Nilotinib (AMN-107) 化学構造
分子量: 529.52

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Quality Control & MSDS

製品説明

  • Compare Bcr-Abl Inhibitors
    Bcr-Abl製品生物活性の比較
  • 研究分野
  • Combination Therapy
    併用療法

製品の説明

生物活性

製品説明 Nilotinib (AMN-107)は、30nM未満のIC50によるBcr-Abl阻害剤です。
ターゲット Bcr-Abl
IC50 30 nM [1]
In vitro試験 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 LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
EoL-1-cell M{HxTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmnoTWM2OD1yLkCwNFE1PCEQvF2= NIXm[pZUSU6JRWK=
KU812 Mnn5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVTJR|UxRTBwMECyOFgh|ryP NFTmUphUSU6JRWK=
EM-2 MljTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHT3U4JKSzVyPUCuNFA1OSEQvF2= MXvTRW5ITVJ?
LAMA-84 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2LsO2lEPTB;MD6wNFQ6KM7:TR?= M3HrfnNCVkeHUh?=
MEG-01 M3fJRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NE\TW2JKSzVyPUCuNFA5OjhizszN Mlz3V2FPT0WU
BV-173 M1fWRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3zyOmlEPTB;MD6wNVA5QSEQvF2= MkPWV2FPT0WU
KASUMI-1 MnHLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHTqRlFKSzVyPUCuNFI1OTNizszN M2T4WHNCVkeHUh?=
NB7 NFjwOXBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2jmRWlEPTB;MD6xN|Q{QSEQvF2= NVnuO41xW0GQR1XS
BHT-101 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4nU[2lEPTB;MD62OFI3OyEQvF2= M1PYcnNCVkeHUh?=
CGTH-W-1 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEHOSIFKSzVyPUCuOlQ5PyEQvF2= NYrFOFRCW0GQR1XS
HMV-II NE\RdnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWnHeFdvUUN3ME2wMlc1QDd2IN88US=> M3\vfXNCVkeHUh?=
NKM-1 M4LvXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoPuTWM2OD1yLkmwNVUh|ryP NVHqeGc1W0GQR1XS
LB2241-RCC MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHXSZ4FKSzVyPUGuNFIzOjhizszN NXn1[I0zW0GQR1XS
NCI-H1703 NH62OXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWTJR|UxRTFwMUi4O{DPxE1? M1[2fnNCVkeHUh?=
BE-13 NGHqXWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1vNd2lEPTB;MT6yO|QyPiEQvF2= M3;wN3NCVkeHUh?=
ACN NEPGV|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIrnR5dKSzVyPUGuOVUxPzdizszN MUXTRW5ITVJ?
A204 M{D4dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH3xfG1KSzVyPUGuOVczODVizszN NXPXdZoxW0GQR1XS
HOP-62 NGDLNlFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3;xSWlEPTB;MT64NlA4PyEQvF2= MUDTRW5ITVJ?
H9 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NInK[pZKSzVyPUKuO|M4QTNizszN NFe4Z29USU6JRWK=
HCC1806 NVH4XGRxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHfZdJJKSzVyPUKuO|Q{OjdizszN NWexeIUxW0GQR1XS
NOS-1 MlfOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1qyc2lEPTB;Mj64O|ExOiEQvF2= MnPXV2FPT0WU
RS4-11 M{Lk[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUS3S4RTUUN3ME2yMlkxPjJ|IN88US=> NIH3Z3lUSU6JRWK=
JAR MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYjJR|UxRTJwOUKwPFQh|ryP MXjTRW5ITVJ?
T98G M2fZOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkXyTWM2OD1|LkCxN|E{KM7:TR?= M4rETXNCVkeHUh?=
NCI-SNU-1 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF3FboFKSzVyPUOuOFAxQTJizszN M1nrZ3NCVkeHUh?=
SK-MEL-1 NYTGclhpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{LmRWlEPTB;Mz60N|AzQSEQvF2= NHSxfnVUSU6JRWK=
L-363 M{TxWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NY\BWIxDUUN3ME2zMlYyOTB5IN88US=> MW\TRW5ITVJ?
SW982 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkfFTWM2OD1|Lk[0NVY6KM7:TR?= MVTTRW5ITVJ?
HT-1080 MoH2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{K0TmlEPTB;Mz65NVc4PSEQvF2= MWXTRW5ITVJ?
G-402 NEW0[VRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYXMXG4yUUN3ME20MlMyOjB|IN88US=> NXTPeHpQW0GQR1XS
HOS MnLnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUTqNFJ2UUN3ME20MlgxOjh{IN88US=> MmD5V2FPT0WU
SK-NEP-1 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIT2WnNKSzVyPUSuPFMyQTFizszN NWDsXnpRW0GQR1XS
HAL-01 MmLnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVHJR|UxRTRwOEiyOFIh|ryP NIDrU45USU6JRWK=
SBC-1 NYO1[Io4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkXjTWM2OD12LkmwPVA4KM7:TR?= M1;aWXNCVkeHUh?=
CTV-1 M3zK[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUHUcmJPUUN3ME21MlQ5QTN6IN88US=> M1rCSXNCVkeHUh?=
LCLC-103H NYrneWRCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFPxNodKSzVyPUWuO|c1PzFizszN MnTjV2FPT0WU
RVH-421 M4Ly[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV;JR|UxRTVwN{e1N|Yh|ryP NWjrSlA5W0GQR1XS
K-562 M2TRU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWnFfW5LUUN3ME21MlkxOzZizszN MWXTRW5ITVJ?
CAL-33 Mly2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1XVVmlEPTB;Nj6zNVM2QSEQvF2= MoC5V2FPT0WU
MDA-MB-361 NUT2WWZ3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIDzOY9KSzVyPU[uN|M3QTlizszN NHq5T|hUSU6JRWK=
IGROV-1 NITGOYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYTJR|UxRTZwNEexPVEh|ryP NHfhfmdUSU6JRWK=
NY M{HZVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MknZTWM2OD14LkWzOVk6KM7:TR?= M4naeHNCVkeHUh?=
Ramos-2G6-4C10 M1Hy[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUPJR|UxRTZwNk[5N|Eh|ryP NXr0bWoyW0GQR1XS
HuO9 NUe0doxZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEHlNGtKSzVyPU[uO|M6PjRizszN NID2fJBUSU6JRWK=
MS-1 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXXJR|UxRTdwMUG5OVMh|ryP NXjzb4xCW0GQR1XS
RPMI-8226 NG\aWW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1\uS2lEPTB;Nz6yPFI5PyEQvF2= MYTTRW5ITVJ?
HDLM-2 M1;MVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3fnU2lEPTB;Nz60NFE1QSEQvF2= M2jINnNCVkeHUh?=
D-566MG NUDPZZMyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmL5TWM2OD15LkS3NVU2KM7:TR?= MYLTRW5ITVJ?
SK-MEL-24 NVzIUFBDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH21TW1KSzVyPUeuOlM{QTJizszN NULZNm5VW0GQR1XS
COLO-679 M2niRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MULJR|UxRTdwOUi2O|Eh|ryP NXWyeZhmW0GQR1XS
EW-13 NXnHflV3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGHIPXdKSzVyPUiuN|IxPTRizszN NXHLWIVZW0GQR1XS
A388 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHn6OWZKSzVyPUiuN|g1QDFizszN M3TUXnNCVkeHUh?=
UM-UC-3 NHfLNolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXnJR|UxRThwNEO5OVYh|ryP MmDSV2FPT0WU
NUGC-3 NXWzblRyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3nXUmlEPTB;OD61N|U5OiEQvF2= MYfTRW5ITVJ?
COLO-668 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3[xZ2lEPTB;OD61PVQ6OSEQvF2= MUDTRW5ITVJ?
MOLT-4 MnzaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXTJR|UxRThwNkKzOVMh|ryP M{HsZ3NCVkeHUh?=
D-423MG NVXaUmF[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmDrTWM2OD16LkizO|U3KM7:TR?= MVzTRW5ITVJ?
CTB-1 M4nQcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWnJR|UxRThwOEexNlgh|ryP MVzTRW5ITVJ?
BCPAP MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1LaW2lEPTB;OT6wNlU3OiEQvF2= NVKxTpJsW0GQR1XS
GCT NH:yUoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUfMfIdkUUN3ME25MlA6QDNzIN88US=> NYTDeZN{W0GQR1XS
ACHN MmHGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXLJR|UxRTlwMkO2N|Ih|ryP NIfmNJBUSU6JRWK=
KYSE-520 NVOxb5dYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUDJR|UxRTlwM{O0PFIh|ryP NXnMTI1DW0GQR1XS
LB771-HNC NUD2c5cxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUjPOWg4UUN3ME25Mlc3PDl5IN88US=> MoO1V2FPT0WU
MLMA Ml3HS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkfITWM2OD1zMD6wNVMzKM7:TR?= MVPTRW5ITVJ?
HEC-1 M1K2cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2TkV2lEPTB;MUCuNlgxPCEQvF2= NF3jZoVUSU6JRWK=
HL-60 MmHlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYDYcFJsUUN3ME2xNE43QDV|IN88US=> MkPXV2FPT0WU
A101D NVTLZYJlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkPaTWM2OD1zMD64PVI{KM7:TR?= MWLTRW5ITVJ?
A2058 M1XMNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml;LTWM2OD1zMD65NlQ2KM7:TR?= NHrMZWFUSU6JRWK=
KARPAS-45 NY\FPXBFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXP1dXl7UUN3ME2xNU4xPjN3IN88US=> NVXSSmxqW0GQR1XS
697 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXLJR|UxRTFzLkKxNFEh|ryP NEnvfm1USU6JRWK=
NCI-N87 Moe4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFjCUVhKSzVyPUGxMlc4OzFizszN NV2yOYp{W0GQR1XS
DSH1 NUnNOGI1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHOwUIFKSzVyPUGxMlc6PTNizszN NYXCc2hWW0GQR1XS
HLE MoPGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVfJR|UxRTFzLki4N|kh|ryP M{LMcHNCVkeHUh?=
NCI-H720 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoewTWM2OD1zMj62PFAyKM7:TR?= NFS3TWRUSU6JRWK=
EW-3 M3zpXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{jFTGlEPTB;MUKuPVMxPyEQvF2= NHzI[llUSU6JRWK=
AGS NITa[JBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXHJR|UxRTF|LkCzOVEh|ryP NF71NWtUSU6JRWK=
ES5 NFLtTHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWnJR|UxRTF|LkC1NVIh|ryP MWnTRW5ITVJ?
DB Ml;TS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX;JR|UxRTF|LkOyOVYh|ryP NH;4UoxUSU6JRWK=
A4-Fuk NWTLSYhZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFTpV3JKSzVyPUGzMlQyODJizszN NFTXc2pUSU6JRWK=
A427 NH\Ec4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYe4TmtkUUN3ME2xN{41QTd{IN88US=> NETlWVVUSU6JRWK=
MN-60 NWHi[2dST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXPGR4JjUUN3ME2xN{42QDR|IN88US=> M4jLRnNCVkeHUh?=
HCC2218 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3SyN2lEPTB;MUOuOVg2PiEQvF2= MVnTRW5ITVJ?
MV-4-11 NV\acIgxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVj0No5RUUN3ME2xN{45OTN5IN88US=> M4DXeXNCVkeHUh?=
GI-1 NVm4eItJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXTLfpdVUUN3ME2xOE4yOTh2IN88US=> MUfTRW5ITVJ?
JVM-3 M1\idmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX7JR|UxRTF2LkK2OVYh|ryP MUXTRW5ITVJ?
NCI-H2029 M2DId2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NI\TOY1KSzVyPUG0MlI4OjdizszN NFq4R4dUSU6JRWK=
TE-12 Mmj5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGTFfYZKSzVyPUG0MlYxPDZizszN M1fjbHNCVkeHUh?=
WM-115 NYf1XlNpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mkf3TWM2OD1zNT61Olg{KM7:TR?= MkWzV2FPT0WU
BB65-RCC M2W3cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1mySmlEPTB;MU[uNFI1OSEQvF2= M4DaTnNCVkeHUh?=
NCI-H1693 MlGxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{\rXmlEPTB;MU[uN|gxOiEQvF2= M3qxRXNCVkeHUh?=
KARPAS-299 NGnoNZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmL0TWM2OD1zNj62NlA{KM7:TR?= MoLRV2FPT0WU
UACC-257 NGf6THhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXK4VYt6UUN3ME2xO{4xPTh{IN88US=> MV7TRW5ITVJ?
RKO NUjOUXdIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4D1NGlEPTB;MUeuOlQ{OyEQvF2= M4qzb3NCVkeHUh?=
HT-29 M3;OUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml3BTWM2OD1zNz63PFg6KM7:TR?= MlG1V2FPT0WU
ES7 M4X3dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3PVZ2lEPTB;MUiuNVEzOiEQvF2= M3nwO3NCVkeHUh?=
DEL NX;jN3ZkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoP1TWM2OD1zOD6zNVczKM7:TR?= Ml6yV2FPT0WU
BT-549 MnKxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmjFTWM2OD1zOD60NFkzKM7:TR?= MV3TRW5ITVJ?
NCI-H1755 M3O5fmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYDJR|UxRTF6LkW3NlMh|ryP NY\oSWtYW0GQR1XS
HCE-T NVLRNVByT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnXHTWM2OD1zOD64N|QyKM7:TR?= MmjvV2FPT0WU
LU-139 M2\XdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnPvTWM2OD1zOT6wOFU5KM7:TR?= MXzTRW5ITVJ?
ECC10 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWH6e|dZUUN3ME2xPU4zPDd3IN88US=> MWPTRW5ITVJ?
769-P M2\wVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlPjTWM2OD1zOT62N|M2KM7:TR?= M3riWnNCVkeHUh?=
BALL-1 NIPNdFJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUXJR|UxRTF7Lk[3O|Uh|ryP NUiyc4UzW0GQR1XS
LXF-289 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUHzWoFqUUN3ME2xPU45QTd7IN88US=> NFPkdJpUSU6JRWK=
TYK-nu NIHRfFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWf2WVVIUUN3ME2xPU46OzF3IN88US=> MVjTRW5ITVJ?
NCI-H630 NUXaSm1WT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVK1[Y9ZUUN3ME2xPU46Ozd6IN88US=> NInrTHRUSU6JRWK=
EW-18 M2LwNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NE\6dGtKSzVyPUKwMlM5ODJizszN NETGUGRUSU6JRWK=
KYSE-150 MknES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVHWTnp1UUN3ME2yNE44ODR5IN88US=> MULTRW5ITVJ?
LOXIMVI NYfJS|dQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVrJR|UxRTJyLke1PFYh|ryP NVXpR2hVW0GQR1XS
HuP-T3 NVv5S2llT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mo\vTWM2OD1{MT6wPFUzKM7:TR?= M{L0V3NCVkeHUh?=
MFE-280 NXK1XHJKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{HuO2lEPTB;MkGuOVY4QSEQvF2= NXnRbpVvW0GQR1XS
SK-OV-3 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2XDNmlEPTB;MkGuPFQxQCEQvF2= MVrTRW5ITVJ?
QIMR-WIL NUXrU2lVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MknFTWM2OD1{Mj6wOFc5KM7:TR?= M1;0RnNCVkeHUh?=
NCI-H69 NFfPd2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M17SR2lEPTB;MkKuOFI6QSEQvF2= MnvzV2FPT0WU
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NCI-H1993 MoDjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHfJdItKSzVyPUKyMlQ6PzFizszN MX7TRW5ITVJ?
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J82 NWTNRop2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmW4TWM2OD12OD63NlQzKM7:TR?= NYrUdoh5W0GQR1XS
ML-2 NF7jOVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWLsRYNFUUN3ME20PU41PjB3IN88US=> NUm3RZRZW0GQR1XS
NCI-H2030 NWS4cY5lT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYDJR|UxRTR7LkexNVch|ryP NX\MSFhIW0GQR1XS
NCI-H1792 NHnRWpRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVnsZY42UUN3ME20PU45PTF6IN88US=> NV24TWNVW0GQR1XS

... Click to View More Cell Line Experimental Data

In vivo試験 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]
臨床試験 Nilotinib has entered in a phase IV clinical trial in the treatment of philadelphia chromosome positive and chronic myelogenous leukemia in chronic phase.
特集 A selective inhibitor of native and mutant Bcr-Abl.

プロトコル (参考用のみ)

細胞アッセイ: [4]

細胞株 Human primary Schwann and schwannoma cells
濃度 1-10 μM
反応時間 72 hours
実験の流れ 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.

動物実験: [6]

動物モデル 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
製剤 10% NMP-90% PEG300, PEG300
投薬量 75 mg/kg, 100 mg/kg
投与方法 Oral administration

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)0.020.151.80.40.0810312
Body Surface Area (m2)0.0070.0250.150.050.020.50.240.6
Km factor361285201220
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

参考

化学情報

Download Nilotinib (AMN-107) SDF
分子量 529.52
化学式

C28H22F3N7O

CAS No. 641571-10-0
保管 2年-20℃
6月-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 27 mg/mL (50.98 mM)
<1 mg/mL (<1 mM)
エタノール <1 mg/mL (<1 mM)
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.
化学名 4-methyl-N-(3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)phenyl)-3-(4-(pyridin-3-yl)pyrimidin-2-ylamino)benzamide

カスタマーフィードバック (5)


Click to enlarge
Rating
Source FASEB J , 2011, 25, 3661-3673. Nilotinib (AMN-107) purchased from Selleck
Method Analyzing cell apoptosis
Cell Lines Ba/F3-p210T315I cells
Concentrations 0-5 μM
Incubation Time 24 h
Results In a parallel study using imatinib/PDMP or nilotinib/PDMP combinations, to our surprise, similar significant synergy in Ba/F3-p210T315I cells was observed.

Click to enlarge
Rating
Source Molecules, 2014, 19, 3356-75. Nilotinib (AMN-107) purchased from Selleck
Method Western blot
Cell Lines K562, CD34+CD38- cells
Concentrations 0, 0.01, 0.1, 1 uM
Incubation Time 12 h
Results Since nilotinib targets the Bcr-Abl kinase in CML cells, we evaluated its ability to inhibit kinase activity in ABCB1- and ABCG2-overexpressing CD34+CD38- cells. In K562 cells, nilotinib effectively inhibited the phosphorylation of Bcr-Abl and CrkL (a surrogate marker of Bcr-Abl activity) at a concentration of 0.1 umol/L. However, in CD34+CD38- cells, nilotinib failed to completely inhibit the phosphorylation of Bcr-Abl and CrkL even when cells were exposed to concentration up to 1.0 umol/L.

Click to enlarge
Rating
Source Leukemia Res, 2012, 36, 1311-1314. Nilotinib (AMN-107) purchased from Selleck
Method Thymidine uptake Uptake assay
Cell Lines K562, MEG-01 cells
Concentrations 0.1-10uM
Incubation Time 20 min
Results Nilotinib was much more potent than imatinib to inhibit nucleoside transport. It prevented the uptake of thymidine in K562 cells by 97% at 10 uM, a level that was similar to the one obtained with the vasodilatator molecule dipyridamole. Nilotinib was also very efficient at 1 and 0.1 uM; it blocked the entry of thymidine by 90 and 74%, respectively (Fig. 2a). With the MEG-01 cell line, nilotinib was also extremely potent and blocked the entry of thymidine by 96, 92 and 60% with 10, 1 and 0.1 uM nilotinib, respectively (Fig. 2b).

Click to enlarge
Rating
Source Urol Oncol, 2014, 0.1016/j.urolonc.2014.06.001. Nilotinib (AMN-107) purchased from Selleck
Method Immunoblot analyses
Cell Lines LNCaP, PC-3, DU-145 cells
Concentrations 10 uM
Incubation Time 24 h
Results It shows a robust overexpression of phospho-ERK1/2 T202/Y204 in nilotinib-treated DU-145 cells (B). An up-regulation of phospho-ERK1/2 T202/Y204 was also detectable in nilotinib-treated LNCaP cells, albeit at a lower level, and was not found in PC-3 cells (C).

Click to enlarge
Rating
Source Urol Oncol, 2014, 0.1016/j.urolonc.2014.06.001. Nilotinib (AMN-107) purchased from Selleck
Method Immunohistochemical staining
Cell Lines Xenografted DU-145 cells
Concentrations 5 mg/kg/d
Incubation Time 21 days
Results Accoding to published animals experiments, DU-145 xenografts from a representative experiment in which nilotinib was used at a 75-mg/kg/d concentration. It's found a significant increase of phospho-ERK-positive residual tumor cells from a mean of 67.5 cells per high-powerfield in controls to 131.1 cells per high-powerfield in DU-145 xenografts treated for 21 days with nilotinib (P< 0.0005).

文献中の引用 (18)

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Related Bcr-Abl 阻害剤

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    PX-478 2HCl is an orally active, and selective hypoxia-inducible factor-1α (HIF-1α) inhibitor. Phase 1.

  • Defactinib (VS-6063, PF-04554878)

    Defactinib (VS-6063, PF-04554878) is a selective, and orally active FAK inhibitor. Phase 2.

  • SU6656

    SU 6656 is a selective Src family kinase inhibitor with IC50 of 280 nM, 20 nM, 130 nM, and 170 nM for Src, Yes, Lyn, and Fyn, respectively.

  • Dasatinib Monohydrate

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  • Imatinib Mesylate (STI571)

    Imatinib Mesylate (STI571) は口でImatinibの生物学的利用能メシラート塩です。そして、それは v-Ablc-KitPDGFRのマルチターゲット阻害剤で、IC50 がそれぞれ 0.6 μM、 0.1 μM、 0.1 μMです。

  • Ponatinib (AP24534)

    Ponatinib (AP24534) は、PI3KγとPI4KIIIβの新しくて強力な阻害剤で、IC50 がそれぞれ16 nM と 19 nMになる。

  • Bafetinib (INNO-406)

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    Features:Dual Bcr-Abl/Lyn inhibitor.

  • Degrasyn (WP1130)

    Degrasyn (WP1130)は、選択的な非ユビキチンアーゼ(DUB)阻害剤です。WP1130は、5人のダブズを妨げます:USP5、UCH-L1、USP9x、USP14とUCH37。

    Features:WP1130 has an advantage over imatinib mesylate in that its activity is not inhibited by a variety of Abl kinase mutations, including T315I.

  • DCC-2036 (Rebastinib)

    DCC-2036 (Rebastinib)は、Abl1とT315I Abl1の構造的な支配阻害剤で、IC50 がそれぞれ 0.8 nM と 4 nMです。

    Features:A conformational control inhibitor of Abl1 and T315I Abl1.

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