Nilotinib (AMN-107)

For research use only.

Catalog No.S1033

82 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 82 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 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoK3TWM2OD1yLkCwNFE1PCEQvF2= MWTTRW5ITVJ?
KU812 NVfx[3JiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MknJTWM2OD1yLkCwNlQ5KM7:TR?= MVTTRW5ITVJ?
EM-2 MnW0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYjJR|UxRTBwMEC0NUDPxE1? NGHKXWNUSU6JRWK=
LAMA-84 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkHETWM2OD1yLkCwOFkh|ryP NYjF[Zc5W0GQR1XS
MEG-01 NIWxZodIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3LXS2lEPTB;MD6wNFgzQCEQvF2= NXnpXmE4W0GQR1XS
BV-173 NIPNb|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4DHS2lEPTB;MD6wNVA5QSEQvF2= NWDEfHU5W0GQR1XS
KASUMI-1 Mm\kS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2\Je2lEPTB;MD6wNlQyOyEQvF2= NFHz[GpUSU6JRWK=
NB7 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3nNcmlEPTB;MD6xN|Q{QSEQvF2= Mk\GV2FPT0WU
BHT-101 MlzLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoHVTWM2OD1yLk[0NlY{KM7:TR?= M1vpVHNCVkeHUh?=
CGTH-W-1 NG\F[4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NU\NU3FbUUN3ME2wMlY1QDdizszN Mn;VV2FPT0WU
HMV-II Mmq0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH;vbFVKSzVyPUCuO|Q5PzRizszN MV3TRW5ITVJ?
NKM-1 Mor4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4nRXWlEPTB;MD65NFE2KM7:TR?= NV\idZhKW0GQR1XS
LB2241-RCC Mn\zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH3ZR2VKSzVyPUGuNFIzOjhizszN NH:1OFZUSU6JRWK=
NCI-H1703 MnfnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV3YN45HUUN3ME2xMlE5QDdizszN NGS0OZBUSU6JRWK=
BE-13 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWjjZXNWUUN3ME2xMlI4PDF4IN88US=> NULYPWZ{W0GQR1XS
ACN M{f0U2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3G3e2lEPTB;MT61OVA4PyEQvF2= M2PncXNCVkeHUh?=
A204 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGfPbpVKSzVyPUGuOVczODVizszN MlPxV2FPT0WU
HOP-62 NFG0d3ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHLRU3BKSzVyPUGuPFIxPzdizszN Mm\mV2FPT0WU
H9 NF3RbpBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{O4NWlEPTB;Mj63N|c6OyEQvF2= NWPWelBKW0GQR1XS
HCC1806 M3zqW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4T0ZWlEPTB;Mj63OFMzPyEQvF2= MXPTRW5ITVJ?
NOS-1 NIL0RVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFPPUXpKSzVyPUKuPFcyODJizszN NVzBWYtGW0GQR1XS
RS4-11 M33OeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXHJR|UxRTJwOUC2NlMh|ryP M2myT3NCVkeHUh?=
JAR MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYjJR|UxRTJwOUKwPFQh|ryP MnHPV2FPT0WU
T98G MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXfPPGx7UUN3ME2zMlAyOzF|IN88US=> M4fCeHNCVkeHUh?=
NCI-SNU-1 M13ZR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWLFbJpNUUN3ME2zMlQxODl{IN88US=> NV[0[2JmW0GQR1XS
SK-MEL-1 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEjpWmlKSzVyPUOuOFMxOjlizszN NUS5cJhEW0GQR1XS
L-363 NHzlcWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2naWWlEPTB;Mz62NVExPyEQvF2= MVjTRW5ITVJ?
SW982 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF;EfpVKSzVyPUOuOlQyPjlizszN NIXWd4tUSU6JRWK=
HT-1080 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXrwWJZ7UUN3ME2zMlkyPzd3IN88US=> NF3ze|NUSU6JRWK=
G-402 NWXDe5A1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWXJR|UxRTRwM{GyNFMh|ryP NVrvd2I5W0GQR1XS
HOS NHjzWHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH;jN2xKSzVyPUSuPFAzQDJizszN NF3TcGhUSU6JRWK=
SK-NEP-1 M3;zbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEnVeItKSzVyPUSuPFMyQTFizszN NYjofnZjW0GQR1XS
HAL-01 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2fodmlEPTB;ND64PFI1OiEQvF2= M2r2[nNCVkeHUh?=
SBC-1 NEHWeWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{HodWlEPTB;ND65NFkxPyEQvF2= MWfTRW5ITVJ?
CTV-1 NEDXSGdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV\4No9[UUN3ME21MlQ5QTN6IN88US=> MlLUV2FPT0WU
LCLC-103H M2rITmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmPJTWM2OD13Lke3OFcyKM7:TR?= NHfGVIlUSU6JRWK=
RVH-421 M3fpRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnLzTWM2OD13Lke3OVM3KM7:TR?= MVXTRW5ITVJ?
K-562 NIX0O3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX3JR|UxRTVwOUCzOkDPxE1? NWLMfXJzW0GQR1XS
CAL-33 M{TGTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWTJR|UxRTZwM{GzOVkh|ryP M{PRcnNCVkeHUh?=
MDA-MB-361 Mli2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{P3XmlEPTB;Nj6zN|Y6QSEQvF2= NUSySokxW0GQR1XS
IGROV-1 NGTJZWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mk\ZTWM2OD14LkS3NVkyKM7:TR?= MmCyV2FPT0WU
NY M{\hb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEXFVYFKSzVyPU[uOVM2QTlizszN MWHTRW5ITVJ?
Ramos-2G6-4C10 NWGw[oZCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2HaZmlEPTB;Nj62Olk{OSEQvF2= M3\nfXNCVkeHUh?=
HuO9 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXvYXlJVUUN3ME22Mlc{QTZ2IN88US=> M4PORnNCVkeHUh?=
MS-1 NV[5Om02T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGLWTmJKSzVyPUeuNVE6PTNizszN MUfTRW5ITVJ?
RPMI-8226 M{TqR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYrJR|UxRTdwMkiyPFch|ryP NHvyfXBUSU6JRWK=
HDLM-2 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYez[|I5UUN3ME23MlQxOTR7IN88US=> MXnTRW5ITVJ?
D-566MG MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXXEOo4zUUN3ME23MlQ4OTV3IN88US=> Mmf5V2FPT0WU
SK-MEL-24 MnrMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M17UR2lEPTB;Nz62N|M6OiEQvF2= Mn;kV2FPT0WU
COLO-679 MmPXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXjJR|UxRTdwOUi2O|Eh|ryP NGewXGdUSU6JRWK=
EW-13 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHHnco1KSzVyPUiuN|IxPTRizszN MlezV2FPT0WU
A388 NE\BXZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHzCN4JKSzVyPUiuN|g1QDFizszN M4rROXNCVkeHUh?=
UM-UC-3 M1LFdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MojRTWM2OD16LkSzPVU3KM7:TR?= NHS2PW1USU6JRWK=
NUGC-3 MnftS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWLmenRVUUN3ME24MlU{PTh{IN88US=> MULTRW5ITVJ?
COLO-668 MkPlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXX2WIJQUUN3ME24MlU6PDlzIN88US=> M3;5cnNCVkeHUh?=
MOLT-4 M1jN[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmjoTWM2OD16Lk[yN|U{KM7:TR?= NUCyZmFVW0GQR1XS
D-423MG M3;oO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFvVepZKSzVyPUiuPFM4PTZizszN MmrxV2FPT0WU
CTB-1 NYrVbpBFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXPWbWNjUUN3ME24Mlg4OTJ6IN88US=> MmnVV2FPT0WU
BCPAP MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3;IfGlEPTB;OT6wNlU3OiEQvF2= MlfhV2FPT0WU
GCT M3HOd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVewd4tpUUN3ME25MlA6QDNzIN88US=> MkXLV2FPT0WU
ACHN NIPlTppIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGntR3BKSzVyPUmuNlM3OzJizszN MkDyV2FPT0WU
KYSE-520 MlSyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFTJVppKSzVyPUmuN|M1QDJizszN MUPTRW5ITVJ?
LB771-HNC NWnkXoQ4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFfwb2xKSzVyPUmuO|Y1QTdizszN NEXRUFlUSU6JRWK=
MLMA MmPES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV\6S|lLUUN3ME2xNE4xOTN{IN88US=> Mnn5V2FPT0WU
HEC-1 Mom2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFn0PG9KSzVyPUGwMlI5ODRizszN MXTTRW5ITVJ?
HL-60 NHewbZZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MULJR|UxRTFyLk[4OVMh|ryP MUDTRW5ITVJ?
A101D M3L0Wmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4LSfWlEPTB;MUCuPFkzOyEQvF2= NGLN[YhUSU6JRWK=
A2058 M4facGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2\USGlEPTB;MUCuPVI1PSEQvF2= NICyW3hUSU6JRWK=
KARPAS-45 MoTtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWfJR|UxRTFzLkC2N|Uh|ryP MYDTRW5ITVJ?
697 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3rROmlEPTB;MUGuNlExOSEQvF2= NGO0NHVUSU6JRWK=
NCI-N87 Mn\HS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlSzTWM2OD1zMT63O|MyKM7:TR?= NVrSfoVvW0GQR1XS
DSH1 Mn2wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXLJR|UxRTFzLke5OVMh|ryP MV;TRW5ITVJ?
HLE NI\sWHhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXXJR|UxRTFzLki4N|kh|ryP NE\6O4dUSU6JRWK=
NCI-H720 MoHKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1TOeGlEPTB;MUKuOlgxOSEQvF2= M4\BfnNCVkeHUh?=
EW-3 NYPLUWtVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVfJR|UxRTF{LkmzNFch|ryP NHfiN2RUSU6JRWK=
AGS NFexTWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFjp[XpKSzVyPUGzMlA{PTFizszN NUT0OIZYW0GQR1XS
ES5 NIfBT|JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NULQOZFsUUN3ME2xN{4xPTF{IN88US=> NWDB[4lIW0GQR1XS
DB NFPlelBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVXJR|UxRTF|LkOyOVYh|ryP M3XNZnNCVkeHUh?=
A4-Fuk NEDrU5VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4X1S2lEPTB;MUOuOFExOiEQvF2= NXnXcGl2W0GQR1XS
A427 MoLSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVjOOXNCUUN3ME2xN{41QTd{IN88US=> M3mzc3NCVkeHUh?=
MN-60 M4DjPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1LY[GlEPTB;MUOuOVg1OyEQvF2= MUjTRW5ITVJ?
HCC2218 MmLiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYLtZ4t6UUN3ME2xN{42QDV4IN88US=> M3fJWHNCVkeHUh?=
MV-4-11 MnjwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlHNTWM2OD1zMz64NVM4KM7:TR?= NE\wcJpUSU6JRWK=
GI-1 Mn71S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF\w[2dKSzVyPUG0MlEyQDRizszN NW\wUJg4W0GQR1XS
JVM-3 NV3nfm5HT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIXTNHJKSzVyPUG0MlI3PTZizszN NFLUXFBUSU6JRWK=
NCI-H2029 NEmwOpVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXvQcpNVUUN3ME2xOE4zPzJ5IN88US=> MWrTRW5ITVJ?
TE-12 NYe5WWZLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoryTWM2OD1zND62NFQ3KM7:TR?= MYXTRW5ITVJ?
WM-115 MlnNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEeyUGNKSzVyPUG1MlU3QDNizszN M3ftTXNCVkeHUh?=
BB65-RCC MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3[1S2lEPTB;MU[uNFI1OSEQvF2= NHfaPFhUSU6JRWK=
NCI-H1693 M2j2eGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYDJR|UxRTF4LkO4NFIh|ryP M4rJdXNCVkeHUh?=
KARPAS-299 NVLQWmNpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MULJR|UxRTF4Lk[yNFMh|ryP NF3VUIJUSU6JRWK=
UACC-257 NUjNb2MxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYHJR|UxRTF5LkC1PFIh|ryP MoXFV2FPT0WU
RKO MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH7kTW1KSzVyPUG3MlY1OzNizszN MX7TRW5ITVJ?
HT-29 M{TKRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M334fWlEPTB;MUeuO|g5QSEQvF2= M3vsenNCVkeHUh?=
ES7 M2PH[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmOwTWM2OD1zOD6xNVIzKM7:TR?= NITYNGFUSU6JRWK=
DEL MljOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmjxTWM2OD1zOD6zNVczKM7:TR?= Mo\NV2FPT0WU
BT-549 NWS3TW9oT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUDjS5FKUUN3ME2xPE41ODl{IN88US=> NUXRTJBDW0GQR1XS
NCI-H1755 NHvNeW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NULDWpQ3UUN3ME2xPE42PzJ|IN88US=> NHHNRYZUSU6JRWK=
HCE-T MkLjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1vRVGlEPTB;MUiuPFM1OSEQvF2= MlHMV2FPT0WU
LU-139 NUnvSIY2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX3JR|UxRTF7LkC0OVgh|ryP Mk\1V2FPT0WU
ECC10 NYrWSlJ2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHvQdnBKSzVyPUG5MlI1PzVizszN MXnTRW5ITVJ?
769-P NXv3WG5MT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MULJR|UxRTF7Lk[zN|Uh|ryP MoPGV2FPT0WU
BALL-1 NYjFOo9FT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmjjTWM2OD1zOT62O|c2KM7:TR?= NWjreppSW0GQR1XS
LXF-289 MkDaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVfJR|UxRTF7Lki5O|kh|ryP Mn2wV2FPT0WU
TYK-nu NVXReZRoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3PUOGlEPTB;MUmuPVMyPSEQvF2= M33qNHNCVkeHUh?=
NCI-H630 M3rIPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MojyTWM2OD1zOT65N|c5KM7:TR?= MnzmV2FPT0WU
EW-18 NH25T4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4jsbmlEPTB;MkCuN|gxOiEQvF2= NX3vN4Y4W0GQR1XS
KYSE-150 NVPsTJhtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYfJR|UxRTJyLkewOFch|ryP M1TlVXNCVkeHUh?=
LOXIMVI MojUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF63SWVKSzVyPUKwMlc2QDZizszN M{PFOnNCVkeHUh?=
HuP-T3 M2TzWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnvKTWM2OD1{MT6wPFUzKM7:TR?= NX\XeHJNW0GQR1XS
MFE-280 M2W0dGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2PzbGlEPTB;MkGuOVY4QSEQvF2= NGntO2RUSU6JRWK=
SK-OV-3 MnW0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUnJR|UxRTJzLki0NFgh|ryP NH\aemtUSU6JRWK=
QIMR-WIL M{fkcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYHJR|UxRTJ{LkC0O|gh|ryP MVnTRW5ITVJ?
NCI-H69 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX7iXIxlUUN3ME2yNk41Ojl7IN88US=> M3rrWnNCVkeHUh?=
TE-5 NYH2TY9bT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX7MZ3lZUUN3ME2yNk41QTZ3IN88US=> MXvTRW5ITVJ?
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ES8 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYDJR|UxRTR|LkO2PVgh|ryP MY\TRW5ITVJ?
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GAMG M4Xw[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV\JR|UxRTR|LkS1NVch|ryP MWjTRW5ITVJ?
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GI-ME-N NHP6PHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX;JR|UxRTR3Lki5OVIh|ryP MXnTRW5ITVJ?
D-392MG M3\wVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXXJR|UxRTR3LkmyOVYh|ryP NYH1PVhOW0GQR1XS
KALS-1 NFfibXBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEOwc3VKSzVyPUS2MlczPTdizszN NX;HXoF5W0GQR1XS
MMAC-SF NX7H[3NqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn3QTWM2OD12Nj65PVUzKM7:TR?= MXfTRW5ITVJ?
HSC-3 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEDyd3dKSzVyPUS3MlM3ODhizszN M2DmN3NCVkeHUh?=
KM-H2 NH7HWlRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn;lTWM2OD12Nz62NFA4KM7:TR?= NHuxbGlUSU6JRWK=
LoVo M1\kcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXLrbFBOUUN3ME20PE4yODB{IN88US=> M1n6cHNCVkeHUh?=
NCI-H510A NWWxfHJzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnfkTWM2OD12OD6xPFcyKM7:TR?= M4\XXXNCVkeHUh?=
EW-11 M4O5c2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MojLTWM2OD12OD6yN|Q5KM7:TR?= M{XSUHNCVkeHUh?=
HCC2998 M{ftdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mmi4TWM2OD12OD62NlM3KM7:TR?= MUjTRW5ITVJ?
J82 NGHBRndIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH\KfnZKSzVyPUS4MlczPDJizszN NGrhTXFUSU6JRWK=
ML-2 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{G3dWlEPTB;NEmuOFYxPSEQvF2= NEOzeo1USU6JRWK=
NCI-H2030 MlniS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NU\Nd5I5UUN3ME20PU44OTF5IN88US=> NH:0TmlUSU6JRWK=
NCI-H1792 NEHSRZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFHoSWVKSzVyPUS5Mlg2OThizszN MlfMV2FPT0WU

... 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

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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

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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

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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