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)は一種のBcr-Abl阻害剤で、マウス類骨髄前駆細胞の中にIC50値が30 nM以下です。
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 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYDRZ21rUUN3ME2wMlAxODF2NDFOwG0> MnHmV2FPT0WU
KU812 NX\MXVd[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmPNTWM2OD1yLkCwNlQ5KM7:TR?= NV\ndG5lW0GQR1XS
EM-2 M4nWdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2D3OGlEPTB;MD6wNFQyKM7:TR?= NH\XTY1USU6JRWK=
LAMA-84 NHLzcIFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVPqboFWUUN3ME2wMlAxPDlizszN NF3Vb|hUSU6JRWK=
MEG-01 Ml3QS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{PDNGlEPTB;MD6wNFgzQCEQvF2= MULTRW5ITVJ?
BV-173 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2\GXWlEPTB;MD6wNVA5QSEQvF2= MonFV2FPT0WU
KASUMI-1 NIjWc2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MU\JR|UxRTBwMEK0NVMh|ryP MWLTRW5ITVJ?
NB7 NUXVT21CT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVHJR|UxRTBwMUO0N|kh|ryP MWLTRW5ITVJ?
BHT-101 NYrxOmVZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFjRfJVKSzVyPUCuOlQzPjNizszN NXnmb5FKW0GQR1XS
CGTH-W-1 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF;oOFZKSzVyPUCuOlQ5PyEQvF2= MYjTRW5ITVJ?
HMV-II M3P0d2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVq0NYxXUUN3ME2wMlc1QDd2IN88US=> MkX1V2FPT0WU
NKM-1 Mn[yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{HHUWlEPTB;MD65NFE2KM7:TR?= NEjKWlJUSU6JRWK=
LB2241-RCC MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NY\VU5o4UUN3ME2xMlAzOjJ6IN88US=> M3u2NHNCVkeHUh?=
NCI-H1703 NVTsRYNOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYHDeZB[UUN3ME2xMlE5QDdizszN NXrQcYhQW0GQR1XS
BE-13 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV:0OnR[UUN3ME2xMlI4PDF4IN88US=> M1\hfXNCVkeHUh?=
ACN NVLuO4hVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFjVV5FKSzVyPUGuOVUxPzdizszN MYTTRW5ITVJ?
A204 M3TzdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MojaTWM2OD1zLkW3NlA2KM7:TR?= NG\Od4JUSU6JRWK=
HOP-62 NF\hUopIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1XI[WlEPTB;MT64NlA4PyEQvF2= M4fpVXNCVkeHUh?=
H9 NXHZWJd7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYLtWGt1UUN3ME2yMlc{Pzl|IN88US=> M{LlWnNCVkeHUh?=
HCC1806 NE\pe|JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXrsW5diUUN3ME2yMlc1OzJ5IN88US=> NYHpe2sxW0GQR1XS
NOS-1 NF;LS41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnmzTWM2OD1{Lki3NVAzKM7:TR?= NUXCVlNOW0GQR1XS
RS4-11 NGraSmhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGHYT5VKSzVyPUKuPVA3OjNizszN NEHue5dUSU6JRWK=
JAR NX3FdYtTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1rJUWlEPTB;Mj65NlA5PCEQvF2= NX7hPHNjW0GQR1XS
T98G M1;JfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV\JR|UxRTNwMEGzNVMh|ryP NVe4XnU2W0GQR1XS
NCI-SNU-1 NHL2dGdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1W4fGlEPTB;Mz60NFA6OiEQvF2= Mm\WV2FPT0WU
SK-MEL-1 NECyW2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4rN[2lEPTB;Mz60N|AzQSEQvF2= MXzTRW5ITVJ?
L-363 NEKwSWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWCyXmhSUUN3ME2zMlYyOTB5IN88US=> NVnxR|lJW0GQR1XS
SW982 M3;j[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnHKTWM2OD1|Lk[0NVY6KM7:TR?= NWfrdnh2W0GQR1XS
HT-1080 MmPXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXPjXVluUUN3ME2zMlkyPzd3IN88US=> M3XiZXNCVkeHUh?=
G-402 NGq3OXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHe4XG1KSzVyPUSuN|EzODNizszN NYLweohqW0GQR1XS
HOS NUnvZpc{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1X1emlEPTB;ND64NFI5OiEQvF2= NFqySWRUSU6JRWK=
SK-NEP-1 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4PZZ2lEPTB;ND64N|E6OSEQvF2= MoXIV2FPT0WU
HAL-01 M4PVcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3Hjd2lEPTB;ND64PFI1OiEQvF2= MWXTRW5ITVJ?
SBC-1 NEO4TJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWnJR|UxRTRwOUC5NFch|ryP MXrTRW5ITVJ?
CTV-1 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M17JWGlEPTB;NT60PFk{QCEQvF2= MkfnV2FPT0WU
LCLC-103H MoPnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYP5U|l{UUN3ME21Mlc4PDdzIN88US=> M4K0XHNCVkeHUh?=
RVH-421 M2DnO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{jKbGlEPTB;NT63O|U{PiEQvF2= MV7TRW5ITVJ?
K-562 NGrp[pRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmTiTWM2OD13LkmwN|Yh|ryP MoHMV2FPT0WU
CAL-33 NInHWndIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkTPTWM2OD14LkOxN|U6KM7:TR?= MWjTRW5ITVJ?
MDA-MB-361 NFPtXFRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGPITZRKSzVyPU[uN|M3QTlizszN NUnZe45kW0GQR1XS
IGROV-1 NV3oO41xT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFLLfndKSzVyPU[uOFcyQTFizszN NGnYUY9USU6JRWK=
NY MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYjJR|UxRTZwNUO1PVkh|ryP MYPTRW5ITVJ?
Ramos-2G6-4C10 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoHqTWM2OD14Lk[2PVMyKM7:TR?= NFL1bmtUSU6JRWK=
HuO9 M{XMdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1;2cmlEPTB;Nj63N|k3PCEQvF2= MWLTRW5ITVJ?
MS-1 Mn;nS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUD2TIZKUUN3ME23MlEyQTV|IN88US=> NHm4UXZUSU6JRWK=
RPMI-8226 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVrJR|UxRTdwMkiyPFch|ryP MU\TRW5ITVJ?
HDLM-2 M1ixVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYTu[mU5UUN3ME23MlQxOTR7IN88US=> MkK0V2FPT0WU
D-566MG MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoLTTWM2OD15LkS3NVU2KM7:TR?= M{DVNXNCVkeHUh?=
SK-MEL-24 NF3qWo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXm4UXViUUN3ME23MlY{Ozl{IN88US=> MoDCV2FPT0WU
COLO-679 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVvtPJc5UUN3ME23Mlk5PjdzIN88US=> NH3ocI9USU6JRWK=
EW-13 NHLrOZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVzJR|UxRThwM{KwOVQh|ryP M1nifnNCVkeHUh?=
A388 NWe3foRST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MofSTWM2OD16LkO4OFgyKM7:TR?= NVHlNlJ1W0GQR1XS
UM-UC-3 MmjnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mo\JTWM2OD16LkSzPVU3KM7:TR?= MmmzV2FPT0WU
NUGC-3 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3n4N2lEPTB;OD61N|U5OiEQvF2= MkfFV2FPT0WU
COLO-668 M2D0RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVLJR|UxRThwNUm0PVEh|ryP NXXSTW9CW0GQR1XS
MOLT-4 NHqx[ZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV[4TIN7UUN3ME24MlYzOzV|IN88US=> NGLOfFRUSU6JRWK=
D-423MG MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MorrTWM2OD16LkizO|U3KM7:TR?= NV\RT4llW0GQR1XS
CTB-1 NELmbJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIDJeGxKSzVyPUiuPFcyOjhizszN MoizV2FPT0WU
BCPAP NXO1ZXpOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFfaellKSzVyPUmuNFI2PjJizszN MnPUV2FPT0WU
GCT NE\TcWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXjJR|UxRTlwMEm4N|Eh|ryP MnO4V2FPT0WU
ACHN NH;teXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1nUeGlEPTB;OT6yN|Y{OiEQvF2= NVfaN|RZW0GQR1XS
KYSE-520 M2L4NGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV7JR|UxRTlwM{O0PFIh|ryP M3zyZnNCVkeHUh?=
LB771-HNC NGHGR2hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkjtTWM2OD17Lke2OFk4KM7:TR?= M3jVTnNCVkeHUh?=
MLMA M4jVOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M37sOWlEPTB;MUCuNFE{OiEQvF2= NV7PNoJMW0GQR1XS
HEC-1 NGj4c|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVTw[opLUUN3ME2xNE4zQDB2IN88US=> NUiwOFhVW0GQR1XS
HL-60 M1XC[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn7uTWM2OD1zMD62PFU{KM7:TR?= NX7aVnVDW0GQR1XS
A101D M3fkXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlTXTWM2OD1zMD64PVI{KM7:TR?= NIH3cXlUSU6JRWK=
A2058 MonXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVnJR|UxRTFyLkmyOFUh|ryP M4mzd3NCVkeHUh?=
KARPAS-45 NEfZeIFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVjDcXJGUUN3ME2xNU4xPjN3IN88US=> NXmzNW5IW0GQR1XS
697 M3L4dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXHJR|UxRTFzLkKxNFEh|ryP MoiyV2FPT0WU
NCI-N87 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NETl[m9KSzVyPUGxMlc4OzFizszN MnjaV2FPT0WU
DSH1 MlHCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoS4TWM2OD1zMT63PVU{KM7:TR?= NV3OcWlWW0GQR1XS
HLE NInr[HNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUHJR|UxRTFzLki4N|kh|ryP MmfqV2FPT0WU
NCI-H720 NGT0RmNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV7JR|UxRTF{Lk[4NFEh|ryP Mni3V2FPT0WU
EW-3 NYTZO5VkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml\HTWM2OD1zMj65N|A4KM7:TR?= M32wPXNCVkeHUh?=
AGS NVfITItyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIXDenZKSzVyPUGzMlA{PTFizszN M{C0UHNCVkeHUh?=
ES5 NYW5R|llT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1z1c2lEPTB;MUOuNFUyOiEQvF2= MXHTRW5ITVJ?
DB M4X6NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYPJR|UxRTF|LkOyOVYh|ryP NYT4flNsW0GQR1XS
A4-Fuk MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF\ZWFFKSzVyPUGzMlQyODJizszN NGDNfHFUSU6JRWK=
A427 M2XmZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFLlW29KSzVyPUGzMlQ6PzJizszN NYPEc4J4W0GQR1XS
MN-60 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEHYXYZKSzVyPUGzMlU5PDNizszN NF\ZPYhUSU6JRWK=
HCC2218 NV3sVplUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVvJR|UxRTF|LkW4OVYh|ryP MlvMV2FPT0WU
MV-4-11 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYe3eJZDUUN3ME2xN{45OTN5IN88US=> NInX[HdUSU6JRWK=
GI-1 NVHtSJV6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWHCUHZwUUN3ME2xOE4yOTh2IN88US=> NGnMSnhUSU6JRWK=
JVM-3 MojoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWG4[okxUUN3ME2xOE4zPjV4IN88US=> NY\yXIluW0GQR1XS
NCI-H2029 NVHzOlFQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUPJR|UxRTF2LkK3Nlch|ryP M3zIcnNCVkeHUh?=
TE-12 NXuyUW5WT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkC1TWM2OD1zND62NFQ3KM7:TR?= MYPTRW5ITVJ?
WM-115 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYHJR|UxRTF3LkW2PFMh|ryP MX\TRW5ITVJ?
BB65-RCC M1zBNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEe0OHlKSzVyPUG2MlAzPDFizszN NE\DbnVUSU6JRWK=
NCI-H1693 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX;XbmRTUUN3ME2xOk4{QDB{IN88US=> NVj6S5pQW0GQR1XS
KARPAS-299 Mk\JS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGLRU5dKSzVyPUG2MlYzODNizszN NXfQSXdsW0GQR1XS
UACC-257 NV;6WoRtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1u3WWlEPTB;MUeuNFU5OiEQvF2= NIDpSI5USU6JRWK=
RKO NXvYNVNnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUeybHNwUUN3ME2xO{43PDN|IN88US=> M1zw[HNCVkeHUh?=
HT-29 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXjJR|UxRTF5Lke4PFkh|ryP MUTTRW5ITVJ?
ES7 NU[yVHZpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHTy[mVKSzVyPUG4MlEyOjJizszN MoHnV2FPT0WU
DEL M2DL[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFLpd4FKSzVyPUG4MlMyPzJizszN NWrzb4RTW0GQR1XS
BT-549 M{L6Omdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4nHbGlEPTB;MUiuOFA6OiEQvF2= M3zhOHNCVkeHUh?=
NCI-H1755 NFTXV5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEHjbYJKSzVyPUG4MlU4OjNizszN M2HnfnNCVkeHUh?=
HCE-T M4nkT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYHGUHF{UUN3ME2xPE45OzRzIN88US=> NGTXfZNUSU6JRWK=
LU-139 NXmzfGF[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXf1VpR{UUN3ME2xPU4xPDV6IN88US=> NYrpS2JPW0GQR1XS
ECC10 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXjGenhKUUN3ME2xPU4zPDd3IN88US=> MVjTRW5ITVJ?
769-P M3nuRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVH0cHhkUUN3ME2xPU43OzN3IN88US=> M37LPXNCVkeHUh?=
BALL-1 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkfPTWM2OD1zOT62O|c2KM7:TR?= NG\HZmZUSU6JRWK=
LXF-289 M3XB[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYTBNXA6UUN3ME2xPU45QTd7IN88US=> Ml3tV2FPT0WU
TYK-nu MmG5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXjpUJkyUUN3ME2xPU46OzF3IN88US=> MV\TRW5ITVJ?
NCI-H630 NVT4d|VoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmfZTWM2OD1zOT65N|c5KM7:TR?= MV7TRW5ITVJ?
EW-18 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkGxTWM2OD1{MD6zPFAzKM7:TR?= NV7ZPIc{W0GQR1XS
KYSE-150 M4XMOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXXTflM6UUN3ME2yNE44ODR5IN88US=> Mo[1V2FPT0WU
LOXIMVI M4LZVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWDJR|UxRTJyLke1PFYh|ryP M2LHdnNCVkeHUh?=
HuP-T3 NFHSdVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlzYTWM2OD1{MT6wPFUzKM7:TR?= MVXTRW5ITVJ?
MFE-280 NHrwWpdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYfCdo5sUUN3ME2yNU42Pjd7IN88US=> MkDYV2FPT0WU
SK-OV-3 M1T4Wmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NULae4gzUUN3ME2yNU45PDB6IN88US=> NEGxV4JUSU6JRWK=
QIMR-WIL NHrIfGtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlvrTWM2OD1{Mj6wOFc5KM7:TR?= MU\TRW5ITVJ?
NCI-H69 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGPUOZdKSzVyPUKyMlQzQTlizszN NFuzeldUSU6JRWK=
TE-5 NIf4TZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEjkcZpKSzVyPUKyMlQ6PjVizszN NYfZOYRRW0GQR1XS
NCI-H1993 M2fKbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH3SVVhKSzVyPUKyMlQ6PzFizszN M1vaTXNCVkeHUh?=
NCI-H1092 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF7wdGJKSzVyPUKzMlI5PDNizszN Mnq4V2FPT0WU
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DBTRG-05MG MofjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEG4fWFKSzVyPUKzMlg1PzJizszN NVjuWWFWW0GQR1XS
Mo-T MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVvJR|UxRTJ|Lkmg{txO NVft[lRKW0GQR1XS
HD-MY-Z MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWC4NIxCUUN3ME2yOE4zOzZ{IN88US=> M4\jPHNCVkeHUh?=
NCI-H2342 NVvaSZltT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVvJR|UxRTJ2Lk[3Olch|ryP NFrq[5ZUSU6JRWK=
C32 M3HNU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mmi2TWM2OD1{ND65OVc3KM7:TR?= NFnnc3FUSU6JRWK=
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NCI-H358 NYjMWYVMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVXnNo9UUUN3ME2yOU4{QTR|IN88US=> NF:yZm1USU6JRWK=
CAL-85-1 Ml3CS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2\VPGlEPTB;MkWuOFU4PyEQvF2= M3rO[nNCVkeHUh?=
HT-1197 MmX0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NI\nVVVKSzVyPUK1MlU{OTlizszN MYXTRW5ITVJ?
A172 Ml3xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4myc2lEPTB;MkWuO|E{PiEQvF2= Mlm5V2FPT0WU
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SK-MEL-2 M4LqbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHjYRpJKSzVyPUK2MlA{OTJizszN MnPiV2FPT0WU
LU-65 NETBXWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX\JR|UxRTJ4LkC0OVIh|ryP Mo\ZV2FPT0WU
KMOE-2 NEjtWIFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1e4NmlEPTB;Mk[uNFkyPSEQvF2= NFX3OlBUSU6JRWK=
H-EMC-SS MmryS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoHhTWM2OD1{Nj60NVE1KM7:TR?= MUXTRW5ITVJ?
H4 Mm\NS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn\uTWM2OD1{Nj60NlQ{KM7:TR?= MX3TRW5ITVJ?
DU-4475 MmXRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYLJR|UxRTJ5LkG4O|Ih|ryP MnT4V2FPT0WU
HCT-116 M4DhZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MULJR|UxRTJ5LkSzOFkh|ryP MXHTRW5ITVJ?
MSTO-211H M2i2Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MorlTWM2OD1{Nz62NlU2KM7:TR?= MmHzV2FPT0WU
NCI-H292 MnLrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVP4SJBIUUN3ME2yO{46PjF5IN88US=> MknsV2FPT0WU
NCI-H446 MlfES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1\pRWlEPTB;MkiuNlExPSEQvF2= MVXTRW5ITVJ?
NCI-H2009 NVnPSZFsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXvmU4ZRUUN3ME2yPU4yPDNzIN88US=> NXmwb|ZNW0GQR1XS
MHH-ES-1 Mn:5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mo\WTWM2OD1{OT6zOlg2KM7:TR?= M17EbnNCVkeHUh?=
TI-73 MlvFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHLScHNKSzVyPUK5MlQxODFizszN NF\QZlhUSU6JRWK=
NCI-H2228 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mor6TWM2OD1{OT60OVgh|ryP MW\TRW5ITVJ?
MHH-PREB-1 MoD5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWPKSnoxUUN3ME2yPU42PTB3IN88US=> NF;qUW1USU6JRWK=
ChaGo-K-1 MoLjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVLJR|UxRTJ7Lk[wPVch|ryP M1XoOnNCVkeHUh?=
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NBsusSR NFLhblhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV7CepF[UUN3ME2yPU46QTB2IN88US=> MmLNV2FPT0WU
NCI-H1304 MofsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUfNWo5rUUN3ME2zNE42PzF4IN88US=> MmjVV2FPT0WU
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HCC1419 NF7GVZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXzmd2poUUN3ME2zNU4zPCEQvF2= Mn7GV2FPT0WU
KG-1 NWKycGhFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHLPfZRKSzVyPUOxMlc1OjlizszN NH\Je5ZUSU6JRWK=
A2780 NE\tSHhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnO0TWM2OD1|MT64N|U5KM7:TR?= M3jYRXNCVkeHUh?=
NCI-H28 NEPaVGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGLVWXRKSzVyPUOxMlk5PjFizszN NWm1RmtQW0GQR1XS
C2BBe1 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYjIb29VUUN3ME2zNk4zPjN2IN88US=> NFL5cVBUSU6JRWK=
VA-ES-BJ Ml2yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmD4TWM2OD1|Mj6zNUDPxE1? M4HSeXNCVkeHUh?=
SBC-5 M3fEfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV\JR|UxRTN{Lki1NVEh|ryP NFnTS2JUSU6JRWK=
OVCAR-4 NFvOelVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVfrXWpPUUN3ME2zN{41QDR6IN88US=> M3vXbnNCVkeHUh?=
COR-L88 M3H2V2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoraTWM2OD1|ND6wO|QyKM7:TR?= MXXTRW5ITVJ?
SW954 NY[zdG5JT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHfRPZVKSzVyPUO0MlA4PTJizszN NH7PW5VUSU6JRWK=
COLO-684 NXPTTlVoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{jTWWlEPTB;M{SuN|QxPCEQvF2= M3q4XnNCVkeHUh?=
HCC70 NVftPZBlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnXOTWM2OD1|ND65OVE1KM7:TR?= MlvLV2FPT0WU
NCI-H1770 NYTY[3dJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M325WWlEPTB;M{SuPVYyKM7:TR?= M1PiNnNCVkeHUh?=
NCI-H1666 NUP1Toc6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn3oTWM2OD1|NT64NlU{KM7:TR?= Mm[4V2FPT0WU
YH-13 M2fGd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXjXPJl3UUN3ME2zOU46OiEQvF2= M3fKb3NCVkeHUh?=
DJM-1 MkLqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3vyXmlEPTB;M{[uPFA1QSEQvF2= Mn7iV2FPT0WU
KNS-62 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1vIR2lEPTB;M{[uPVQ{QCEQvF2= MV3TRW5ITVJ?
SK-MEL-30 M1XqO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3\iUWlEPTB;M{euPFc{PyEQvF2= MljNV2FPT0WU
SJRH30 NYTJOYNOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnXvTWM2OD1|OD63N|QyKM7:TR?= MnGzV2FPT0WU
GP5d M1u0U2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWnxTmlsUUN3ME2zPE45PjV|IN88US=> M3S0fXNCVkeHUh?=
SW1116 NYi3VZVtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmfWTWM2OD1|OT6yPFA2KM7:TR?= NV34SXhQW0GQR1XS
COLO-800 MnPES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1HGUWlEPTB;M{muN|Y{QCEQvF2= MkTmV2FPT0WU
RD M{LJNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXPJe2ZwUUN3ME2zPU42OjV6IN88US=> MV7TRW5ITVJ?
NCI-SNU-5 NXzUWYZWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXTJR|UxRTN7Lk[5NVYh|ryP MlLtV2FPT0WU
HuO-3N1 NITaVGtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnrTTWM2OD12MD6xNFgh|ryP NX\sXXAzW0GQR1XS
SK-UT-1 MkDSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXHud5J5UUN3ME20NE42Pjd2IN88US=> NF32dWxUSU6JRWK=
SK-MEL-3 NWHUenF2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXrJR|UxRTRyLkW5N|Ih|ryP NXrhR4lNW0GQR1XS
SK-MEL-28 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1HPZWlEPTB;NECuOlQ{PSEQvF2= MUHTRW5ITVJ?
SCC-4 M1jKRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MofPTWM2OD12MT6yNVM4KM7:TR?= NHLVU25USU6JRWK=
no-11 NFrlT21Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYPJR|UxRTRzLkezOVQh|ryP NUO2bYk{W0GQR1XS
HT-144 MoWwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUXJR|UxRTR{LkC1Olch|ryP MYjTRW5ITVJ?
MFM-223 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M33QWGlEPTB;NEKuOFAzKM7:TR?= MknIV2FPT0WU
ONS-76 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NI\Y[WJKSzVyPUSyMlgxOThizszN NWDTU4l4W0GQR1XS
ES8 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVrJR|UxRTR|LkO2PVgh|ryP Mn;EV2FPT0WU
T-24 NUHIPHNST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXvJR|UxRTR|LkSzOlkh|ryP NVPxTIttW0GQR1XS
GAMG MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXHhWYhmUUN3ME20N{41PTF5IN88US=> MX7TRW5ITVJ?
LU-135 Mk\6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV24c2txUUN3ME20OE4xQTJ|IN88US=> NIXFNHFUSU6JRWK=
HCC1187 NVTFd|NjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmnCTWM2OD12ND64NlYzKM7:TR?= NWPvZotCW0GQR1XS
TE-1 NV\6e29qT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4KwNWlEPTB;NEWuNVY2PCEQvF2= NYXI[JNyW0GQR1XS
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D-392MG Mmf0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVTuepVoUUN3ME20OU46OjV4IN88US=> NWPhXIQzW0GQR1XS
KALS-1 M1PNd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEXBZpRKSzVyPUS2MlczPTdizszN M2e2OnNCVkeHUh?=
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HSC-3 MofDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGjaNmVKSzVyPUS3MlM3ODhizszN MoSwV2FPT0WU
KM-H2 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYjRU|ZCUUN3ME20O{43ODB5IN88US=> MVjTRW5ITVJ?
LoVo M3i4UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NILDc5dKSzVyPUS4MlExODJizszN MoLwV2FPT0WU
NCI-H510A NYDRZVR1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXW3SHJpUUN3ME20PE4yQDdzIN88US=> NFm5fHZUSU6JRWK=
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HCC2998 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXuwR451UUN3ME20PE43OjN4IN88US=> MYnTRW5ITVJ?
J82 M1XUUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX\JR|UxRTR6LkeyOFIh|ryP Mnf6V2FPT0WU
ML-2 NYD5fm9ST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEDxPI1KSzVyPUS5MlQ3ODVizszN NU\4So5QW0GQR1XS
NCI-H2030 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWjIR2NZUUN3ME20PU44OTF5IN88US=> MV\TRW5ITVJ?
NCI-H1792 NGTINIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYPJR|UxRTR7Lki1NVgh|ryP M4\ZWXNCVkeHUh?=

... 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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    Degrasyn (WP1130)は一種の選択性的なdeubiquitinase(DUB: USP5、UCH-L1、USP9x、USP14と UCH37)阻害剤ですが、Bcr/Ablを抑制する作用があります。Degrasyn (WP1130)も一種のJAK2トランスデューサ(20Sプロテアソームに影響を与えない)と転写活性剤(STAT)です。

    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)は一種のBcr-Abl阻害剤で、Abl1(WT)とAbl1(T315I)に作用する時のIC50値が0.8 nMと4 nMです。DCC-2036 (Rebastinib)はSRC、LYN、FGR、HCK、KDR、FLT3とTie-2も抑制しますが、c-Kitに低い抑制活性を表します。臨床1期。

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

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Tags: Nilotinib (AMN-107)を買う | Nilotinib (AMN-107)供給者 | Nilotinib (AMN-107)を購入する | Nilotinib (AMN-107)費用 | Nilotinib (AMN-107)生産者 | オーダーNilotinib (AMN-107) | Nilotinib (AMN-107)代理店
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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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