Nilotinib (AMN-107) 化学構造
分子量: 529.52

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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 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{HJU2lEPTB;MD6wNFAyPDRizszN NF\nVmZUSU6JRWK=
KU812 NVm4UYtpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2\3[2lEPTB;MD6wNFI1QCEQvF2= M2faOnNCVkeHUh?=
EM-2 M3PMbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFjZZmhKSzVyPUCuNFA1OSEQvF2= MYPTRW5ITVJ?
LAMA-84 NFrVXJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFPZdm1KSzVyPUCuNFA1QSEQvF2= M2HWe3NCVkeHUh?=
MEG-01 M2LMR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIT4WZFKSzVyPUCuNFA5OjhizszN MVXTRW5ITVJ?
BV-173 M2rocGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3PweGlEPTB;MD6wNVA5QSEQvF2= NIPJTmZUSU6JRWK=
KASUMI-1 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYPJR|UxRTBwMEK0NVMh|ryP NVKwOFB5W0GQR1XS
NB7 Mnj2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFexUXZKSzVyPUCuNVM1OzlizszN MYHTRW5ITVJ?
BHT-101 M2DNeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NULEcGZtUUN3ME2wMlY1OjZ|IN88US=> M3\EenNCVkeHUh?=
CGTH-W-1 NIDxOoJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mln4TWM2OD1yLk[0PFch|ryP M1i2dXNCVkeHUh?=
HMV-II NFrtPVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYTJR|UxRTBwN{S4O|Qh|ryP MXjTRW5ITVJ?
NKM-1 NG[wWlJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXTKSpliUUN3ME2wMlkxOTVizszN M1zn[3NCVkeHUh?=
LB2241-RCC NFnDOJJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M17uUWlEPTB;MT6wNlIzQCEQvF2= NHqwXZZUSU6JRWK=
NCI-H1703 MlvES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXzobFRLUUN3ME2xMlE5QDdizszN NHPJeJNUSU6JRWK=
BE-13 NFvRemhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF:wOGdKSzVyPUGuNlc1OTZizszN MX\TRW5ITVJ?
ACN MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWG0d3ZXUUN3ME2xMlU2ODd5IN88US=> M2e5TnNCVkeHUh?=
A204 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIHPfIFKSzVyPUGuOVczODVizszN MXzTRW5ITVJ?
HOP-62 NUXHR2lST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUnMOYREUUN3ME2xMlgzODd5IN88US=> M3S4T3NCVkeHUh?=
H9 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkfHTWM2OD1{LkezO|k{KM7:TR?= NEHFbJdUSU6JRWK=
HCC1806 M4rSXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NY\VfXpWUUN3ME2yMlc1OzJ5IN88US=> NWDw[VlqW0GQR1XS
NOS-1 MoLKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFrNZ2RKSzVyPUKuPFcyODJizszN NIqzRoZUSU6JRWK=
RS4-11 NWP1V4x4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2L1S2lEPTB;Mj65NFYzOyEQvF2= MlvjV2FPT0WU
JAR MnvIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVXFNW53UUN3ME2yMlkzODh2IN88US=> NY\u[YF{W0GQR1XS
T98G M4jYUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXrjXmJlUUN3ME2zMlAyOzF|IN88US=> MnHXV2FPT0WU
NCI-SNU-1 NFnxb2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2P3OGlEPTB;Mz60NFA6OiEQvF2= NYPsfnBsW0GQR1XS
SK-MEL-1 NIXBT3VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIXuZoxKSzVyPUOuOFMxOjlizszN M{DrcnNCVkeHUh?=
L-363 NHXmWYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlrjTWM2OD1|Lk[xNVA4KM7:TR?= NHn0[|BUSU6JRWK=
SW982 M{LOZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3Pue2lEPTB;Mz62OFE3QSEQvF2= M{nyNnNCVkeHUh?=
HT-1080 M3HwW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{L6PGlEPTB;Mz65NVc4PSEQvF2= MlLrV2FPT0WU
G-402 NVjLUIR{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M37uc2lEPTB;ND6zNVIxOyEQvF2= MYXTRW5ITVJ?
HOS MoD2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{PRVGlEPTB;ND64NFI5OiEQvF2= M4rBNHNCVkeHUh?=
SK-NEP-1 NXn3[o13T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV;JR|UxRTRwOEOxPVEh|ryP MVLTRW5ITVJ?
HAL-01 MlK5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnTaTWM2OD12Lki4NlQzKM7:TR?= MWfTRW5ITVJ?
SBC-1 NEjM[IVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2jwOGlEPTB;ND65NFkxPyEQvF2= MYTTRW5ITVJ?
CTV-1 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4\ZUmlEPTB;NT60PFk{QCEQvF2= MkXMV2FPT0WU
LCLC-103H NGnMTVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXnJR|UxRTVwN{e0O|Eh|ryP NF[4OZRUSU6JRWK=
RVH-421 NYTHNlF7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGS1bWJKSzVyPUWuO|c2OzZizszN M2D5ZnNCVkeHUh?=
K-562 M{DrXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH3DeHBKSzVyPUWuPVA{PiEQvF2= MWPTRW5ITVJ?
CAL-33 Ml\LS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmLNTWM2OD14LkOxN|U6KM7:TR?= M1HoSXNCVkeHUh?=
MDA-MB-361 MkD2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVzme5JQUUN3ME22MlM{Pjl7IN88US=> M122TnNCVkeHUh?=
IGROV-1 Mn7FS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHTqTFVKSzVyPU[uOFcyQTFizszN MkDDV2FPT0WU
NY MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4LJXmlEPTB;Nj61N|U6QSEQvF2= MX7TRW5ITVJ?
Ramos-2G6-4C10 NHfKSIFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX\NRnBlUUN3ME22MlY3QTNzIN88US=> MVrTRW5ITVJ?
HuO9 M1fFSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWXYNoU3UUN3ME22Mlc{QTZ2IN88US=> NYHvWWI5W0GQR1XS
MS-1 NHXEbllIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MonLTWM2OD15LkGxPVU{KM7:TR?= NV;wVIdwW0GQR1XS
RPMI-8226 NHHzdVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{LUNmlEPTB;Nz6yPFI5PyEQvF2= NXPzW4VxW0GQR1XS
HDLM-2 M4LWfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M17QWGlEPTB;Nz60NFE1QSEQvF2= NULaNmJ7W0GQR1XS
D-566MG M4XqXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlrtTWM2OD15LkS3NVU2KM7:TR?= MVfTRW5ITVJ?
SK-MEL-24 Mmj2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEfNboFKSzVyPUeuOlM{QTJizszN MWTTRW5ITVJ?
COLO-679 NHq4WodIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWXJR|UxRTdwOUi2O|Eh|ryP NXnpSGFrW0GQR1XS
EW-13 NUnMVYtlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mlu2TWM2OD16LkOyNFU1KM7:TR?= NYTQOppNW0GQR1XS
A388 NVLvTmYxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MULJR|UxRThwM{i0PFEh|ryP MV\TRW5ITVJ?
UM-UC-3 NF;uZ4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MULJR|UxRThwNEO5OVYh|ryP MULTRW5ITVJ?
NUGC-3 NI\pZnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUjyOIw4UUN3ME24MlU{PTh{IN88US=> M4\aTnNCVkeHUh?=
COLO-668 NUfJUll3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYrpRlJoUUN3ME24MlU6PDlzIN88US=> NYXGUHQ2W0GQR1XS
MOLT-4 MlzQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NI\HOZpKSzVyPUiuOlI{PTNizszN NVXU[5U{W0GQR1XS
D-423MG M3HHRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1LUV2lEPTB;OD64N|c2PiEQvF2= NITMfYxUSU6JRWK=
CTB-1 NV\JOHN7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3LETmlEPTB;OD64O|EzQCEQvF2= NFfFWmhUSU6JRWK=
BCPAP MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoC5TWM2OD17LkCyOVYzKM7:TR?= MUPTRW5ITVJ?
GCT M{Owdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUDLd5pOUUN3ME25MlA6QDNzIN88US=> MVPTRW5ITVJ?
ACHN NUXGfIVlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3fRbGlEPTB;OT6yN|Y{OiEQvF2= MULTRW5ITVJ?
KYSE-520 MlfMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3S2[WlEPTB;OT6zN|Q5OiEQvF2= NW\QV3lIW0GQR1XS
LB771-HNC MlXNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGr0Z4pKSzVyPUmuO|Y1QTdizszN M{S4W3NCVkeHUh?=
MLMA NYXR[|lvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWXJR|UxRTFyLkCxN|Ih|ryP MVfTRW5ITVJ?
HEC-1 NYPWeotDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlrBTWM2OD1zMD6yPFA1KM7:TR?= NG\seFBUSU6JRWK=
HL-60 NWrTTGpIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3v3TmlEPTB;MUCuOlg2OyEQvF2= NH72d2hUSU6JRWK=
A101D MkfFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NW\LSllTUUN3ME2xNE45QTJ|IN88US=> NF3yXHVUSU6JRWK=
A2058 M1fzO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MY\JR|UxRTFyLkmyOFUh|ryP NGXu[m1USU6JRWK=
KARPAS-45 MmDzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVvVeolZUUN3ME2xNU4xPjN3IN88US=> NUfHcoUyW0GQR1XS
697 NWHadYZzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkPLTWM2OD1zMT6yNVAyKM7:TR?= NXPMSJVtW0GQR1XS
NCI-N87 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M13ENGlEPTB;MUGuO|c{OSEQvF2= NYPkb|JZW0GQR1XS
DSH1 NVfLWVF2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M33XXWlEPTB;MUGuO|k2OyEQvF2= NGjle3RUSU6JRWK=
HLE MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4rqdWlEPTB;MUGuPFg{QSEQvF2= MWfTRW5ITVJ?
NCI-H720 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV;BRpdxUUN3ME2xNk43QDBzIN88US=> M2HEUnNCVkeHUh?=
EW-3 M2rLNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVPJR|UxRTF{LkmzNFch|ryP MmfnV2FPT0WU
AGS MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGjpPVlKSzVyPUGzMlA{PTFizszN M1;jZXNCVkeHUh?=
ES5 NGrsZY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mlu1TWM2OD1zMz6wOVEzKM7:TR?= NIHFeGhUSU6JRWK=
DB M2DkSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYjJR|UxRTF|LkOyOVYh|ryP MYPTRW5ITVJ?
A4-Fuk NHTSbJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFnNSWNKSzVyPUGzMlQyODJizszN NX\YdHllW0GQR1XS
A427 NWnmcYF7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYXJR|UxRTF|LkS5O|Ih|ryP M1TVZXNCVkeHUh?=
MN-60 NHnLW49Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NU\GTmlRUUN3ME2xN{42QDR|IN88US=> NHLCOWhUSU6JRWK=
HCC2218 MmXZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIDkR49KSzVyPUGzMlU5PTZizszN NVvP[JBoW0GQR1XS
MV-4-11 Mm\zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWS3cXZuUUN3ME2xN{45OTN5IN88US=> M3fVR3NCVkeHUh?=
GI-1 M3\sRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWDJR|UxRTF2LkGxPFQh|ryP NH\TUFVUSU6JRWK=
JVM-3 M365O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUjJR|UxRTF2LkK2OVYh|ryP MYHTRW5ITVJ?
NCI-H2029 MorTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFzTXGpKSzVyPUG0MlI4OjdizszN MWTTRW5ITVJ?
TE-12 NGTHepJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGrneXlKSzVyPUG0MlYxPDZizszN NU\lc4ZTW0GQR1XS
WM-115 MkK2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEnJVmtKSzVyPUG1MlU3QDNizszN M4XH[3NCVkeHUh?=
BB65-RCC M{TZV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3zTcGlEPTB;MU[uNFI1OSEQvF2= M1Pp[3NCVkeHUh?=
NCI-H1693 M4Thd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXLOfYI2UUN3ME2xOk4{QDB{IN88US=> MkPGV2FPT0WU
KARPAS-299 M4C0cWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MljhTWM2OD1zNj62NlA{KM7:TR?= MUjTRW5ITVJ?
UACC-257 MmHCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUnJR|UxRTF5LkC1PFIh|ryP M1T4bnNCVkeHUh?=
RKO M1PYW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF:ycnRKSzVyPUG3MlY1OzNizszN NIXjUGZUSU6JRWK=
HT-29 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M13YOWlEPTB;MUeuO|g5QSEQvF2= NFTxdIhUSU6JRWK=
ES7 NUDkUXZPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnLGTWM2OD1zOD6xNVIzKM7:TR?= NYewSIVUW0GQR1XS
DEL NYnKOYJqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUnJR|UxRTF6LkOxO|Ih|ryP NUeyR3lCW0GQR1XS
BT-549 NFP0UpZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHX2ZlZKSzVyPUG4MlQxQTJizszN Mkf3V2FPT0WU
NCI-H1755 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYnJR|UxRTF6LkW3NlMh|ryP MYLTRW5ITVJ?
HCE-T NXvyNIVWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIraVpFKSzVyPUG4Mlg{PDFizszN NGDYXGZUSU6JRWK=
LU-139 M1vDdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1L5V2lEPTB;MUmuNFQ2QCEQvF2= MXPTRW5ITVJ?
ECC10 NEKwZpRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M37zNWlEPTB;MUmuNlQ4PSEQvF2= MVfTRW5ITVJ?
769-P NY\SWplwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFHiOoVKSzVyPUG5MlY{OzVizszN M3L3R3NCVkeHUh?=
BALL-1 NGrwVoNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4DuNmlEPTB;MUmuOlc4PSEQvF2= MVTTRW5ITVJ?
LXF-289 M4rGcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGmzUWdKSzVyPUG5Mlg6PzlizszN NHPsSXFUSU6JRWK=
TYK-nu NE[xU3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{\ScWlEPTB;MUmuPVMyPSEQvF2= NYTRNpZZW0GQR1XS
NCI-H630 M1HlfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYXJR|UxRTF7LkmzO|gh|ryP M2ryUnNCVkeHUh?=
EW-18 Ml23S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{Syd2lEPTB;MkCuN|gxOiEQvF2= NYnwbnFsW0GQR1XS
KYSE-150 Mn\CS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYjJR|UxRTJyLkewOFch|ryP M2HwPHNCVkeHUh?=
LOXIMVI NH3pV4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX;JR|UxRTJyLke1PFYh|ryP MYXTRW5ITVJ?
HuP-T3 M3fzW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHyydYZKSzVyPUKxMlA5PTJizszN MmTwV2FPT0WU
MFE-280 M1y2RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUn6[WtXUUN3ME2yNU42Pjd7IN88US=> NFzzcpBUSU6JRWK=
SK-OV-3 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFLIN2JKSzVyPUKxMlg1ODhizszN MoG4V2FPT0WU
QIMR-WIL M1nQe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnTmTWM2OD1{Mj6wOFc5KM7:TR?= MlPnV2FPT0WU
NCI-H69 M2nTU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGHGcpdKSzVyPUKyMlQzQTlizszN Mli0V2FPT0WU
TE-5 NVLpPGhIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVzPPYoyUUN3ME2yNk41QTZ3IN88US=> MmPUV2FPT0WU
NCI-H1993 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoCxTWM2OD1{Mj60PVcyKM7:TR?= MVnTRW5ITVJ?
NCI-H1092 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWfJR|UxRTJ|LkK4OFMh|ryP Moi4V2FPT0WU
RH-1 M2[1SWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1;TW2lEPTB;MkOuOVM2PyEQvF2= NYDlSG9DW0GQR1XS
DBTRG-05MG M4LONmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1zMXGlEPTB;MkOuPFQ4OiEQvF2= M1;4T3NCVkeHUh?=
Mo-T NFu1UJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVHJR|UxRTJ|Lkmg{txO M1exSnNCVkeHUh?=
HD-MY-Z MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4\PPWlEPTB;MkSuNlM3OiEQvF2= NWfKNodWW0GQR1XS
NCI-H2342 M1\lNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M33aT2lEPTB;MkSuOlc3PyEQvF2= MVjTRW5ITVJ?
C32 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MojXTWM2OD1{ND65OVc3KM7:TR?= M3\DT3NCVkeHUh?=
HTC-C3 MonkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2LMd2lEPTB;MkWuN|U4PyEQvF2= MUPTRW5ITVJ?
NCI-H358 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NW\UeW03UUN3ME2yOU4{QTR|IN88US=> NFzRSYpUSU6JRWK=
CAL-85-1 NEDvW4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUPZ[pMzUUN3ME2yOU41PTd5IN88US=> NWHLNpJzW0GQR1XS
HT-1197 NFLzTVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHnvSldKSzVyPUK1MlU{OTlizszN Mnr4V2FPT0WU
A172 NV;CWXgyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX3JR|UxRTJ3LkexN|Yh|ryP NVjkcoZvW0GQR1XS
SW1573 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXTZV2F6UUN3ME2yOU44Pzh3IN88US=> M2K5[XNCVkeHUh?=
EW-24 M1rk[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH;MPG5KSzVyPUK1Mlk3OiEQvF2= M3XuZnNCVkeHUh?=
SK-MEL-2 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn\CTWM2OD1{Nj6wN|EzKM7:TR?= MofFV2FPT0WU
LU-65 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml;kTWM2OD1{Nj6wOFUzKM7:TR?= MU\TRW5ITVJ?
KMOE-2 NUW1OVhnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXTJR|UxRTJ4LkC5NVUh|ryP M{jFTHNCVkeHUh?=
H-EMC-SS MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHjkfJBKSzVyPUK2MlQyOTRizszN M2L5[HNCVkeHUh?=
H4 M3ruWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVLvVlhJUUN3ME2yOk41OjR|IN88US=> NYfpSJNKW0GQR1XS
DU-4475 M3\Ubmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXvJR|UxRTJ5LkG4O|Ih|ryP NWHwSlBTW0GQR1XS
HCT-116 Ml;iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYLJR|UxRTJ5LkSzOFkh|ryP MnTCV2FPT0WU
MSTO-211H NEDub5JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkjxTWM2OD1{Nz62NlU2KM7:TR?= M2L3WHNCVkeHUh?=
NCI-H292 NVfqbYtUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV7NcWFwUUN3ME2yO{46PjF5IN88US=> MnTrV2FPT0WU
NCI-H446 M2DkW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{HmT2lEPTB;MkiuNlExPSEQvF2= NWq2NmU6W0GQR1XS
NCI-H2009 NGrpcYhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF;Le5BKSzVyPUK5MlE1OzFizszN MoXuV2FPT0WU
MHH-ES-1 Mom0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFmxNnpKSzVyPUK5MlM3QDVizszN NH21VohUSU6JRWK=
TI-73 NV;kellET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHLONJdKSzVyPUK5MlQxODFizszN MULTRW5ITVJ?
NCI-H2228 MlPPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVXJR|UxRTJ7LkS1PEDPxE1? NYLEXHVJW0GQR1XS
MHH-PREB-1 MmTlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYPMNZlRUUN3ME2yPU42PTB3IN88US=> MmjNV2FPT0WU
ChaGo-K-1 MofMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEjSc5ZKSzVyPUK5MlYxQTdizszN NG\HVnhUSU6JRWK=
KY821 MoHYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVXJR|UxRTJ7Lk[0N|Mh|ryP Ml\VV2FPT0WU
NCI-H209 NGP4fFBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3zpXWlEPTB;MkmuPFM3PiEQvF2= NIO5[41USU6JRWK=
NBsusSR MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2HkTmlEPTB;MkmuPVkxPCEQvF2= Mmr5V2FPT0WU
NCI-H1304 NGnSN4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml3yTWM2OD1|MD61O|E3KM7:TR?= NWT5XZJbW0GQR1XS
NB14 MnHCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{i1XmlEPTB;M{GuNFQ1PiEQvF2= MlnyV2FPT0WU
HCC1419 NHvQWGNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4j5OWlEPTB;M{GuNlQh|ryP NF;kXIhUSU6JRWK=
KG-1 M3P4dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX7JR|UxRTNzLke0Nlkh|ryP M{TJc3NCVkeHUh?=
A2780 NVPxW21HT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkTGTWM2OD1|MT64N|U5KM7:TR?= M4LxVHNCVkeHUh?=
NCI-H28 M17KZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFLzb5NKSzVyPUOxMlk5PjFizszN MkPwV2FPT0WU
C2BBe1 NYfhRndUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MW\JR|UxRTN{LkK2N|Qh|ryP NXPGXHVoW0GQR1XS
VA-ES-BJ NGrpVWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXrJR|UxRTN{LkOxJO69VQ>? M1fsbHNCVkeHUh?=
SBC-5 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGLndGJKSzVyPUOyMlg2OTFizszN M3vuUXNCVkeHUh?=
OVCAR-4 Mn7yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3z4TmlEPTB;M{OuOFg1QCEQvF2= Mk\OV2FPT0WU
COR-L88 MkDBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV76dGp[UUN3ME2zOE4xPzRzIN88US=> MkDyV2FPT0WU
SW954 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXrmNYJxUUN3ME2zOE4xPzV{IN88US=> NVPCdZVpW0GQR1XS
COLO-684 MojDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2TMfmlEPTB;M{SuN|QxPCEQvF2= MV\TRW5ITVJ?
HCC70 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV;wT5FiUUN3ME2zOE46PTF2IN88US=> MoTPV2FPT0WU
NCI-H1770 NXXUR417T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmLJTWM2OD1|ND65OlEh|ryP MnP0V2FPT0WU
NCI-H1666 Ml;NS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnTMTWM2OD1|NT64NlU{KM7:TR?= NFTiO2pUSU6JRWK=
YH-13 MojlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NG\JSVNKSzVyPUO1MlkzKM7:TR?= MUXTRW5ITVJ?
DJM-1 MoXYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUTh[GRmUUN3ME2zOk45ODR7IN88US=> MkLDV2FPT0WU
KNS-62 NGLvNVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M365RmlEPTB;M{[uPVQ{QCEQvF2= NETqcXNUSU6JRWK=
SK-MEL-30 NFPwUYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXr0XpBKUUN3ME2zO{45PzN5IN88US=> MnrEV2FPT0WU
SJRH30 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmH1TWM2OD1|OD63N|QyKM7:TR?= NVjrWJNZW0GQR1XS
GP5d NYe1e3VRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MU\JR|UxRTN6Lki2OVMh|ryP M2PsR3NCVkeHUh?=
SW1116 NXLNbo5RT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEjWTXdKSzVyPUO5MlI5ODVizszN MkXlV2FPT0WU
COLO-800 NEfF[VdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3TkNmlEPTB;M{muN|Y{QCEQvF2= M2\4SnNCVkeHUh?=
RD MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M33KWWlEPTB;M{muOVI2QCEQvF2= MmXQV2FPT0WU
NCI-SNU-5 NHHJco1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{js[WlEPTB;M{muOlkyPiEQvF2= NIfnb2NUSU6JRWK=
HuO-3N1 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MonZTWM2OD12MD6xNFgh|ryP NH\1dVJUSU6JRWK=
SK-UT-1 M2HxUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF7mWGVKSzVyPUSwMlU3PzRizszN M3jPcnNCVkeHUh?=
SK-MEL-3 NI\1eVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYTvO4NRUUN3ME20NE42QTN{IN88US=> NVPWPHJsW0GQR1XS
SK-MEL-28 NF\KbFNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NW\aeXVsUUN3ME20NE43PDN3IN88US=> MYLTRW5ITVJ?
SCC-4 MnvmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXPJR|UxRTRzLkKxN|ch|ryP M1T6WnNCVkeHUh?=
no-11 NYrKfW12T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4eyNGlEPTB;NEGuO|M2PCEQvF2= MVvTRW5ITVJ?
HT-144 MofFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVTJR|UxRTR{LkC1Olch|ryP NF\GPHlUSU6JRWK=
MFM-223 NEPVO4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoLnTWM2OD12Mj60NFIh|ryP M2fjVHNCVkeHUh?=
ONS-76 NX3X[3pZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYLxXZM{UUN3ME20Nk45ODF6IN88US=> M2nIOHNCVkeHUh?=
ES8 NUTGPIx5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4\qNGlEPTB;NEOuN|Y6QCEQvF2= NVTafo5kW0GQR1XS
T-24 NFi1[o5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYPJR|UxRTR|LkSzOlkh|ryP M1jJWHNCVkeHUh?=
GAMG NXXNVpo4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVqzPHlPUUN3ME20N{41PTF5IN88US=> NY\nPZpoW0GQR1XS
LU-135 NYfiVWpVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoTlTWM2OD12ND6wPVI{KM7:TR?= MXzTRW5ITVJ?
HCC1187 NH\vfmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mnq4TWM2OD12ND64NlYzKM7:TR?= M4S0XnNCVkeHUh?=
TE-1 MnXhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{\HRWlEPTB;NEWuNVY2PCEQvF2= MXHTRW5ITVJ?
J-RT3-T3-5 NHvjN3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXPJR|UxRTR3LkSzNVUh|ryP MonuV2FPT0WU
GI-ME-N MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1XPTGlEPTB;NEWuPFk2OiEQvF2= NHHBNFVUSU6JRWK=
D-392MG NHPk[VhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUe0bZY2UUN3ME20OU46OjV4IN88US=> MknvV2FPT0WU
KALS-1 MlztS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXLtSXdRUUN3ME20Ok44OjV5IN88US=> MWnTRW5ITVJ?
MMAC-SF M3TPb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{SyXGlEPTB;NE[uPVk2OiEQvF2= NHvQR4NUSU6JRWK=
HSC-3 M4r6R2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4GxSWlEPTB;NEeuN|YxQCEQvF2= Ml30V2FPT0WU
KM-H2 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoKwTWM2OD12Nz62NFA4KM7:TR?= MY\TRW5ITVJ?
LoVo M4DVe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWjJR|UxRTR6LkGwNFIh|ryP MYfTRW5ITVJ?
NCI-H510A M4HETWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnLwTWM2OD12OD6xPFcyKM7:TR?= NXzDfolWW0GQR1XS
EW-11 NWrPe|lIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGjmTo1KSzVyPUS4MlI{PDhizszN M13ZTHNCVkeHUh?=
HCC2998 M1zLZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYLJR|UxRTR6Lk[yN|Yh|ryP NHLkNIlUSU6JRWK=
J82 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX7oXnRkUUN3ME20PE44OjR{IN88US=> MV\TRW5ITVJ?
ML-2 M1TRXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{Dq[2lEPTB;NEmuOFYxPSEQvF2= NV\aW29SW0GQR1XS
NCI-H2030 M1rRZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3vwb2lEPTB;NEmuO|EyPyEQvF2= M3HCeHNCVkeHUh?=
NCI-H1792 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXH3UGdLUUN3ME20PU45PTF6IN88US=> NHTyfGxUSU6JRWK=

... 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 3年-20℃
2年-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 27 mg/mL (50.98 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
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

文献中の引用 (19)

技術サポート&よくある質問(FAQ)

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最近チェックしたアイテム

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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