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 M3nzZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml7TTWM2OD1yLkCwNFE1PCEQvF2= NX3qTnNTW0GQR1XS
KU812 NGe1O2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{\Pb2lEPTB;MD6wNFI1QCEQvF2= NHLWTnBUSU6JRWK=
EM-2 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFv2OHhKSzVyPUCuNFA1OSEQvF2= NH;MdoVUSU6JRWK=
LAMA-84 M3\iR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXPJR|UxRTBwMEC0PUDPxE1? M1ziRXNCVkeHUh?=
MEG-01 M{\Db2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUjJR|UxRTBwMEC4Nlgh|ryP MYrTRW5ITVJ?
BV-173 NFf3XY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGnVVotKSzVyPUCuNFExQDlizszN MnzvV2FPT0WU
KASUMI-1 M3X6fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2nJVWlEPTB;MD6wNlQyOyEQvF2= NHzpRZdUSU6JRWK=
NB7 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2G0e2lEPTB;MD6xN|Q{QSEQvF2= MVTTRW5ITVJ?
BHT-101 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWizTVdGUUN3ME2wMlY1OjZ|IN88US=> MnjkV2FPT0WU
CGTH-W-1 NILye3FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4LySmlEPTB;MD62OFg4KM7:TR?= MkGwV2FPT0WU
HMV-II MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4HnVGlEPTB;MD63OFg4PCEQvF2= NXW1XFNTW0GQR1XS
NKM-1 NUPEPXRwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIT5OoVKSzVyPUCuPVAyPSEQvF2= NIK5SW9USU6JRWK=
LB2241-RCC M33teWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHnjXWpKSzVyPUGuNFIzOjhizszN MmjMV2FPT0WU
NCI-H1703 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXjJR|UxRTFwMUi4O{DPxE1? NH\OfHhUSU6JRWK=
BE-13 NGnU[lNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIX6bZNKSzVyPUGuNlc1OTZizszN NF3GeHFUSU6JRWK=
ACN NXfPWGgzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmHCTWM2OD1zLkW1NFc4KM7:TR?= NWfiNotPW0GQR1XS
A204 NH;6cIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVW0PJlOUUN3ME2xMlU4OjB3IN88US=> M4mxe3NCVkeHUh?=
HOP-62 NFTrVIdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVjMc|BVUUN3ME2xMlgzODd5IN88US=> NXrBXIJnW0GQR1XS
H9 NIT1V4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFmzPHlKSzVyPUKuO|M4QTNizszN MV3TRW5ITVJ?
HCC1806 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUOwRlV7UUN3ME2yMlc1OzJ5IN88US=> NFqxXYxUSU6JRWK=
NOS-1 NVL2bIdIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MljPTWM2OD1{Lki3NVAzKM7:TR?= MnjuV2FPT0WU
RS4-11 NXuyO|NyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVHRXXRDUUN3ME2yMlkxPjJ|IN88US=> M{TM[XNCVkeHUh?=
JAR NEn3So9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4[5cGlEPTB;Mj65NlA5PCEQvF2= Mkf5V2FPT0WU
T98G Mki0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2S1T2lEPTB;Mz6wNVMyOyEQvF2= M2rYfnNCVkeHUh?=
NCI-SNU-1 NUXtWnRIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWTJR|UxRTNwNECwPVIh|ryP Mn\yV2FPT0WU
SK-MEL-1 NXjaVodPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFj5TFVKSzVyPUOuOFMxOjlizszN MoTaV2FPT0WU
L-363 NX3sNYg4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3jsb2lEPTB;Mz62NVExPyEQvF2= MYnTRW5ITVJ?
SW982 NEHI[YVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnvUTWM2OD1|Lk[0NVY6KM7:TR?= Ml7PV2FPT0WU
HT-1080 NVL5OJVmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV\JR|UxRTNwOUG3O|Uh|ryP MVfTRW5ITVJ?
G-402 MknmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml\LTWM2OD12LkOxNlA{KM7:TR?= MXvTRW5ITVJ?
HOS M1jvU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{DLbGlEPTB;ND64NFI5OiEQvF2= M4fVXnNCVkeHUh?=
SK-NEP-1 M4LTV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX;JR|UxRTRwOEOxPVEh|ryP NFTqe3dUSU6JRWK=
HAL-01 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlzNTWM2OD12Lki4NlQzKM7:TR?= NFzZfVdUSU6JRWK=
SBC-1 M{\MV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV;ld2FuUUN3ME20MlkxQTB5IN88US=> M{SzV3NCVkeHUh?=
CTV-1 M3;CNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYnQRWRwUUN3ME21MlQ5QTN6IN88US=> NHjEZoZUSU6JRWK=
LCLC-103H M{H2N2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIGwPVBKSzVyPUWuO|c1PzFizszN NULMcow1W0GQR1XS
RVH-421 NVnHb5VHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn7NTWM2OD13Lke3OVM3KM7:TR?= MX3TRW5ITVJ?
K-562 M{DPcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoTDTWM2OD13LkmwN|Yh|ryP M{DwdnNCVkeHUh?=
CAL-33 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mkj5TWM2OD14LkOxN|U6KM7:TR?= MmnEV2FPT0WU
MDA-MB-361 NX\LT|U3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEfSb2NKSzVyPU[uN|M3QTlizszN MkDJV2FPT0WU
IGROV-1 M37UZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1\1O2lEPTB;Nj60O|E6OSEQvF2= M3H5ZXNCVkeHUh?=
NY NITESGdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVfJR|UxRTZwNUO1PVkh|ryP M4X5cHNCVkeHUh?=
Ramos-2G6-4C10 NGe1W2ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2LKeGlEPTB;Nj62Olk{OSEQvF2= MUDTRW5ITVJ?
HuO9 NUX3[5cyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXW4dotHUUN3ME22Mlc{QTZ2IN88US=> NYS4XJFuW0GQR1XS
MS-1 NVrQeGVsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVLYdIVsUUN3ME23MlEyQTV|IN88US=> NWq1b3F4W0GQR1XS
RPMI-8226 M33PRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWXncVM6UUN3ME23MlI5Ojh5IN88US=> NUPNV|h2W0GQR1XS
HDLM-2 NWjkTVE6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVjJR|UxRTdwNECxOFkh|ryP Mk\KV2FPT0WU
D-566MG MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHXsTo1KSzVyPUeuOFcyPTVizszN MV;TRW5ITVJ?
SK-MEL-24 NGLGTZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2[wUWlEPTB;Nz62N|M6OiEQvF2= MV7TRW5ITVJ?
COLO-679 NXvXUFEyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFrCd5FKSzVyPUeuPVg3PzFizszN MVzTRW5ITVJ?
EW-13 NFjvNGhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFnTWVRKSzVyPUiuN|IxPTRizszN M{XlVHNCVkeHUh?=
A388 NWDZdGFWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NITofZVKSzVyPUiuN|g1QDFizszN NVS0cm81W0GQR1XS
UM-UC-3 NXS2S|RjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoTITWM2OD16LkSzPVU3KM7:TR?= M3LtPXNCVkeHUh?=
NUGC-3 MkPOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{nMfGlEPTB;OD61N|U5OiEQvF2= M{DtNnNCVkeHUh?=
COLO-668 NXrMVpZkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVzDUFQ3UUN3ME24MlU6PDlzIN88US=> NHvtUG1USU6JRWK=
MOLT-4 NYTjfZpjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{HSOGlEPTB;OD62NlM2OyEQvF2= MkL4V2FPT0WU
D-423MG MnPVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYXNO2dyUUN3ME24Mlg{PzV4IN88US=> M{jXWHNCVkeHUh?=
CTB-1 MmPiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVnJR|UxRThwOEexNlgh|ryP MV\TRW5ITVJ?
BCPAP NFP2SHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEnt[4dKSzVyPUmuNFI2PjJizszN NVL5PZNpW0GQR1XS
GCT MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXzJR|UxRTlwMEm4N|Eh|ryP MkjrV2FPT0WU
ACHN NHjl[nFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH65So9KSzVyPUmuNlM3OzJizszN NETFdG9USU6JRWK=
KYSE-520 M33IXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlvxTWM2OD17LkOzOFgzKM7:TR?= NHvMU29USU6JRWK=
LB771-HNC NYC0cWxOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M37OW2lEPTB;OT63OlQ6PyEQvF2= NF3EcnlUSU6JRWK=
MLMA NUnUcWo4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUjJR|UxRTFyLkCxN|Ih|ryP NUPwcHhxW0GQR1XS
HEC-1 NVf2TGZiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NViyO2F{UUN3ME2xNE4zQDB2IN88US=> MkjwV2FPT0WU
HL-60 NIrCfYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnPrTWM2OD1zMD62PFU{KM7:TR?= MX3TRW5ITVJ?
A101D NEO2OWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkiwTWM2OD1zMD64PVI{KM7:TR?= Mn;PV2FPT0WU
A2058 NU[yWHNWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFPxdoZKSzVyPUGwMlkzPDVizszN MYDTRW5ITVJ?
KARPAS-45 Mn64S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1\ZS2lEPTB;MUGuNFY{PSEQvF2= NFPmSm5USU6JRWK=
697 MmfkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MorLTWM2OD1zMT6yNVAyKM7:TR?= MUHTRW5ITVJ?
NCI-N87 NFjGWGtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnjjTWM2OD1zMT63O|MyKM7:TR?= NF7hZ5lUSU6JRWK=
DSH1 NHfBSZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWHzXGUyUUN3ME2xNU44QTV|IN88US=> NV6zNZFQW0GQR1XS
HLE M{ixe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWPJR|UxRTFzLki4N|kh|ryP MkToV2FPT0WU
NCI-H720 M2fx[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWjJR|UxRTF{Lk[4NFEh|ryP NWHBbJVJW0GQR1XS
EW-3 Ml;MS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml7DTWM2OD1zMj65N|A4KM7:TR?= M1zBXHNCVkeHUh?=
AGS NF\J[ItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWPHNo1kUUN3ME2xN{4xOzVzIN88US=> MW\TRW5ITVJ?
ES5 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MojOTWM2OD1zMz6wOVEzKM7:TR?= MULTRW5ITVJ?
DB M1G3S2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1jrdmlEPTB;MUOuN|I2PiEQvF2= NV\HfXVmW0GQR1XS
A4-Fuk M4jG[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEj5N4NKSzVyPUGzMlQyODJizszN MmXwV2FPT0WU
A427 NUH6TlFXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVfJR|UxRTF|LkS5O|Ih|ryP NUG3[HBiW0GQR1XS
MN-60 NVuzT3JtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1K1emlEPTB;MUOuOVg1OyEQvF2= NYH1OI9pW0GQR1XS
HCC2218 NX7wSIpKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn\XTWM2OD1zMz61PFU3KM7:TR?= NYOzXld6W0GQR1XS
MV-4-11 MlvHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnjlTWM2OD1zMz64NVM4KM7:TR?= NIHO[WNUSU6JRWK=
GI-1 Ml3uS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M13BUWlEPTB;MUSuNVE5PCEQvF2= M4[4TXNCVkeHUh?=
JVM-3 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXvWfJR1UUN3ME2xOE4zPjV4IN88US=> M4TGfXNCVkeHUh?=
NCI-H2029 M2\jNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHLBUnBKSzVyPUG0MlI4OjdizszN MVXTRW5ITVJ?
TE-12 MoDiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3\GTGlEPTB;MUSuOlA1PiEQvF2= NGjmfnVUSU6JRWK=
WM-115 MofrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYG3WmJTUUN3ME2xOU42Pjh|IN88US=> NEjSNXhUSU6JRWK=
BB65-RCC NV7NVFVTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoC1TWM2OD1zNj6wNlQyKM7:TR?= M3zDTXNCVkeHUh?=
NCI-H1693 M3fTSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUL1bVlwUUN3ME2xOk4{QDB{IN88US=> MnfLV2FPT0WU
KARPAS-299 M4S1WWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVn0TYxvUUN3ME2xOk43OjB|IN88US=> NGfOUndUSU6JRWK=
UACC-257 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NInlPJdKSzVyPUG3MlA2QDJizszN NH7POFVUSU6JRWK=
RKO NIrZdYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1HWNmlEPTB;MUeuOlQ{OyEQvF2= NIjQc5dUSU6JRWK=
HT-29 MnrwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV\DV5FUUUN3ME2xO{44QDh7IN88US=> NET1elNUSU6JRWK=
ES7 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXTJR|UxRTF6LkGxNlIh|ryP M17LW3NCVkeHUh?=
DEL NHOwTm1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIXJTphKSzVyPUG4MlMyPzJizszN MYjTRW5ITVJ?
BT-549 M3;wbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2nKPWlEPTB;MUiuOFA6OiEQvF2= MlXyV2FPT0WU
NCI-H1755 MonVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXXJR|UxRTF6LkW3NlMh|ryP MYnTRW5ITVJ?
HCE-T MlXPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHj0UnRKSzVyPUG4Mlg{PDFizszN MVzTRW5ITVJ?
LU-139 NUHr[o06T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlfQTWM2OD1zOT6wOFU5KM7:TR?= NWrSXYdvW0GQR1XS
ECC10 NV7ERoVDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX3JR|UxRTF7LkK0O|Uh|ryP NV3UZoxjW0GQR1XS
769-P NVTyXYptT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXjwOm1qUUN3ME2xPU43OzN3IN88US=> MljFV2FPT0WU
BALL-1 NFz2SHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF:3VndKSzVyPUG5MlY4PzVizszN MmrmV2FPT0WU
LXF-289 NIDrbpBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkXZTWM2OD1zOT64PVc6KM7:TR?= NE\SR3FUSU6JRWK=
TYK-nu M2LtWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFWxZ2NKSzVyPUG5Mlk{OTVizszN NHzzPG1USU6JRWK=
NCI-H630 NUDaVZd2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIHlUmhKSzVyPUG5Mlk{PzhizszN NVG3cFR{W0GQR1XS
EW-18 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUHJR|UxRTJyLkO4NFIh|ryP NYO4Rm5qW0GQR1XS
KYSE-150 MmDBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFmzNmJKSzVyPUKwMlcxPDdizszN NIrDfmFUSU6JRWK=
LOXIMVI NGrUO2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFi5c|NKSzVyPUKwMlc2QDZizszN MUHTRW5ITVJ?
HuP-T3 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGHK[lNKSzVyPUKxMlA5PTJizszN MXjTRW5ITVJ?
MFE-280 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NETWd5FKSzVyPUKxMlU3PzlizszN NUHhUIlpW0GQR1XS
SK-OV-3 M{C4eGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkSzTWM2OD1{MT64OFA5KM7:TR?= M1:1VXNCVkeHUh?=
QIMR-WIL MoLiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVywT3hSUUN3ME2yNk4xPDd6IN88US=> M1zaVXNCVkeHUh?=
NCI-H69 NUHZV2VFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX\JR|UxRTJ{LkSyPVkh|ryP NILX[ndUSU6JRWK=
TE-5 NF;iNZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWfJR|UxRTJ{LkS5OlUh|ryP MmfpV2FPT0WU
NCI-H1993 NE\RTY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIDFV25KSzVyPUKyMlQ6PzFizszN MWfTRW5ITVJ?
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HSC-3 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWXJR|UxRTR5LkO2NFgh|ryP MX3TRW5ITVJ?
KM-H2 MmLxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVfJR|UxRTR5Lk[wNFch|ryP M3;lRXNCVkeHUh?=
LoVo MluyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1TLTmlEPTB;NEiuNVAxOiEQvF2= NWX4NnZYW0GQR1XS
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J82 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkC3TWM2OD12OD63NlQzKM7:TR?= M2TMZ3NCVkeHUh?=
ML-2 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4LFU2lEPTB;NEmuOFYxPSEQvF2= MnL1V2FPT0WU
NCI-H2030 NHqwcnBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXrUOGFbUUN3ME20PU44OTF5IN88US=> NEXtT3FUSU6JRWK=
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... 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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