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 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1HkU2lEPTB;MD6wNFAyPDRizszN NIC5d5FUSU6JRWK=
KU812 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkfGTWM2OD1yLkCwNlQ5KM7:TR?= NFSyeFBUSU6JRWK=
EM-2 M{[wS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mmf3TWM2OD1yLkCwOFEh|ryP M{GxR3NCVkeHUh?=
LAMA-84 Mk\RS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXX3PVExUUN3ME2wMlAxPDlizszN MkfaV2FPT0WU
MEG-01 MlH6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4nTSmlEPTB;MD6wNFgzQCEQvF2= NULaPIFUW0GQR1XS
BV-173 MoLqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX[5cGFEUUN3ME2wMlAyODh7IN88US=> M3X0WHNCVkeHUh?=
KASUMI-1 NFO4U|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mnj1TWM2OD1yLkCyOFE{KM7:TR?= MlzwV2FPT0WU
NB7 M2[3[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NW\qcVRKUUN3ME2wMlE{PDN7IN88US=> NX;6N2JuW0GQR1XS
BHT-101 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3u4SWlEPTB;MD62OFI3OyEQvF2= M161[3NCVkeHUh?=
CGTH-W-1 M3iwd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX7JR|UxRTBwNkS4O{DPxE1? NXH2ZYg2W0GQR1XS
HMV-II NWjzNVZjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX3hO3ljUUN3ME2wMlc1QDd2IN88US=> NH35PYdUSU6JRWK=
NKM-1 NUDvUmtGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWTJR|UxRTBwOUCxOUDPxE1? MXzTRW5ITVJ?
LB2241-RCC NIS1TFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVPJR|UxRTFwMEKyNlgh|ryP NEXub5VUSU6JRWK=
NCI-H1703 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlL2TWM2OD1zLkG4PFch|ryP NHX2S3pUSU6JRWK=
BE-13 Moi0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4XFbGlEPTB;MT6yO|QyPiEQvF2= MkXoV2FPT0WU
ACN NEHFNmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYnJR|UxRTFwNUWwO|ch|ryP NWi0Z4pjW0GQR1XS
A204 MkPuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NILxVmtKSzVyPUGuOVczODVizszN MYTTRW5ITVJ?
HOP-62 NFvtZ|hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV;JR|UxRTFwOEKwO|ch|ryP NFzFZphUSU6JRWK=
H9 MkW5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV\JR|UxRTJwN{O3PVMh|ryP NIn3TXVUSU6JRWK=
HCC1806 NHnvUFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXnJR|UxRTJwN{SzNlch|ryP M2Dt[XNCVkeHUh?=
NOS-1 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVu0XpNWUUN3ME2yMlg4OTB{IN88US=> NGHvfoVUSU6JRWK=
RS4-11 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFi0PWFKSzVyPUKuPVA3OjNizszN M2iyOXNCVkeHUh?=
JAR NEPrU5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4HnfmlEPTB;Mj65NlA5PCEQvF2= NUToXGRmW0GQR1XS
T98G M3vIXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIqze4FKSzVyPUOuNFE{OTNizszN MYjTRW5ITVJ?
NCI-SNU-1 MlXkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXTJR|UxRTNwNECwPVIh|ryP MmnXV2FPT0WU
SK-MEL-1 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{TGZ2lEPTB;Mz60N|AzQSEQvF2= MYDTRW5ITVJ?
L-363 NWjBfm1wT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUDJR|UxRTNwNkGxNFch|ryP NFnzfmNUSU6JRWK=
SW982 M2PMeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2P1VmlEPTB;Mz62OFE3QSEQvF2= NUfhWVBEW0GQR1XS
HT-1080 NHO4fGRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVy0eZdwUUN3ME2zMlkyPzd3IN88US=> Ml7uV2FPT0WU
G-402 MlK3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mlq5TWM2OD12LkOxNlA{KM7:TR?= NXX3SnNTW0GQR1XS
HOS Ml7ZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoL6TWM2OD12LkiwNlgzKM7:TR?= NEOwOmJUSU6JRWK=
SK-NEP-1 NUGyRlhLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MY\JR|UxRTRwOEOxPVEh|ryP NVjQNJMxW0GQR1XS
HAL-01 M{DUPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHLNN5dKSzVyPUSuPFgzPDJizszN MVzTRW5ITVJ?
SBC-1 NGDBfYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlLHTWM2OD12LkmwPVA4KM7:TR?= MVfTRW5ITVJ?
CTV-1 M1\3bGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnLmTWM2OD13LkS4PVM5KM7:TR?= M1\YSHNCVkeHUh?=
LCLC-103H MlrIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2rGfmlEPTB;NT63O|Q4OSEQvF2= MnPFV2FPT0WU
RVH-421 NXPGd3JiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX:2eW95UUN3ME21Mlc4PTN4IN88US=> NVPGXGRiW0GQR1XS
K-562 NYDXPZp4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUTJR|UxRTVwOUCzOkDPxE1? MWnTRW5ITVJ?
CAL-33 NG\ac21Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4jpPGlEPTB;Nj6zNVM2QSEQvF2= NHKz[5NUSU6JRWK=
MDA-MB-361 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYTvS2tbUUN3ME22MlM{Pjl7IN88US=> NH[1TG1USU6JRWK=
IGROV-1 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIK2XHVKSzVyPU[uOFcyQTFizszN NWLZNZNFW0GQR1XS
NY MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml;jTWM2OD14LkWzOVk6KM7:TR?= NIH1d|FUSU6JRWK=
Ramos-2G6-4C10 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGDUPGpKSzVyPU[uOlY6OzFizszN NVfK[ZMxW0GQR1XS
HuO9 Mm[zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGryXpNKSzVyPU[uO|M6PjRizszN MV3TRW5ITVJ?
MS-1 MnnES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NW\vRoRPUUN3ME23MlEyQTV|IN88US=> NITFNlJUSU6JRWK=
RPMI-8226 M2q4U2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2PWO2lEPTB;Nz6yPFI5PyEQvF2= MWrTRW5ITVJ?
HDLM-2 M2rOVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF;PV4FKSzVyPUeuOFAyPDlizszN MonzV2FPT0WU
D-566MG M33YXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF7oO29KSzVyPUeuOFcyPTVizszN NWm5OHplW0GQR1XS
SK-MEL-24 M3naeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4HFdGlEPTB;Nz62N|M6OiEQvF2= NFnsT|VUSU6JRWK=
COLO-679 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmPZTWM2OD15Lkm4OlcyKM7:TR?= M3T4fHNCVkeHUh?=
EW-13 NUO4OoN1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3fCRWlEPTB;OD6zNlA2PCEQvF2= NHP1fpNUSU6JRWK=
A388 Ml22S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1nTOGlEPTB;OD6zPFQ5OSEQvF2= M4LpNHNCVkeHUh?=
UM-UC-3 MmnuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2Th[GlEPTB;OD60N|k2PiEQvF2= MV\TRW5ITVJ?
NUGC-3 NGXrcWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2LmNGlEPTB;OD61N|U5OiEQvF2= NHe2XWJUSU6JRWK=
COLO-668 MlTsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MY\JR|UxRThwNUm0PVEh|ryP M1TBfXNCVkeHUh?=
MOLT-4 NHfMfnVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmL6TWM2OD16Lk[yN|U{KM7:TR?= MkPxV2FPT0WU
D-423MG MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIfrVHJKSzVyPUiuPFM4PTZizszN MWPTRW5ITVJ?
CTB-1 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoDDTWM2OD16Lki3NVI5KM7:TR?= MlrBV2FPT0WU
BCPAP MnHHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4fqTmlEPTB;OT6wNlU3OiEQvF2= MlPqV2FPT0WU
GCT NXvkZldkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFnwNJVKSzVyPUmuNFk5OzFizszN MYLTRW5ITVJ?
ACHN NWLWPIdtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4LOdGlEPTB;OT6yN|Y{OiEQvF2= NVnHV4g{W0GQR1XS
KYSE-520 NVqwRY1TT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1TKdGlEPTB;OT6zN|Q5OiEQvF2= MVvTRW5ITVJ?
LB771-HNC NYDrbmRIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYTJR|UxRTlwN{[0PVch|ryP NXnvUlJTW0GQR1XS
MLMA Mmn2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkPXTWM2OD1zMD6wNVMzKM7:TR?= NHTJOIFUSU6JRWK=
HEC-1 MofDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NILLc3dKSzVyPUGwMlI5ODRizszN MYnTRW5ITVJ?
HL-60 M3PBWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWO3NllmUUN3ME2xNE43QDV|IN88US=> M2G4U3NCVkeHUh?=
A101D MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoHQTWM2OD1zMD64PVI{KM7:TR?= MlfPV2FPT0WU
A2058 NUXneFR{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEHSU4JKSzVyPUGwMlkzPDVizszN NXzyW|Y2W0GQR1XS
KARPAS-45 NGTBcFNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWrJR|UxRTFzLkC2N|Uh|ryP NYnxSnhKW0GQR1XS
697 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVHpW5FWUUN3ME2xNU4zOTBzIN88US=> MX3TRW5ITVJ?
NCI-N87 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXXJR|UxRTFzLke3N|Eh|ryP NGiy[2RUSU6JRWK=
DSH1 NGfFd|hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmHvTWM2OD1zMT63PVU{KM7:TR?= MnvDV2FPT0WU
HLE MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWrjWVBlUUN3ME2xNU45QDN7IN88US=> M1PRcHNCVkeHUh?=
NCI-H720 NVPHUIx4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1ThT2lEPTB;MUKuOlgxOSEQvF2= M2fQSnNCVkeHUh?=
EW-3 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYPJR|UxRTF{LkmzNFch|ryP NGLMTZBUSU6JRWK=
AGS NGnLTmxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2fHdGlEPTB;MUOuNFM2OSEQvF2= MUDTRW5ITVJ?
ES5 MmjsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUL4bGhYUUN3ME2xN{4xPTF{IN88US=> NYi5bZVjW0GQR1XS
DB MmHZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlL5TWM2OD1zMz6zNlU3KM7:TR?= NYS0VVZ7W0GQR1XS
A4-Fuk MnmzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3jyOGlEPTB;MUOuOFExOiEQvF2= NWnkSVF4W0GQR1XS
A427 M{TKVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHzTbJNKSzVyPUGzMlQ6PzJizszN NY\1fGFZW0GQR1XS
MN-60 NVOxU3VmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2\w[2lEPTB;MUOuOVg1OyEQvF2= M1T5RXNCVkeHUh?=
HCC2218 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH;xT|FKSzVyPUGzMlU5PTZizszN MXTTRW5ITVJ?
MV-4-11 MnLJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGKzUZpKSzVyPUGzMlgyOzdizszN M1HJbnNCVkeHUh?=
GI-1 M2X0SWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGr0fllKSzVyPUG0MlEyQDRizszN M3nwO3NCVkeHUh?=
JVM-3 NUCyWmIyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYfJR|UxRTF2LkK2OVYh|ryP M1LsbHNCVkeHUh?=
NCI-H2029 NFXlU21Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mkn3TWM2OD1zND6yO|I4KM7:TR?= MUXTRW5ITVJ?
TE-12 M3zpSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXq0RXJMUUN3ME2xOE43ODR4IN88US=> M13kSnNCVkeHUh?=
WM-115 NWTLcGNXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYDvb4pVUUN3ME2xOU42Pjh|IN88US=> M3;jfnNCVkeHUh?=
BB65-RCC MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{P4XmlEPTB;MU[uNFI1OSEQvF2= NGD0WWZUSU6JRWK=
NCI-H1693 MmXQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoHaTWM2OD1zNj6zPFAzKM7:TR?= M1fycXNCVkeHUh?=
KARPAS-299 NEDiO2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUHQVFdlUUN3ME2xOk43OjB|IN88US=> MnvQV2FPT0WU
UACC-257 NVf6N4NTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYTKdGk1UUN3ME2xO{4xPTh{IN88US=> MVPTRW5ITVJ?
RKO MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUnJR|UxRTF5Lk[0N|Mh|ryP MXfTRW5ITVJ?
HT-29 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2XKUmlEPTB;MUeuO|g5QSEQvF2= NGi3XWdUSU6JRWK=
ES7 NXPDR5NQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVfJR|UxRTF6LkGxNlIh|ryP MY\TRW5ITVJ?
DEL M3HjXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWr1enZCUUN3ME2xPE4{OTd{IN88US=> NXXaXms6W0GQR1XS
BT-549 NYeyfos{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mln4TWM2OD1zOD60NFkzKM7:TR?= MkHpV2FPT0WU
NCI-H1755 NHvON4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXnVWVJrUUN3ME2xPE42PzJ|IN88US=> NXrNW3JDW0GQR1XS
HCE-T NXTNUphsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWXkOpljUUN3ME2xPE45OzRzIN88US=> NEPEW4xUSU6JRWK=
LU-139 Mm\6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml3pTWM2OD1zOT6wOFU5KM7:TR?= NUL5T|ZEW0GQR1XS
ECC10 M1rVNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NICxPVhKSzVyPUG5MlI1PzVizszN Mn7iV2FPT0WU
769-P Mm\HS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWrJR|UxRTF7Lk[zN|Uh|ryP M2fOT3NCVkeHUh?=
BALL-1 NF3PNWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX[xVmY5UUN3ME2xPU43Pzd3IN88US=> NVXqTZBlW0GQR1XS
LXF-289 M4j0PWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MorWTWM2OD1zOT64PVc6KM7:TR?= MYLTRW5ITVJ?
TYK-nu NF3GVI5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVTBSHlbUUN3ME2xPU46OzF3IN88US=> NEX6SGVUSU6JRWK=
NCI-H630 M4G3UWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFjhRVJKSzVyPUG5Mlk{PzhizszN NV;hWIZ6W0GQR1XS
EW-18 M1rV[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYryUG1xUUN3ME2yNE4{QDB{IN88US=> NX;3c4JwW0GQR1XS
KYSE-150 NHO5O4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWG1fWxbUUN3ME2yNE44ODR5IN88US=> MVvTRW5ITVJ?
LOXIMVI NYThb4toT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{DRVWlEPTB;MkCuO|U5PiEQvF2= NHTJOVBUSU6JRWK=
HuP-T3 MmTES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUXJR|UxRTJzLkC4OVIh|ryP NESyOJFUSU6JRWK=
MFE-280 NVTxdHFPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV35TXR{UUN3ME2yNU42Pjd7IN88US=> MYfTRW5ITVJ?
SK-OV-3 MlfzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkjFTWM2OD1{MT64OFA5KM7:TR?= NXvETYNRW0GQR1XS
QIMR-WIL M2LJb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWrJR|UxRTJ{LkC0O|gh|ryP NILWbnVUSU6JRWK=
NCI-H69 NFHMOnVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFjrUIdKSzVyPUKyMlQzQTlizszN MX7TRW5ITVJ?
TE-5 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NE[1T21KSzVyPUKyMlQ6PjVizszN M4PFfHNCVkeHUh?=
NCI-H1993 NH;PW4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MorwTWM2OD1{Mj60PVcyKM7:TR?= Mln3V2FPT0WU
NCI-H1092 NYHrbYYyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWXTWHFpUUN3ME2yN{4zQDR|IN88US=> NX7BW5k5W0GQR1XS
RH-1 M17DOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVTMOpd{UUN3ME2yN{42OzV5IN88US=> M{D5UXNCVkeHUh?=
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NCI-H2342 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn\tTWM2OD1{ND62O|Y4KM7:TR?= MlzJV2FPT0WU
C32 Mm\0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF7ZOmxKSzVyPUK0Mlk2PzZizszN NIizTZdUSU6JRWK=
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NCI-H358 M{fVVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn;XTWM2OD1{NT6zPVQ{KM7:TR?= MkLpV2FPT0WU
CAL-85-1 NHHUc2lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVP6bnNNUUN3ME2yOU41PTd5IN88US=> MUHTRW5ITVJ?
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H-EMC-SS NWf3OJU2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWPJR|UxRTJ4LkSxNVQh|ryP Mn23V2FPT0WU
H4 NXq0fnVXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{TLVmlEPTB;Mk[uOFI1OyEQvF2= MkKxV2FPT0WU
DU-4475 M{LK[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoG5TWM2OD1{Nz6xPFczKM7:TR?= MX3TRW5ITVJ?
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MSTO-211H MmrMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4LKS2lEPTB;MkeuOlI2PSEQvF2= M3LOfnNCVkeHUh?=
NCI-H292 NFX1fWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXHJR|UxRTJ5Lkm2NVch|ryP NXrscoVbW0GQR1XS
NCI-H446 M2SwSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn3PTWM2OD1{OD6yNVA2KM7:TR?= MWHTRW5ITVJ?
NCI-H2009 M1rmTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlftTWM2OD1{OT6xOFMyKM7:TR?= NFm3eohUSU6JRWK=
MHH-ES-1 NGnHZ4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUPJR|UxRTJ7LkO2PFUh|ryP NV[3SWlUW0GQR1XS
TI-73 M1HRfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUH2V4VvUUN3ME2yPU41ODBzIN88US=> NHnoNWdUSU6JRWK=
NCI-H2228 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIX2RmpKSzVyPUK5MlQ2QCEQvF2= MkW2V2FPT0WU
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ChaGo-K-1 Mm\US5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUHJR|UxRTJ7Lk[wPVch|ryP NE\JT5ZUSU6JRWK=
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NBsusSR NGH6OmxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUXJR|UxRTJ7Lkm5NFQh|ryP Mn3DV2FPT0WU
NCI-H1304 MnHrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEnIc|BKSzVyPUOwMlU4OTZizszN M1OzZ3NCVkeHUh?=
NB14 M4LRd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlGyTWM2OD1|MT6wOFQ3KM7:TR?= NUfyXmo5W0GQR1XS
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KG-1 M2rSR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoWzTWM2OD1|MT63OFI6KM7:TR?= MXPTRW5ITVJ?
A2780 M4LQUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVPVU5JRUUN3ME2zNU45OzV6IN88US=> M2TJWHNCVkeHUh?=
NCI-H28 MknMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIXEc|ZKSzVyPUOxMlk5PjFizszN M{T4TnNCVkeHUh?=
C2BBe1 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF7nfFFKSzVyPUOyMlI3OzRizszN M2S2VnNCVkeHUh?=
VA-ES-BJ NVrqd29MT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWDrUGI5UUN3ME2zNk4{OSEQvF2= Ml\4V2FPT0WU
SBC-5 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYG4bHF3UUN3ME2zNk45PTFzIN88US=> NFHON4pUSU6JRWK=
OVCAR-4 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXnJR|UxRTN|LkS4OFgh|ryP MlvCV2FPT0WU
COR-L88 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3;RUGlEPTB;M{SuNFc1OSEQvF2= MWLTRW5ITVJ?
SW954 NYDHb2lTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MknXTWM2OD1|ND6wO|UzKM7:TR?= NEXjOpZUSU6JRWK=
COLO-684 NVKyfJNXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{HrO2lEPTB;M{SuN|QxPCEQvF2= NVHBe5Z3W0GQR1XS
HCC70 NF;N[2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYnG[HVIUUN3ME2zOE46PTF2IN88US=> NUDXRpB[W0GQR1XS
NCI-H1770 M1PJXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NESyXoFKSzVyPUO0Mlk3OSEQvF2= MlKxV2FPT0WU
NCI-H1666 NET2TnBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXfNcoNNUUN3ME2zOU45OjV|IN88US=> NFPCZ3dUSU6JRWK=
YH-13 NV65OpZmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{LDc2lEPTB;M{WuPVIh|ryP NFXT[opUSU6JRWK=
DJM-1 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml\uTWM2OD1|Nj64NFQ6KM7:TR?= NGTwWlRUSU6JRWK=
KNS-62 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWm2bnlIUUN3ME2zOk46PDN6IN88US=> M2PSOXNCVkeHUh?=
SK-MEL-30 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXfnOY5LUUN3ME2zO{45PzN5IN88US=> NYjEdYRTW0GQR1XS
SJRH30 NX3VdYxTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWi3U3R7UUN3ME2zPE44OzRzIN88US=> NEThelRUSU6JRWK=
GP5d NXHEWWlGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmHGTWM2OD1|OD64OlU{KM7:TR?= MlTJV2FPT0WU
SW1116 NX\KR5J1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYnsUXNHUUN3ME2zPU4zQDB3IN88US=> MnTFV2FPT0WU
COLO-800 M4jET2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVPzdYlwUUN3ME2zPU4{PjN6IN88US=> NGe5WnFUSU6JRWK=
RD MnfqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVXJR|UxRTN7LkWyOVgh|ryP NY\rNZdNW0GQR1XS
NCI-SNU-5 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2X4eWlEPTB;M{muOlkyPiEQvF2= MlzTV2FPT0WU
HuO-3N1 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1nrd2lEPTB;NECuNVA5KM7:TR?= NEnBdGRUSU6JRWK=
SK-UT-1 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkT6TWM2OD12MD61Olc1KM7:TR?= MlLYV2FPT0WU
SK-MEL-3 Ml;GS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmTtTWM2OD12MD61PVMzKM7:TR?= M{nWeXNCVkeHUh?=
SK-MEL-28 M2j6dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmTyTWM2OD12MD62OFM2KM7:TR?= M37qfHNCVkeHUh?=
SCC-4 M1Lwb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYjJR|UxRTRzLkKxN|ch|ryP MoHtV2FPT0WU
no-11 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2rNT2lEPTB;NEGuO|M2PCEQvF2= MWLTRW5ITVJ?
HT-144 NGrLb|JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWXJR|UxRTR{LkC1Olch|ryP MWXTRW5ITVJ?
MFM-223 MnHoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1jEU2lEPTB;NEKuOFAzKM7:TR?= MorpV2FPT0WU
ONS-76 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV7JR|UxRTR{LkiwNVgh|ryP NXX0dJRlW0GQR1XS
ES8 M2eyU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWrUWHh5UUN3ME20N{4{Pjl6IN88US=> NXTV[3pUW0GQR1XS
T-24 M{T3c2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIrj[nVKSzVyPUSzMlQ{PjlizszN M3PrSXNCVkeHUh?=
GAMG M4\kZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml\qTWM2OD12Mz60OVE4KM7:TR?= Mk\hV2FPT0WU
LU-135 NWCzfGttT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIXxcWNKSzVyPUS0MlA6OjNizszN MmH3V2FPT0WU
HCC1187 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIHlNZZKSzVyPUS0MlgzPjJizszN M3:5OnNCVkeHUh?=
TE-1 M4LuUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MU\JR|UxRTR3LkG2OVQh|ryP MnPpV2FPT0WU
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GI-ME-N NUPZdI5rT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1naPWlEPTB;NEWuPFk2OiEQvF2= M1XMeXNCVkeHUh?=
D-392MG MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoHyTWM2OD12NT65NlU3KM7:TR?= Mn;vV2FPT0WU
KALS-1 M{\wUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHjaSm9KSzVyPUS2MlczPTdizszN MVHTRW5ITVJ?
MMAC-SF M37YbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2DJfGlEPTB;NE[uPVk2OiEQvF2= NWOz[GZ7W0GQR1XS
HSC-3 M4nwT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFmzNFlKSzVyPUS3MlM3ODhizszN Mke5V2FPT0WU
KM-H2 NUfw[49vT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmXrTWM2OD12Nz62NFA4KM7:TR?= MWTTRW5ITVJ?
LoVo NGD2doFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHv1[2JKSzVyPUS4MlExODJizszN M3TaUHNCVkeHUh?=
NCI-H510A MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYTJR|UxRTR6LkG4O|Eh|ryP M4noUnNCVkeHUh?=
EW-11 M{[xS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYPJR|UxRTR6LkKzOFgh|ryP M1rLb3NCVkeHUh?=
HCC2998 MnX1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYHJR|UxRTR6Lk[yN|Yh|ryP MkjDV2FPT0WU
J82 NH7UV4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYfY[JdvUUN3ME20PE44OjR{IN88US=> M3HuUHNCVkeHUh?=
ML-2 NVHnXIdkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUPJR|UxRTR7LkS2NFUh|ryP M3e5cHNCVkeHUh?=
NCI-H2030 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHrEdIJKSzVyPUS5MlcyOTdizszN MlTYV2FPT0WU
NCI-H1792 NYP4dFNUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIHJflZKSzVyPUS5Mlg2OThizszN NGroZ2xUSU6JRWK=

... 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

文献中の引用 (18)

技術サポート&よくある質問(FAQ)

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