Nilotinib (AMN-107)

For research use only.

Catalog No.S1033

92 publications

Nilotinib (AMN-107) Chemical Structure

CAS No. 641571-10-0

Nilotinib (AMN-107) is a selective Bcr-Abl inhibitor with IC50 less than 30 nM in Murine myeloid progenitor cells. Nilotinib induces autophagy through AMPK activition.

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Selleck's Nilotinib (AMN-107) has been cited by 92 publications

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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. Nilotinib induces autophagy through AMPK activition.
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 NVTC[HVPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFS2O4ZKSzVyPUCuNFAxOTR2IN88US=> MXPTRW5ITVJ?
KU812 M2jMcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVnJR|UxRTBwMECyOFgh|ryP Mn;2V2FPT0WU
EM-2 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1nXb2lEPTB;MD6wNFQyKM7:TR?= NWjqO4xMW0GQR1XS
LAMA-84 MmWxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{O4ZmlEPTB;MD6wNFQ6KM7:TR?= NVLTNYRPW0GQR1XS
MEG-01 M3TUe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmThTWM2OD1yLkCwPFI5KM7:TR?= MoDjV2FPT0WU
BV-173 NHrTeplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYjJR|UxRTBwMEGwPFkh|ryP M1\wTHNCVkeHUh?=
KASUMI-1 NH:3OZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{j0dmlEPTB;MD6wNlQyOyEQvF2= MVXTRW5ITVJ?
NB7 NXXBZoZ7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYLjbnNCUUN3ME2wMlE{PDN7IN88US=> NF7Kc4JUSU6JRWK=
BHT-101 NVHWSVNbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXHJR|UxRTBwNkSyOlMh|ryP MWTTRW5ITVJ?
CGTH-W-1 Mn2wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{K5eGlEPTB;MD62OFg4KM7:TR?= MlnMV2FPT0WU
HMV-II NFfqfW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2LUR2lEPTB;MD63OFg4PCEQvF2= MWfTRW5ITVJ?
NKM-1 NUHWdZlGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWLJR|UxRTBwOUCxOUDPxE1? NGfnXnJUSU6JRWK=
LB2241-RCC MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYD4e45JUUN3ME2xMlAzOjJ6IN88US=> MnXrV2FPT0WU
NCI-H1703 NWTHR2xFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUPLbWxHUUN3ME2xMlE5QDdizszN MVvTRW5ITVJ?
BE-13 NW[1[lBXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEXofWlKSzVyPUGuNlc1OTZizszN NVnCUY5QW0GQR1XS
ACN MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mly0TWM2OD1zLkW1NFc4KM7:TR?= MX3TRW5ITVJ?
A204 NH3YS|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYrJR|UxRTFwNUeyNFUh|ryP MVvTRW5ITVJ?
HOP-62 MmXRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYfJR|UxRTFwOEKwO|ch|ryP MYDTRW5ITVJ?
H9 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1TibGlEPTB;Mj63N|c6OyEQvF2= MmHJV2FPT0WU
HCC1806 NYf5S2N3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEfLPWVKSzVyPUKuO|Q{OjdizszN M4fqcXNCVkeHUh?=
NOS-1 NHq2[llIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH73bVNKSzVyPUKuPFcyODJizszN NEW5VpFUSU6JRWK=
RS4-11 NHTCNY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{HIUWlEPTB;Mj65NFYzOyEQvF2= MlzWV2FPT0WU
JAR NV\WS29qT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH;XWHlKSzVyPUKuPVIxQDRizszN NEXYVZhUSU6JRWK=
T98G Mn;lS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MU\JR|UxRTNwMEGzNVMh|ryP NFXwSmdUSU6JRWK=
NCI-SNU-1 NXLuXXR{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXHJR|UxRTNwNECwPVIh|ryP M1jORnNCVkeHUh?=
SK-MEL-1 MmPJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYnJR|UxRTNwNEOwNlkh|ryP NXH2eYFGW0GQR1XS
L-363 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnzDTWM2OD1|Lk[xNVA4KM7:TR?= MoHSV2FPT0WU
SW982 M3rZW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVrJR|UxRTNwNkSxOlkh|ryP NYPXUmppW0GQR1XS
HT-1080 NYHvO2p2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFvKdWhKSzVyPUOuPVE4PzVizszN MUDTRW5ITVJ?
G-402 M2LPcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEjPNYlKSzVyPUSuN|EzODNizszN MUDTRW5ITVJ?
HOS M1rQdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3Xac2lEPTB;ND64NFI5OiEQvF2= M1PZV3NCVkeHUh?=
SK-NEP-1 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXTFc5ZPUUN3ME20Mlg{OTlzIN88US=> NHOzbVlUSU6JRWK=
HAL-01 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXrJR|UxRTRwOEiyOFIh|ryP NYPQeIl5W0GQR1XS
SBC-1 NGrRO4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUnkbnBYUUN3ME20MlkxQTB5IN88US=> M3TpPHNCVkeHUh?=
CTV-1 NYXUclMxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEm1dJpKSzVyPUWuOFg6OzhizszN NEnOSHZUSU6JRWK=
LCLC-103H NI\M[2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWm4fVZbUUN3ME21Mlc4PDdzIN88US=> NX\zWnhCW0GQR1XS
RVH-421 MmLYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mmi0TWM2OD13Lke3OVM3KM7:TR?= Mo\kV2FPT0WU
K-562 NVu3[ppWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYfVV3l5UUN3ME21MlkxOzZizszN MVrTRW5ITVJ?
CAL-33 M1j1NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4HNb2lEPTB;Nj6zNVM2QSEQvF2= NFrGVoFUSU6JRWK=
MDA-MB-361 M4LERmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn3tTWM2OD14LkOzOlk6KM7:TR?= NWDqN|hZW0GQR1XS
IGROV-1 M1\KcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEDOeHFKSzVyPU[uOFcyQTFizszN MX;TRW5ITVJ?
NY MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVjJR|UxRTZwNUO1PVkh|ryP Ml7TV2FPT0WU
Ramos-2G6-4C10 M2DxXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFe2W5ZKSzVyPU[uOlY6OzFizszN MWPTRW5ITVJ?
HuO9 NXHxco9{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXK3bnNLUUN3ME22Mlc{QTZ2IN88US=> MYHTRW5ITVJ?
MS-1 M3HKSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1vGNGlEPTB;Nz6xNVk2OyEQvF2= M1\DT3NCVkeHUh?=
RPMI-8226 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkHzTWM2OD15LkK4Nlg4KM7:TR?= Mlr2V2FPT0WU
HDLM-2 MkjhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoS1TWM2OD15LkSwNVQ6KM7:TR?= MXzTRW5ITVJ?
D-566MG MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXTLTY5zUUN3ME23MlQ4OTV3IN88US=> MYnTRW5ITVJ?
SK-MEL-24 M13JWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXjJR|UxRTdwNkOzPVIh|ryP NVjGXXR3W0GQR1XS
COLO-679 NV60e3o1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mmn4TWM2OD15Lkm4OlcyKM7:TR?= MkjZV2FPT0WU
EW-13 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEjHV|lKSzVyPUiuN|IxPTRizszN MmTIV2FPT0WU
A388 NH3yS4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXHsV5F{UUN3ME24MlM5PDhzIN88US=> MXHTRW5ITVJ?
UM-UC-3 Ml64S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXfJR|UxRThwNEO5OVYh|ryP MVzTRW5ITVJ?
NUGC-3 M4DFc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVnv[VJNUUN3ME24MlU{PTh{IN88US=> M4D0UXNCVkeHUh?=
COLO-668 NUX3emdXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mlj1TWM2OD16LkW5OFkyKM7:TR?= M2nsUXNCVkeHUh?=
MOLT-4 NUHZOJhTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3vDSmlEPTB;OD62NlM2OyEQvF2= NGHieI9USU6JRWK=
D-423MG M{\2Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVzJR|UxRThwOEO3OVYh|ryP M2LWOHNCVkeHUh?=
CTB-1 NWXFPYJmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1va[GlEPTB;OD64O|EzQCEQvF2= NF7T[HJUSU6JRWK=
BCPAP M1vFbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{fQWWlEPTB;OT6wNlU3OiEQvF2= NUHucIJrW0GQR1XS
GCT NHLHTlVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlTzTWM2OD17LkC5PFMyKM7:TR?= MmLZV2FPT0WU
ACHN MoTHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1fuZ2lEPTB;OT6yN|Y{OiEQvF2= NV\JUmpYW0GQR1XS
KYSE-520 MlXSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWi3fVBxUUN3ME25MlM{PDh{IN88US=> MkTzV2FPT0WU
LB771-HNC NFvwfmhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVPJR|UxRTlwN{[0PVch|ryP NEDhTGlUSU6JRWK=
MLMA NGe3O21Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV\JR|UxRTFyLkCxN|Ih|ryP MVjTRW5ITVJ?
HEC-1 NULrS|FRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWfvSo9zUUN3ME2xNE4zQDB2IN88US=> M{DHfXNCVkeHUh?=
HL-60 MknyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkLvTWM2OD1zMD62PFU{KM7:TR?= NUT4boFzW0GQR1XS
A101D MnX3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEe1cnVKSzVyPUGwMlg6OjNizszN MnPnV2FPT0WU
A2058 NVryN5Z2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVvJR|UxRTFyLkmyOFUh|ryP MUnTRW5ITVJ?
KARPAS-45 Mn3qS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFvQfW1KSzVyPUGxMlA3OzVizszN NX\QPFhKW0GQR1XS
697 NXL1[2dTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV;SXVlTUUN3ME2xNU4zOTBzIN88US=> NIjDNIdUSU6JRWK=
NCI-N87 MmDLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NECzUohKSzVyPUGxMlc4OzFizszN MlLOV2FPT0WU
DSH1 M1yzTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVOxfHBJUUN3ME2xNU44QTV|IN88US=> MUXTRW5ITVJ?
HLE Ml;lS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlXrTWM2OD1zMT64PFM6KM7:TR?= MXnTRW5ITVJ?
NCI-H720 NWiwVVZGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3XmemlEPTB;MUKuOlgxOSEQvF2= NEX0[ZFUSU6JRWK=
EW-3 M2HpXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHrafVBKSzVyPUGyMlk{ODdizszN NE\KR4hUSU6JRWK=
AGS MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGf6SnpKSzVyPUGzMlA{PTFizszN M1vq[nNCVkeHUh?=
ES5 Mlm0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{D5NWlEPTB;MUOuNFUyOiEQvF2= NIPubItUSU6JRWK=
DB MkX0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NU\oRZdSUUN3ME2xN{4{OjV4IN88US=> NVe5WJFCW0GQR1XS
A4-Fuk M4e5PGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4TEZ2lEPTB;MUOuOFExOiEQvF2= NIj1clRUSU6JRWK=
A427 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkH3TWM2OD1zMz60PVczKM7:TR?= NIK2boJUSU6JRWK=
MN-60 M{CyVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEXTR5BKSzVyPUGzMlU5PDNizszN NYC1XFhLW0GQR1XS
HCC2218 NWLtfoU3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUTJR|UxRTF|LkW4OVYh|ryP M4P4fnNCVkeHUh?=
MV-4-11 M2fUcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUXJR|UxRTF|LkixN|ch|ryP MWLTRW5ITVJ?
GI-1 NILXdoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4jiRmlEPTB;MUSuNVE5PCEQvF2= NWDkTGRwW0GQR1XS
JVM-3 MmfCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIC5OJZKSzVyPUG0MlI3PTZizszN NHzp[YRUSU6JRWK=
NCI-H2029 NVvmemZGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1O2NGlEPTB;MUSuNlczPyEQvF2= Mk\2V2FPT0WU
TE-12 MojGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmjZTWM2OD1zND62NFQ3KM7:TR?= NFHUWnNUSU6JRWK=
WM-115 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlvITWM2OD1zNT61Olg{KM7:TR?= MkfmV2FPT0WU
BB65-RCC NEPXUIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoX1TWM2OD1zNj6wNlQyKM7:TR?= M4O4W3NCVkeHUh?=
NCI-H1693 NWPJUlZtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MW\JR|UxRTF4LkO4NFIh|ryP MkLyV2FPT0WU
KARPAS-299 M1n6emdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn[1TWM2OD1zNj62NlA{KM7:TR?= MXTTRW5ITVJ?
UACC-257 MnS4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEGwcINKSzVyPUG3MlA2QDJizszN M3zFOHNCVkeHUh?=
RKO Mn3HS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{D3WmlEPTB;MUeuOlQ{OyEQvF2= Mm\hV2FPT0WU
HT-29 MmGzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1L2UmlEPTB;MUeuO|g5QSEQvF2= M3jodnNCVkeHUh?=
ES7 NVHqOlRyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2fGdmlEPTB;MUiuNVEzOiEQvF2= M4i3SHNCVkeHUh?=
DEL M2e1Rmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWXJR|UxRTF6LkOxO|Ih|ryP MYXTRW5ITVJ?
BT-549 NXG1cJBWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFnifVFKSzVyPUG4MlQxQTJizszN M2nZbHNCVkeHUh?=
NCI-H1755 NV30PI9YT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGL6T4lKSzVyPUG4MlU4OjNizszN M2C2XHNCVkeHUh?=
HCE-T M4fCWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2[3dWlEPTB;MUiuPFM1OSEQvF2= M1iwOXNCVkeHUh?=
LU-139 NWnqfoF{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXq0Vm1JUUN3ME2xPU4xPDV6IN88US=> MWTTRW5ITVJ?
ECC10 MmLqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWHSU3ZRUUN3ME2xPU4zPDd3IN88US=> MXPTRW5ITVJ?
769-P M3HaeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFr1blRKSzVyPUG5MlY{OzVizszN M4\aUHNCVkeHUh?=
BALL-1 M17se2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXvpeVVTUUN3ME2xPU43Pzd3IN88US=> NYjxNohTW0GQR1XS
LXF-289 NF;wT21Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MljUTWM2OD1zOT64PVc6KM7:TR?= NEXOS|NUSU6JRWK=
TYK-nu NGLLPWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYjJR|UxRTF7LkmzNVUh|ryP NV;rd5ZzW0GQR1XS
NCI-H630 M2ToVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mlj3TWM2OD1zOT65N|c5KM7:TR?= NFuwNY1USU6JRWK=
EW-18 NVTqfWdjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{jVZ2lEPTB;MkCuN|gxOiEQvF2= M3WybnNCVkeHUh?=
KYSE-150 MlL5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVfJR|UxRTJyLkewOFch|ryP MoCyV2FPT0WU
LOXIMVI MmDHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHvYb5lKSzVyPUKwMlc2QDZizszN NEjwOG5USU6JRWK=
HuP-T3 MoHHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnLkTWM2OD1{MT6wPFUzKM7:TR?= NYTEOFJtW0GQR1XS
MFE-280 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGjqeGJKSzVyPUKxMlU3PzlizszN MnzoV2FPT0WU
SK-OV-3 MnjVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHPMVnpKSzVyPUKxMlg1ODhizszN NFfiUFdUSU6JRWK=
QIMR-WIL MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{nxR2lEPTB;MkKuNFQ4QCEQvF2= NGXYenlUSU6JRWK=
NCI-H69 M1r4fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2n6fGlEPTB;MkKuOFI6QSEQvF2= M1XNS3NCVkeHUh?=
TE-5 MmXvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3nWemlEPTB;MkKuOFk3PSEQvF2= MmO4V2FPT0WU
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NCI-H2228 NH;OUYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M36yS2lEPTB;MkmuOFU5KM7:TR?= MYDTRW5ITVJ?
MHH-PREB-1 M1H6Zmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFe2NplKSzVyPUK5MlU2ODVizszN NF7xUplUSU6JRWK=
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NCI-H209 MnmwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUDJR|UxRTJ7LkizOlYh|ryP M{PGdHNCVkeHUh?=
NBsusSR NFe5Z45Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEmwNFVKSzVyPUK5Mlk6ODRizszN MX;TRW5ITVJ?
NCI-H1304 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVz5XGVkUUN3ME2zNE42PzF4IN88US=> MorGV2FPT0WU
NB14 NFnVTpBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXTJR|UxRTNzLkC0OFYh|ryP MmjwV2FPT0WU
HCC1419 NXzzd2NsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnHCTWM2OD1|MT6yOEDPxE1? MYLTRW5ITVJ?
KG-1 NIi4T|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF7IeGRKSzVyPUOxMlc1OjlizszN MVLTRW5ITVJ?
A2780 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFizSINKSzVyPUOxMlg{PThizszN NFvnfJRUSU6JRWK=
NCI-H28 Mkm3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEPUPWJKSzVyPUOxMlk5PjFizszN MkD4V2FPT0WU
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VA-ES-BJ NYHN[WpjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3rpXGlEPTB;M{KuN|Eh|ryP NUfrbJhyW0GQR1XS
SBC-5 M3zJcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWTJR|UxRTN{Lki1NVEh|ryP MoTuV2FPT0WU
OVCAR-4 NIHYWoVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV7L[HNJUUN3ME2zN{41QDR6IN88US=> Mk\5V2FPT0WU
COR-L88 NEizO4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml76TWM2OD1|ND6wO|QyKM7:TR?= MmDrV2FPT0WU
SW954 M4jkdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH3ZdJpKSzVyPUO0MlA4PTJizszN MoHOV2FPT0WU
COLO-684 NVnwPG5JT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{DZ[mlEPTB;M{SuN|QxPCEQvF2= NGSzTlBUSU6JRWK=
HCC70 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1HRS2lEPTB;M{SuPVUyPCEQvF2= MnHEV2FPT0WU
NCI-H1770 NVjpZoM3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NITIVHhKSzVyPUO0Mlk3OSEQvF2= NFjMZ4lUSU6JRWK=
NCI-H1666 M2rSNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Moj0TWM2OD1|NT64NlU{KM7:TR?= NXLqeo9wW0GQR1XS
YH-13 M1fISmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3X1fmlEPTB;M{WuPVIh|ryP MULTRW5ITVJ?
DJM-1 NILo[5pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkPVTWM2OD1|Nj64NFQ6KM7:TR?= MlPqV2FPT0WU
KNS-62 NELxO2lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2fLc2lEPTB;M{[uPVQ{QCEQvF2= NE\q[GVUSU6JRWK=
SK-MEL-30 NH7ZTXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVHFUZhOUUN3ME2zO{45PzN5IN88US=> Moq4V2FPT0WU
SJRH30 NWTNS|Q1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHj5O4tKSzVyPUO4Mlc{PDFizszN MVfTRW5ITVJ?
GP5d NED6eJRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHvuO3JKSzVyPUO4Mlg3PTNizszN NIfyNoJUSU6JRWK=
SW1116 NGP2WpJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHHqVHRKSzVyPUO5MlI5ODVizszN NXjROWhQW0GQR1XS
COLO-800 NEfXO5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFfpSJZKSzVyPUO5MlM3OzhizszN NIOyVIVUSU6JRWK=
RD NX:xblVuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWrJR|UxRTN7LkWyOVgh|ryP NIXIO4NUSU6JRWK=
NCI-SNU-5 M2XJSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVzJR|UxRTN7Lk[5NVYh|ryP MknYV2FPT0WU
HuO-3N1 M{jDVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlXMTWM2OD12MD6xNFgh|ryP M1\nSXNCVkeHUh?=
SK-UT-1 MkDzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVTJR|UxRTRyLkW2O|Qh|ryP MV7TRW5ITVJ?
SK-MEL-3 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn3nTWM2OD12MD61PVMzKM7:TR?= NHvFV2pUSU6JRWK=
SK-MEL-28 NEL2WIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVj6b5NbUUN3ME20NE43PDN3IN88US=> NH7pVoFUSU6JRWK=
SCC-4 NWD6SWpET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVHYcYJiUUN3ME20NU4zOTN5IN88US=> MoTQV2FPT0WU
no-11 NXOzWYdXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NICzOlZKSzVyPUSxMlc{PTRizszN M4q0SnNCVkeHUh?=
HT-144 MnmyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2GwRmlEPTB;NEKuNFU3PyEQvF2= MYDTRW5ITVJ?
MFM-223 NWnzfmNbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmDMTWM2OD12Mj60NFIh|ryP Ml3OV2FPT0WU
ONS-76 NHKyNoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEjJbFhKSzVyPUSyMlgxOThizszN MUDTRW5ITVJ?
ES8 NVH2d3NIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX[zRYZsUUN3ME20N{4{Pjl6IN88US=> NUiwb|NCW0GQR1XS
T-24 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3vNPGlEPTB;NEOuOFM3QSEQvF2= M3HOb3NCVkeHUh?=
GAMG NG\2SpJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX3JR|UxRTR|LkS1NVch|ryP NVXwfFBkW0GQR1XS
LU-135 NX35SIFZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml;nTWM2OD12ND6wPVI{KM7:TR?= NYjSdXRDW0GQR1XS
HCC1187 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkLFTWM2OD12ND64NlYzKM7:TR?= NHHqSYFUSU6JRWK=
TE-1 NHnFU4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoHpTWM2OD12NT6xOlU1KM7:TR?= MVjTRW5ITVJ?
J-RT3-T3-5 NVf1[mM3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MULJR|UxRTR3LkSzNVUh|ryP M{\1UHNCVkeHUh?=
GI-ME-N MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXnNWYpiUUN3ME20OU45QTV{IN88US=> M1rJbHNCVkeHUh?=
D-392MG MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1HNdmlEPTB;NEWuPVI2PiEQvF2= Mln2V2FPT0WU
KALS-1 NH\uU2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{L2c2lEPTB;NE[uO|I2PyEQvF2= NG[yTI1USU6JRWK=
MMAC-SF NHTINI1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2H2cmlEPTB;NE[uPVk2OiEQvF2= MoLFV2FPT0WU
HSC-3 M3jucmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUnJR|UxRTR5LkO2NFgh|ryP NF;Gd|RUSU6JRWK=
KM-H2 NWLZTodVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGC4NG9KSzVyPUS3MlYxODdizszN MknsV2FPT0WU
LoVo Mnz5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXTJR|UxRTR6LkGwNFIh|ryP NX\LWlNiW0GQR1XS
NCI-H510A NV36eokzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVLJR|UxRTR6LkG4O|Eh|ryP NIHOb3VUSU6JRWK=
EW-11 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWfJR|UxRTR6LkKzOFgh|ryP MXvTRW5ITVJ?
HCC2998 M33ROmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUDJR|UxRTR6Lk[yN|Yh|ryP NUfKdlJuW0GQR1XS
J82 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIXxXFBKSzVyPUS4MlczPDJizszN MorhV2FPT0WU
ML-2 NYXUbYFoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWLJR|UxRTR7LkS2NFUh|ryP NVfMe4E1W0GQR1XS
NCI-H2030 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoDLTWM2OD12OT63NVE4KM7:TR?= Mlq5V2FPT0WU
NCI-H1792 NV3keolLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml73TWM2OD12OT64OVE5KM7:TR?= M1zm[nNCVkeHUh?=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-AMPKα / AMPKα / p-AMPKβ1 / AMPKγ2 / p-LKB1 / LKB1 / CaMKIIβ ; 

PubMed: 23677989     


Dose-dependent analysis of AMPK-related molecules in HCC cells. Cells were exposed to nilotinib at the indicated concentrations for 24 h.

DNMT1 / DNMT3a / DNMT3b ; 

PubMed: 28720666     


Kasumi-1 or MV4-11 cells were treated for 24 h with the indicated doses of nilotinib and subjected western blot analysis to detect the expression levels of DNMT1, DNMT3a, DNMT3b.

pABL1 / p-NF-κB1 / NF-κB / STAT3 / p-STAT3 / IL-1β / IL-6 / COX2 ; 

PubMed: 31396300     


ABL1 regulated the inflammation signaling pathway. Blocking activities of ABL1 with Imatinib and Nilotinib inhibits the inflammatory signaling pathway including activities of NF-κB1, STAT3, IL-1β, IL-6, and COX2.

23677989 28720666 31396300
Growth inhibition assay
Cell viability; 

PubMed: 23677989     


Dose-dependent effects of nilotinib on cell viability. HCC cells were treated with nilotinib at the indicated concentrations for 72 h. Cell viability was measured by MTT assay. Points, mean; bars, S.D. (n = 8). 

23677989
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]
- Collapse
  • 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]
- Collapse
  • 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
  • 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
Smiles CC1=C(C=C(C=C1)C(=O)NC2=CC(=CC(=C2)C(F)(F)F)N3C=C(N=C3)C)NC4=NC=CC(=N4)C5=CN=CC=C5

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Step 2: Enter the in vivo formulation ()
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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 (mg) = Concentration (mM) × Volume (mL) × 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).

The Serial Dilution Calculator Equation

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  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
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Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04326933 Not yet recruiting Drug: Tyrosine kinase Inhibitors (Imatinib & Nilotinib) Patients Diagnosed as Chronic Meyloid Leukemia Assiut University October 20 2020 --
NCT03942094 Recruiting Drug: Nilotinib Chronic Myeloid Leukemia Chronic Phase|Nilotinib Shenzhen Second People''s Hospital June 1 2019 Phase 3
NCT03874858 Recruiting Drug: Nilotinib Chronic Myeloid Leukemia Novartis Pharmaceuticals|Novartis April 1 2019 Phase 2
NCT04002674 Recruiting Drug: Placebo oral capsule|Drug: Nilotinib Oral Capsule Dementia With Lewy Bodies Georgetown University|National Institutes of Health (NIH) January 14 2019 Phase 2
NCT02973711 Suspended Drug: Nilotinib|Drug: Ruxolitinib Leukemia Chronic Myeloid University of Michigan Rogel Cancer Center January 18 2018 Phase 1|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