFgzPDJizszN NWX3W5l5W0GQR1XS
SBC-1 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVvJR|UxRTRwOUC5NFch|ryP MUPTRW5ITVJ?
CTV-1 MnzCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIjUTmZKSzVyPUWuOFg6OzhizszN M3LsVXNCVkeHUh?=
LCLC-103H MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3[zOmlEPTB;NT63O|Q4OSEQvF2= NFX3bJNUSU6JRWK=
RVH-421 M{DyOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M13zeWlEPTB;NT63O|U{PiEQvF2= NXXLc4J{W0GQR1XS
K-562 NGjqeZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFHUUHlKSzVyPUWuPVA{PiEQvF2= Mlv0V2FPT0WU
CAL-33 NVLneWJTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2PLc2lEPTB;Nj6zNVM2QSEQvF2= Mmm0V2FPT0WU
MDA-MB-361 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFv6U2RKSzVyPU[uN|M3QTlizszN MXvTRW5ITVJ?
IGROV-1 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2W0WmlEPTB;Nj60O|E6OSEQvF2= M3rxfXNCVkeHUh?=
NY NHf5cFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGXhe4xKSzVyPU[uOVM2QTlizszN NV7vflc3W0GQR1XS
Ramos-2G6-4C10 MornS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXfW[3RkUUN3ME22MlY3QTNzIN88US=> M4rLenNCVkeHUh?=
HuO9 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUnTVmtuUUN3ME22Mlc{QTZ2IN88US=> NYfT[nV5W0GQR1XS
MS-1 MlniS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4\IV2lEPTB;Nz6xNVk2OyEQvF2= NH3ifFFUSU6JRWK=
RPMI-8226 NVj5NWt7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVfJR|UxRTdwMkiyPFch|ryP MlPjV2FPT0WU
HDLM-2 NUPtUIVrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2DOVWlEPTB;Nz60NFE1QSEQvF2= M3HR[XNCVkeHUh?=
D-566MG MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGPM[JdKSzVyPUeuOFcyPTVizszN NInROYtUSU6JRWK=
SK-MEL-24 NIr3SJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEPJbopKSzVyPUeuOlM{QTJizszN MVrTRW5ITVJ?
COLO-679 M1;3OGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYLMN5RVUUN3ME23Mlk5PjdzIN88US=> NEHrcZdUSU6JRWK=
EW-13 M2\0Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVTJR|UxRThwM{KwOVQh|ryP NVLpbWJZW0GQR1XS
A388 NXzCN3RYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXLtWlZNUUN3ME24MlM5PDhzIN88US=> MkXpV2FPT0WU
UM-UC-3 MmXUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFfDOXZKSzVyPUiuOFM6PTZizszN NGDMfoZUSU6JRWK=
NUGC-3 NFrFT5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGrLTWxKSzVyPUiuOVM2QDJizszN M{\5[XNCVkeHUh?=
COLO-668 NH[zVm1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkH2TWM2OD16LkW5OFkyKM7:TR?= NH6wZ4FUSU6JRWK=
MOLT-4 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH\lZo9KSzVyPUiuOlI{PTNizszN MlXHV2FPT0WU
D-423MG MorLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVrJR|UxRThwOEO3OVYh|ryP NVPV[mJ2W0GQR1XS
CTB-1 MlHXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnvMTWM2OD16Lki3NVI5KM7:TR?= NVnLOHdzW0GQR1XS
BCPAP M1rLO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXvMTWVGUUN3ME25MlAzPTZ{IN88US=> NYHJ[lU2W0GQR1XS
GCT MmLVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmTTTWM2OD17LkC5PFMyKM7:TR?= NVrwXmlMW0GQR1XS
ACHN NX\VXo9zT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX3QUlVXUUN3ME25MlI{PjN{IN88US=> NHnZTGJUSU6JRWK=
KYSE-520 NGr6N49Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MliwTWM2OD17LkOzOFgzKM7:TR?= MWjTRW5ITVJ?
LB771-HNC NG\WR2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4H3VWlEPTB;OT63OlQ6PyEQvF2= NILKSoNUSU6JRWK=
MLMA MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4HjUWlEPTB;MUCuNFE{OiEQvF2= M4\ESHNCVkeHUh?=
HEC-1 M{Dkdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYXJR|UxRTFyLkK4NFQh|ryP MmK3V2FPT0WU
HL-60 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH3OZ5lKSzVyPUGwMlY5PTNizszN MkWyV2FPT0WU
A101D MnrIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWXu[HJqUUN3ME2xNE45QTJ|IN88US=> NHnrNpZUSU6JRWK=
A2058 MofyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmnhTWM2OD1zMD65NlQ2KM7:TR?= M2nmSHNCVkeHUh?=
KARPAS-45 M{LjWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYXJR|UxRTFzLkC2N|Uh|ryP M2jQZ3NCVkeHUh?=
697 Ml7SS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MorHTWM2OD1zMT6yNVAyKM7:TR?= NUnyT3J4W0GQR1XS
NCI-N87 NEfMWXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWXJR|UxRTFzLke3N|Eh|ryP Mn6wV2FPT0WU
DSH1 NVX4TGc1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXXLO21MUUN3ME2xNU44QTV|IN88US=> MXnTRW5ITVJ?
HLE M4\1RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWjiPFU4UUN3ME2xNU45QDN7IN88US=> MY\TRW5ITVJ?
NCI-H720 NXfJbmNpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mlr2TWM2OD1zMj62PFAyKM7:TR?= MljaV2FPT0WU
EW-3 NU\QWXBST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYDJR|UxRTF{LkmzNFch|ryP M2rqfXNCVkeHUh?=
AGS NWnLXmRLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXH1bm9uUUN3ME2xN{4xOzVzIN88US=> NX7Hfms4W0GQR1XS
ES5 NVXjZmJMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUHJR|UxRTF|LkC1NVIh|ryP NWGxTHp{W0GQR1XS
DB MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWjMVnR3UUN3ME2xN{4{OjV4IN88US=> MlXPV2FPT0WU
A4-Fuk MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NECwdpRKSzVyPUGzMlQyODJizszN MXzTRW5ITVJ?
A427 NWPwOop6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlHlTWM2OD1zMz60PVczKM7:TR?= M2nEUHNCVkeHUh?=
MN-60 Ml\xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnvnTWM2OD1zMz61PFQ{KM7:TR?= MXHTRW5ITVJ?
HCC2218 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1rScWlEPTB;MUOuOVg2PiEQvF2= MkDEV2FPT0WU
MV-4-11 NVm4N|dET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFzi[JJKSzVyPUGzMlgyOzdizszN NGHGd2xUSU6JRWK=
GI-1 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIXibWNKSzVyPUG0MlEyQDRizszN NEG0S|lUSU6JRWK=
JVM-3 NXjyWYV5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2nxNmlEPTB;MUSuNlY2PiEQvF2= NVHifFFnW0GQR1XS
NCI-H2029 M{nNR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFi3dIZKSzVyPUG0MlI4OjdizszN MYXTRW5ITVJ?
TE-12 M371dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4DLTWlEPTB;MUSuOlA1PiEQvF2= NX;0PIxxW0GQR1XS
WM-115 M{fhc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVPJNJA4UUN3ME2xOU42Pjh|IN88US=> NIDHOZhUSU6JRWK=
BB65-RCC NVHxR5lVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4\Ud2lEPTB;MU[uNFI1OSEQvF2= MXXTRW5ITVJ?
NCI-H1693 M4jzTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFrobYpKSzVyPUG2MlM5ODJizszN MYLTRW5ITVJ?
KARPAS-299 NXS3VnFLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MojrTWM2OD1zNj62NlA{KM7:TR?= NHy3[|lUSU6JRWK=
UACC-257 M1PnfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4r2cmlEPTB;MUeuNFU5OiEQvF2= NHXqN4pUSU6JRWK=
RKO NGmwRpNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHmwUZpKSzVyPUG3MlY1OzNizszN MYLTRW5ITVJ?
HT-29 Ml7aS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVrWXm8xUUN3ME2xO{44QDh7IN88US=> M{LhXnNCVkeHUh?=
ES7 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{XBXWlEPTB;MUiuNVEzOiEQvF2= MVrTRW5ITVJ?
DEL NYfHPJJIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmT2TWM2OD1zOD6zNVczKM7:TR?= NXfwS21ZW0GQR1XS
BT-549 NYTrXlk4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVnOTFBqUUN3ME2xPE41ODl{IN88US=> MYnTRW5ITVJ?
NCI-H1755 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUnJR|UxRTF6LkW3NlMh|ryP MXjTRW5ITVJ?
HCE-T MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIGzPYFKSzVyPUG4Mlg{PDFizszN MVLTRW5ITVJ?
LU-139 NHnJToZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYrn[Ik6UUN3ME2xPU4xPDV6IN88US=> MYLTRW5ITVJ?
ECC10 NYjJNWpWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mm[xTWM2OD1zOT6yOFc2KM7:TR?= M4mxcXNCVkeHUh?=
769-P NGD5O49Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWLJR|UxRTF7Lk[zN|Uh|ryP MXzTRW5ITVJ?
BALL-1 NU\CS3F6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHTNU2RKSzVyPUG5MlY4PzVizszN MnLuV2FPT0WU
LXF-289 Mn[yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEm5S4hKSzVyPUG5Mlg6PzlizszN NEDYNGtUSU6JRWK=
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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
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.

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