Nilotinib (AMN-107)

For research use only.

Catalog No.S1033

78 publications

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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Selleck's Nilotinib (AMN-107) has been cited by 78 publications

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 MkDLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVjieVFsUUN3ME2wMlAxODF2NDFOwG0> MVHTRW5ITVJ?
KU812 M3yzPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH7vUJpKSzVyPUCuNFAzPDhizszN MWnTRW5ITVJ?
EM-2 NWDN[pBwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXfJR|UxRTBwMEC0NUDPxE1? NHjEOXlUSU6JRWK=
LAMA-84 NFzVXFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFjFTIhKSzVyPUCuNFA1QSEQvF2= NXrNSoQ3W0GQR1XS
MEG-01 NFvGXHhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3nXTmlEPTB;MD6wNFgzQCEQvF2= MkmzV2FPT0WU
BV-173 NUXSTnlwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWn5cpNmUUN3ME2wMlAyODh7IN88US=> M3fyenNCVkeHUh?=
KASUMI-1 MoLCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnGzTWM2OD1yLkCyOFE{KM7:TR?= MUTTRW5ITVJ?
NB7 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkTzTWM2OD1yLkGzOFM6KM7:TR?= MYPTRW5ITVJ?
BHT-101 NFzXcnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV3JR|UxRTBwNkSyOlMh|ryP MXjTRW5ITVJ?
CGTH-W-1 MmLTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn[yTWM2OD1yLk[0PFch|ryP Ml7jV2FPT0WU
HMV-II MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{exVmlEPTB;MD63OFg4PCEQvF2= MoDEV2FPT0WU
NKM-1 M4W1WWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUDYdZIzUUN3ME2wMlkxOTVizszN NYnXSmtuW0GQR1XS
LB2241-RCC NGfxVG1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MorKTWM2OD1zLkCyNlI5KM7:TR?= M1f0RXNCVkeHUh?=
NCI-H1703 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnuyTWM2OD1zLkG4PFch|ryP M1;iOnNCVkeHUh?=
BE-13 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYjsflZmUUN3ME2xMlI4PDF4IN88US=> MWrTRW5ITVJ?
ACN NIDIc5VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlGzTWM2OD1zLkW1NFc4KM7:TR?= NUjRO3dCW0GQR1XS
A204 MlLWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2HzXmlEPTB;MT61O|IxPSEQvF2= MlHxV2FPT0WU
HOP-62 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHnHSYRKSzVyPUGuPFIxPzdizszN NFnjU3FUSU6JRWK=
H9 NVW0d3N7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXvRV3d[UUN3ME2yMlc{Pzl|IN88US=> NGrNe2hUSU6JRWK=
HCC1806 NFe5SHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2nqTmlEPTB;Mj63OFMzPyEQvF2= M2rZd3NCVkeHUh?=
NOS-1 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWTMdZVGUUN3ME2yMlg4OTB{IN88US=> MlnOV2FPT0WU
RS4-11 NVzIcpcxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYXRN4l6UUN3ME2yMlkxPjJ|IN88US=> M1vBZXNCVkeHUh?=
JAR MoTFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1HTRmlEPTB;Mj65NlA5PCEQvF2= NYnIWJhQW0GQR1XS
T98G Mln1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnnwTWM2OD1|LkCxN|E{KM7:TR?= MmDPV2FPT0WU
NCI-SNU-1 Mme1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnvFTWM2OD1|LkSwNFkzKM7:TR?= M3PNPXNCVkeHUh?=
SK-MEL-1 MmK2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoTzTWM2OD1|LkSzNFI6KM7:TR?= MVPTRW5ITVJ?
L-363 NGCxb3JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIXHbGpKSzVyPUOuOlEyODdizszN NXvORWdtW0GQR1XS
SW982 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGHCOYxKSzVyPUOuOlQyPjlizszN M{nqXHNCVkeHUh?=
HT-1080 MlK4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGXCelNKSzVyPUOuPVE4PzVizszN NF;pVo5USU6JRWK=
G-402 M1iwT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX;JR|UxRTRwM{GyNFMh|ryP MVvTRW5ITVJ?
HOS M{XVR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIPNOlJKSzVyPUSuPFAzQDJizszN NGO2U|hUSU6JRWK=
SK-NEP-1 Mn\HS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVzJR|UxRTRwOEOxPVEh|ryP NXnEUFhEW0GQR1XS
HAL-01 NFf3cZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn\qTWM2OD12Lki4NlQzKM7:TR?= NV7QZpRUW0GQR1XS
SBC-1 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIrmbnZKSzVyPUSuPVA6ODdizszN NGLVfHdUSU6JRWK=
CTV-1 MmXZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUHJR|UxRTVwNEi5N|gh|ryP MX3TRW5ITVJ?
LCLC-103H MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoXlTWM2OD13Lke3OFcyKM7:TR?= MWXTRW5ITVJ?
RVH-421 MmPES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3;rPWlEPTB;NT63O|U{PiEQvF2= MVPTRW5ITVJ?
K-562 M4nVbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV7FVWNEUUN3ME21MlkxOzZizszN M{iwUnNCVkeHUh?=
CAL-33 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEjyZYhKSzVyPU[uN|E{PTlizszN MnO1V2FPT0WU
MDA-MB-361 Ml7ES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYiwTG5ZUUN3ME22MlM{Pjl7IN88US=> MVXTRW5ITVJ?
IGROV-1 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWXETFNSUUN3ME22MlQ4OTlzIN88US=> MYnTRW5ITVJ?
NY NXHqUYpKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXPJR|UxRTZwNUO1PVkh|ryP MVvTRW5ITVJ?
Ramos-2G6-4C10 M1XV[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NELFZWhKSzVyPU[uOlY6OzFizszN MYDTRW5ITVJ?
HuO9 NVrVPIRsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHPOclRKSzVyPU[uO|M6PjRizszN M1nmbXNCVkeHUh?=
MS-1 NIHZSVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mo\mTWM2OD15LkGxPVU{KM7:TR?= NXezNHZ3W0GQR1XS
RPMI-8226 M37iS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVvJR|UxRTdwMkiyPFch|ryP M{XqTHNCVkeHUh?=
HDLM-2 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1Xvc2lEPTB;Nz60NFE1QSEQvF2= NYTNdmYxW0GQR1XS
D-566MG NEHLbG1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHrwV4RKSzVyPUeuOFcyPTVizszN MVvTRW5ITVJ?
SK-MEL-24 MmHTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV3JR|UxRTdwNkOzPVIh|ryP MX;TRW5ITVJ?
COLO-679 Ml65S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1fzW2lEPTB;Nz65PFY4OSEQvF2= MnXLV2FPT0WU
EW-13 NWL2ZYJGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV;JR|UxRThwM{KwOVQh|ryP NFnRc3lUSU6JRWK=
A388 NFnufoJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NITIN5NKSzVyPUiuN|g1QDFizszN MX3TRW5ITVJ?
UM-UC-3 NIfVSHFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVPJR|UxRThwNEO5OVYh|ryP Ml;SV2FPT0WU
NUGC-3 MlHyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoTVTWM2OD16LkWzOVgzKM7:TR?= Mn71V2FPT0WU
COLO-668 M4X4UWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYTJR|UxRThwNUm0PVEh|ryP MnrmV2FPT0WU
MOLT-4 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml60TWM2OD16Lk[yN|U{KM7:TR?= MkDGV2FPT0WU
D-423MG M1Xqfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVXSTmZ1UUN3ME24Mlg{PzV4IN88US=> M3rpNHNCVkeHUh?=
CTB-1 NXTVPJpXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHu0OnFKSzVyPUiuPFcyOjhizszN MofhV2FPT0WU
BCPAP Mk\lS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVzJR|UxRTlwMEK1OlIh|ryP NUH2cWVsW0GQR1XS
GCT MkTqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXXVVppmUUN3ME25MlA6QDNzIN88US=> NUXHPJV2W0GQR1XS
ACHN MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4XofmlEPTB;OT6yN|Y{OiEQvF2= MVzTRW5ITVJ?
KYSE-520 MkXFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{nkUWlEPTB;OT6zN|Q5OiEQvF2= MX3TRW5ITVJ?
LB771-HNC NV35WIo5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3;uZWlEPTB;OT63OlQ6PyEQvF2= MV;TRW5ITVJ?
MLMA Ml\NS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlfyTWM2OD1zMD6wNVMzKM7:TR?= MV3TRW5ITVJ?
HEC-1 NXTTcIZNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MojYTWM2OD1zMD6yPFA1KM7:TR?= NGnQTGJUSU6JRWK=
HL-60 NIDBNYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGTaZYlKSzVyPUGwMlY5PTNizszN NIfwXIFUSU6JRWK=
A101D NGTnSWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{i1eWlEPTB;MUCuPFkzOyEQvF2= NXf2R2hWW0GQR1XS
A2058 M2\Q[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGTZbG5KSzVyPUGwMlkzPDVizszN M33IdnNCVkeHUh?=
KARPAS-45 NYj6cZhET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV3IbW1UUUN3ME2xNU4xPjN3IN88US=> M3XaZnNCVkeHUh?=
697 NEPXUmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV7JR|UxRTFzLkKxNFEh|ryP MVPTRW5ITVJ?
NCI-N87 M{TteGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmLzTWM2OD1zMT63O|MyKM7:TR?= NVOwPVlIW0GQR1XS
DSH1 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEK5b2ZKSzVyPUGxMlc6PTNizszN MVjTRW5ITVJ?
HLE MmiwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1zlOGlEPTB;MUGuPFg{QSEQvF2= MnuxV2FPT0WU
NCI-H720 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmqxTWM2OD1zMj62PFAyKM7:TR?= NHTuZotUSU6JRWK=
EW-3 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGjvTFdKSzVyPUGyMlk{ODdizszN NYDFS3BwW0GQR1XS
AGS NEDlU5VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3TDOGlEPTB;MUOuNFM2OSEQvF2= MkTiV2FPT0WU
ES5 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHnEWVdKSzVyPUGzMlA2OTJizszN MX7TRW5ITVJ?
DB NWG5OFNJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV;JR|UxRTF|LkOyOVYh|ryP NEOyZ|JUSU6JRWK=
A4-Fuk NXnuNm9FT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkjTTWM2OD1zMz60NVAzKM7:TR?= MmLVV2FPT0WU
A427 NWr4dWlwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYHSUoZsUUN3ME2xN{41QTd{IN88US=> MUjTRW5ITVJ?
MN-60 NInReFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVnJR|UxRTF|LkW4OFMh|ryP MUPTRW5ITVJ?
HCC2218 M2TPVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIHPOoRKSzVyPUGzMlU5PTZizszN NYTo[FdSW0GQR1XS
MV-4-11 NGLXR4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFy5WplKSzVyPUGzMlgyOzdizszN NF;ZOVdUSU6JRWK=
GI-1 MmTiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEDMTlVKSzVyPUG0MlEyQDRizszN NG\WWXFUSU6JRWK=
JVM-3 NWP5XHczT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{nGRmlEPTB;MUSuNlY2PiEQvF2= NXq1UGtyW0GQR1XS
NCI-H2029 NIHBeIdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3e4S2lEPTB;MUSuNlczPyEQvF2= NI\0UGpUSU6JRWK=
TE-12 M{DHR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYrJR|UxRTF2Lk[wOFYh|ryP NVXIO|V1W0GQR1XS
WM-115 NGPQZYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mo\FTWM2OD1zNT61Olg{KM7:TR?= MXXTRW5ITVJ?
BB65-RCC MlHyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXTJR|UxRTF4LkCyOFEh|ryP NULZVIpXW0GQR1XS
NCI-H1693 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX7JR|UxRTF4LkO4NFIh|ryP NH[0U5NUSU6JRWK=
KARPAS-299 M3fJfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGjscnJKSzVyPUG2MlYzODNizszN NGnyOFJUSU6JRWK=
UACC-257 MljWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUHJR|UxRTF5LkC1PFIh|ryP NVvtZ4JuW0GQR1XS
RKO M2\TVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlvOTWM2OD1zNz62OFM{KM7:TR?= NHHCeVRUSU6JRWK=
HT-29 NHfscHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWPJR|UxRTF5Lke4PFkh|ryP MUnTRW5ITVJ?
ES7 NIHFeZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml\MTWM2OD1zOD6xNVIzKM7:TR?= MVjTRW5ITVJ?
DEL M4jlWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHm5bZlKSzVyPUG4MlMyPzJizszN MkHpV2FPT0WU
BT-549 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXvJR|UxRTF6LkSwPVIh|ryP MYfTRW5ITVJ?
NCI-H1755 NX7RR4dtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoPNTWM2OD1zOD61O|I{KM7:TR?= M2C5VHNCVkeHUh?=
HCE-T MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2D0fGlEPTB;MUiuPFM1OSEQvF2= NHP4fndUSU6JRWK=
LU-139 NXrIZmhiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{juSWlEPTB;MUmuNFQ2QCEQvF2= NVH6UJJ1W0GQR1XS
ECC10 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlTOTWM2OD1zOT6yOFc2KM7:TR?= NEjpd|ZUSU6JRWK=
769-P MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHLaW2xKSzVyPUG5MlY{OzVizszN NVLV[|VkW0GQR1XS
BALL-1 NHiwTXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXfJR|UxRTF7Lk[3O|Uh|ryP NFXYZWpUSU6JRWK=
LXF-289 NUPWd5ZyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{L4cWlEPTB;MUmuPFk4QSEQvF2= MlK5V2FPT0WU
TYK-nu M3LPOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIi5VGhKSzVyPUG5Mlk{OTVizszN M1vCfHNCVkeHUh?=
NCI-H630 M2LVSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIKxTGtKSzVyPUG5Mlk{PzhizszN MV3TRW5ITVJ?
EW-18 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2DjNWlEPTB;MkCuN|gxOiEQvF2= NWDSWnB4W0GQR1XS
KYSE-150 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1PlcGlEPTB;MkCuO|A1PyEQvF2= NGT1UpFUSU6JRWK=
LOXIMVI Mn7QS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3L5fmlEPTB;MkCuO|U5PiEQvF2= MljQV2FPT0WU
HuP-T3 M{i4eGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmDTTWM2OD1{MT6wPFUzKM7:TR?= NU\sNXhRW0GQR1XS
MFE-280 NX\pdpN1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUfvVHJ[UUN3ME2yNU42Pjd7IN88US=> MYXTRW5ITVJ?
SK-OV-3 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYXJR|UxRTJzLki0NFgh|ryP M1S2c3NCVkeHUh?=
QIMR-WIL Mn;wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4DrbmlEPTB;MkKuNFQ4QCEQvF2= Mm\RV2FPT0WU
NCI-H69 M4fPbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVXHcINGUUN3ME2yNk41Ojl7IN88US=> NIDCcWJUSU6JRWK=
TE-5 MkXIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmjkTWM2OD1{Mj60PVY2KM7:TR?= NUXpVFFwW0GQR1XS
NCI-H1993 NVvzdnlqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{joT2lEPTB;MkKuOFk4OSEQvF2= NITMeoxUSU6JRWK=
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NBsusSR NVPkdmFFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUXsTnlrUUN3ME2yPU46QTB2IN88US=> MV7TRW5ITVJ?
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KG-1 M1nx[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV\JR|UxRTNzLke0Nlkh|ryP M3fVUXNCVkeHUh?=
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OVCAR-4 Moj1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmTBTWM2OD1|Mz60PFQ5KM7:TR?= MXXTRW5ITVJ?
COR-L88 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmXNTWM2OD1|ND6wO|QyKM7:TR?= NEjuN2FUSU6JRWK=
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COLO-684 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3HueWlEPTB;M{SuN|QxPCEQvF2= M2Dk[XNCVkeHUh?=
HCC70 M1jYfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1fpbWlEPTB;M{SuPVUyPCEQvF2= M1HQSHNCVkeHUh?=
NCI-H1770 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{\jXGlEPTB;M{SuPVYyKM7:TR?= NETld2lUSU6JRWK=
NCI-H1666 MnmzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXz5PZF1UUN3ME2zOU45OjV|IN88US=> MW\TRW5ITVJ?
YH-13 NXHn[XNQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MY\JR|UxRTN3LkmyJO69VQ>? NYDIVlhMW0GQR1XS
DJM-1 NWXhXGFGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3HZbmlEPTB;M{[uPFA1QSEQvF2= NUDNTXZGW0GQR1XS
KNS-62 NVjuZppvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVfJR|UxRTN4Lkm0N|gh|ryP NH:xNY9USU6JRWK=
SK-MEL-30 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXzIRVBnUUN3ME2zO{45PzN5IN88US=> NYPxXopWW0GQR1XS
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GP5d Mmq1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUfEdXBiUUN3ME2zPE45PjV|IN88US=> MUXTRW5ITVJ?
SW1116 NYH3O4VoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUjJR|UxRTN7LkK4NFUh|ryP M2rROXNCVkeHUh?=
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RD MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVrJR|UxRTN7LkWyOVgh|ryP NH7PRlZUSU6JRWK=
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SK-MEL-3 NWrOS|d1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVLmPFdYUUN3ME20NE42QTN{IN88US=> MYnTRW5ITVJ?
SK-MEL-28 MkHqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkDlTWM2OD12MD62OFM2KM7:TR?= M3vzZnNCVkeHUh?=
SCC-4 M3fi[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFjqfFZKSzVyPUSxMlIyOzdizszN M3v0UHNCVkeHUh?=
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MFM-223 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2TrO2lEPTB;NEKuOFAzKM7:TR?= NWfhbYtEW0GQR1XS
ONS-76 NX7rS4dkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWTtXXpEUUN3ME20Nk45ODF6IN88US=> MnvLV2FPT0WU
ES8 NIHke|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2LobWlEPTB;NEOuN|Y6QCEQvF2= NEPLcmlUSU6JRWK=
T-24 NW\lbVFxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NETaRZNKSzVyPUSzMlQ{PjlizszN MXfTRW5ITVJ?
GAMG MoroS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIDWTlZKSzVyPUSzMlQ2OTdizszN MV7TRW5ITVJ?
LU-135 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF2wPFRKSzVyPUS0MlA6OjNizszN NX2yVYRYW0GQR1XS
HCC1187 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn\sTWM2OD12ND64NlYzKM7:TR?= M2LYR3NCVkeHUh?=
TE-1 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUjJR|UxRTR3LkG2OVQh|ryP MWDTRW5ITVJ?
J-RT3-T3-5 NEfkRWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHzyNZhKSzVyPUS1MlQ{OTVizszN NFfpem5USU6JRWK=
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D-392MG NIrue4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXPJR|UxRTR3LkmyOVYh|ryP MVHTRW5ITVJ?
KALS-1 M3PYO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYHJR|UxRTR4LkeyOVch|ryP M4D4dnNCVkeHUh?=
MMAC-SF NWKyd4tuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF\KcWJKSzVyPUS2Mlk6PTJizszN MWTTRW5ITVJ?
HSC-3 MnvIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEXUS3NKSzVyPUS3MlM3ODhizszN MoLsV2FPT0WU
KM-H2 NXLieFFqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1yzUGlEPTB;NEeuOlAxPyEQvF2= MXrTRW5ITVJ?
LoVo M13oN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX\JR|UxRTR6LkGwNFIh|ryP NWr3eotXW0GQR1XS
NCI-H510A NFzYU5VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUPVbI52UUN3ME20PE4yQDdzIN88US=> Ml3MV2FPT0WU
EW-11 M2fuUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmLpTWM2OD12OD6yN|Q5KM7:TR?= M3joN3NCVkeHUh?=
HCC2998 NVS1Znh4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkOwTWM2OD12OD62NlM3KM7:TR?= NILaNnBUSU6JRWK=
J82 MnG5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NY[4UZg5UUN3ME20PE44OjR{IN88US=> MXPTRW5ITVJ?
ML-2 NIjsOINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3TOd2lEPTB;NEmuOFYxPSEQvF2= M{HyRXNCVkeHUh?=
NCI-H2030 M3P3NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV7ySWpYUUN3ME20PU44OTF5IN88US=> NYPJS5FyW0GQR1XS
NCI-H1792 M1Xrc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1rJfmlEPTB;NEmuPFUyQCEQvF2= Mk\vV2FPT0WU

... 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[N](C=N1)C2=CC(=CC(=C2)C(F)(F)F)NC(=O)C3=CC=C(C)C(=C3)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)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)
% DMSO % % Tween 80 % ddH2O
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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 Active not 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.

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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