Nilotinib (AMN-107)

製品コードS1033

Nilotinib (AMN-107)化学構造

分子量(MW):529.52

Nilotinib (AMN-107) is a selective Bcr-Abl inhibitor with IC50 less than 30 nM in Murine myeloid progenitor cells.

サイズ 価格(税別)  
JPY 15106.00
JPY 11620.00
JPY 34860.00
JPY 78020.00

カスタマーフィードバック(5)

  • Ba/F3-p210T315I cells were treated with indicated concentrations of nilotinib with or without PDMP for 24 h. Apoptosis was determined as in A. Data are shown as percentage of sub-G1 for apoptosis in triplicate cultures. *P<0.05.

    FASEB J 2011 25, 3661-3673. Nilotinib (AMN-107) purchased from Selleck.

    Effect of nilotinib on Bcr-Abl kinase activity in ABCB1- and ABCG2- overexpressing CD34+CD38- cells. K562 parental cells and CD34+CD38- subpopulation isolated from K562 cells were treated with nilotinib at 0.01, 0.1 and 1.0 umol/L for 12 h. Equal amount of protein was loaded for western blot analysis as described in the Experimental section. The experiments were repeated at least three times independently, and a representative experiment is shown.

    Molecules 2014 19, 3356-75. Nilotinib (AMN-107) purchased from Selleck.

  •  

    Inhibition of thymidine (a and b) and cytarabine (c and d) uptake with nilotinib. The legend is similar to Fig. 1, except that imatinib was replaced by nilotinib.

    Leukemia Res 2012 36, 1311-1314. Nilotinib (AMN-107) purchased from Selleck.

    Nilotinib up-regulates the ERK survival signal in prostate cancer cells. (B and C) Immunoblot analyses of DU-145 cells (B) or DU-145 cells in comparison with LNCaP and PC-3 cells (C) treated with nilotinib for the expression of phospho-ERK1/2 T202/Y204 and total ERK. Immunoblot for GAPDH is shown as a loading control.

    Urol Oncol 2014 0.1016/j.urolonc.2014.06.001. Nilotinib (AMN-107) purchased from Selleck.

  • Immunohistochemical staining of xenografted DU-145 cells after 21 days of treatment with 75 mg/kg/d of nilotinib for phospho-ERK1/2 T202/Y204 expression. It can be noted that tumors explanted from vehicle-treated mice showed mostly positivity at the tumor periphery, whereas tumors explanted from nilotinib-treated mice showed a more evenly distributed phospho-ERK immunostaining (left panels). Quantification of phospho-ERK-positive DU-145 xenografts explanted after 21 days of treatment. Mean and standard errors of positive cells per high-power field (HPF; x40) from at least 3 tumors are given (right panel).

    Urol Oncol 2014 0.1016/j.urolonc.2014.06.001. Nilotinib (AMN-107) purchased from Selleck.

製品安全説明書

Bcr-Abl阻害剤の選択性比較

生物活性

製品説明 Nilotinib (AMN-107) is a selective Bcr-Abl inhibitor with IC50 less than 30 nM in Murine myeloid progenitor cells.
特性 A selective inhibitor of native and mutant Bcr-Abl.
ターゲット
Bcr-Abl [1]
(Murine myeloid progenitor cells)
<30 nM
体外試験

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]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
EoL-1-cell NYf5PXByT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVPmcGk5UUN3ME2wMlAxODF2NDFOwG0> M4\wS3NCVkeHUh?=
KU812 NXHITXk{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUDJR|UxRTBwMECyOFgh|ryP NXe5XXByW0GQR1XS
EM-2 M2q4[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWjBTHp6UUN3ME2wMlAxPDFizszN MWTTRW5ITVJ?
LAMA-84 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYDJR|UxRTBwMEC0PUDPxE1? NF[3SGJUSU6JRWK=
MEG-01 M{Xxcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWLJR|UxRTBwMEC4Nlgh|ryP MlXOV2FPT0WU
BV-173 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGWwWm5KSzVyPUCuNFExQDlizszN M4fidHNCVkeHUh?=
KASUMI-1 MnizS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVnoeVA2UUN3ME2wMlAzPDF|IN88US=> MnG4V2FPT0WU
NB7 NEXNO2RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXPqNXllUUN3ME2wMlE{PDN7IN88US=> M1e3eXNCVkeHUh?=
BHT-101 NXThc2lNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHLCUpVKSzVyPUCuOlQzPjNizszN MVHTRW5ITVJ?
CGTH-W-1 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYDUV5pmUUN3ME2wMlY1QDdizszN MnSwV2FPT0WU
HMV-II M1;oXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH\2em5KSzVyPUCuO|Q5PzRizszN Mn\xV2FPT0WU
NKM-1 NG\PTHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYfscmNpUUN3ME2wMlkxOTVizszN NWf5UpRJW0GQR1XS
LB2241-RCC MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MofSTWM2OD1zLkCyNlI5KM7:TR?= NGHvZ4dUSU6JRWK=
NCI-H1703 M1ToVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYfJR|UxRTFwMUi4O{DPxE1? MYXTRW5ITVJ?
BE-13 NXHCdJkyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXG0XI9mUUN3ME2xMlI4PDF4IN88US=> M1jiN3NCVkeHUh?=
ACN M{e5ZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlXuTWM2OD1zLkW1NFc4KM7:TR?= MoizV2FPT0WU
A204 NH;ETpRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXrTVJNJUUN3ME2xMlU4OjB3IN88US=> NXzpNGxvW0GQR1XS
HOP-62 MknxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUnTTYp[UUN3ME2xMlgzODd5IN88US=> M{nnfXNCVkeHUh?=
H9 MnPKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mmi0TWM2OD1{LkezO|k{KM7:TR?= Mkj0V2FPT0WU
HCC1806 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4HwSmlEPTB;Mj63OFMzPyEQvF2= MXLTRW5ITVJ?
NOS-1 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYT4fXZoUUN3ME2yMlg4OTB{IN88US=> M3zhOHNCVkeHUh?=
RS4-11 Ml[wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIfWOZlKSzVyPUKuPVA3OjNizszN MWjTRW5ITVJ?
JAR MoTPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIXaSlFKSzVyPUKuPVIxQDRizszN MXzTRW5ITVJ?
T98G MkPlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVnW[oRwUUN3ME2zMlAyOzF|IN88US=> NYf2SmpMW0GQR1XS
NCI-SNU-1 M4DRVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVXpWlIxUUN3ME2zMlQxODl{IN88US=> NFjWR2lUSU6JRWK=
SK-MEL-1 M4HLOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NETOdGRKSzVyPUOuOFMxOjlizszN NV74bHp{W0GQR1XS
L-363 MmXzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV\JR|UxRTNwNkGxNFch|ryP MVfTRW5ITVJ?
SW982 NHWwSoxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2rZNWlEPTB;Mz62OFE3QSEQvF2= NVfL[ZZrW0GQR1XS
HT-1080 NH3B[o9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2j0XGlEPTB;Mz65NVc4PSEQvF2= Mlz2V2FPT0WU
G-402 M{TidWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVHUWJFrUUN3ME20MlMyOjB|IN88US=> Mk\vV2FPT0WU
HOS MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHzmO3RKSzVyPUSuPFAzQDJizszN MUnTRW5ITVJ?
SK-NEP-1 NF75d2tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV\JR|UxRTRwOEOxPVEh|ryP NF\CXopUSU6JRWK=
HAL-01 NGHHXIFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGj6U2NKSzVyPUSuPFgzPDJizszN M37sc3NCVkeHUh?=
SBC-1 NG\hd|FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX:wNlRWUUN3ME20MlkxQTB5IN88US=> MXjTRW5ITVJ?
CTV-1 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXHJR|UxRTVwNEi5N|gh|ryP NIHqXXNUSU6JRWK=
LCLC-103H NEL5[VFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXPJR|UxRTVwN{e0O|Eh|ryP NUfTeIREW0GQR1XS
RVH-421 NHjLNXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlvGTWM2OD13Lke3OVM3KM7:TR?= MV;TRW5ITVJ?
K-562 MnfqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYXJR|UxRTVwOUCzOkDPxE1? NWfzcWpGW0GQR1XS
CAL-33 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV:xXFlWUUN3ME22MlMyOzV7IN88US=> M3y3cXNCVkeHUh?=
MDA-MB-361 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFLlbJFKSzVyPU[uN|M3QTlizszN NHfGSllUSU6JRWK=
IGROV-1 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWjJR|UxRTZwNEexPVEh|ryP MXHTRW5ITVJ?
NY NI\2bYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV\YeZFjUUN3ME22MlU{PTl7IN88US=> NIizS29USU6JRWK=
Ramos-2G6-4C10 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGnCTodKSzVyPU[uOlY6OzFizszN MXzTRW5ITVJ?
HuO9 NHXYPXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVrJR|UxRTZwN{O5OlQh|ryP MV3TRW5ITVJ?
MS-1 MofNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYDJR|UxRTdwMUG5OVMh|ryP NVHBNnR4W0GQR1XS
RPMI-8226 NWDJSnkyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NInOd3dKSzVyPUeuNlgzQDdizszN M2WxOXNCVkeHUh?=
HDLM-2 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mmm1TWM2OD15LkSwNVQ6KM7:TR?= MXjTRW5ITVJ?
D-566MG NGnNVohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3zQNWlEPTB;Nz60O|E2PSEQvF2= NV3WPXo6W0GQR1XS
SK-MEL-24 MlnlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVHsPFh4UUN3ME23MlY{Ozl{IN88US=> NGPSbGhUSU6JRWK=
COLO-679 NHLiSpVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2q5PWlEPTB;Nz65PFY4OSEQvF2= MWfTRW5ITVJ?
EW-13 M{TEbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWLJR|UxRThwM{KwOVQh|ryP Mn3SV2FPT0WU
A388 M{D5PWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXPPWG5lUUN3ME24MlM5PDhzIN88US=> MnLUV2FPT0WU
UM-UC-3 NUXHdpNtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2C1cGlEPTB;OD60N|k2PiEQvF2= M1\Uc3NCVkeHUh?=
NUGC-3 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3jLUmlEPTB;OD61N|U5OiEQvF2= M1nVZnNCVkeHUh?=
COLO-668 MoXYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MW\JR|UxRThwNUm0PVEh|ryP NE\UO25USU6JRWK=
MOLT-4 Mo\LS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlvZTWM2OD16Lk[yN|U{KM7:TR?= M1zXV3NCVkeHUh?=
D-423MG M3m5OWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkPiTWM2OD16LkizO|U3KM7:TR?= NVW4TW9NW0GQR1XS
CTB-1 MmHnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFjBWpZKSzVyPUiuPFcyOjhizszN NIi5Z3dUSU6JRWK=
BCPAP NGG2XXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV7JR|UxRTlwMEK1OlIh|ryP MWfTRW5ITVJ?
GCT M{D0XWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVnCdI14UUN3ME25MlA6QDNzIN88US=> M{fSSnNCVkeHUh?=
ACHN Mme1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVPPPG5KUUN3ME25MlI{PjN{IN88US=> NVPFZ4JDW0GQR1XS
KYSE-520 MonFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3KwfGlEPTB;OT6zN|Q5OiEQvF2= MVnTRW5ITVJ?
LB771-HNC NX3aU5hrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2Lhd2lEPTB;OT63OlQ6PyEQvF2= MWDTRW5ITVJ?
MLMA NGPlWGNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVLmdY17UUN3ME2xNE4xOTN{IN88US=> NVnxXFhyW0GQR1XS
HEC-1 NH7NfHhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3K2d2lEPTB;MUCuNlgxPCEQvF2= M4PjenNCVkeHUh?=
HL-60 NFTWNpBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmLnTWM2OD1zMD62PFU{KM7:TR?= NVHqbXVWW0GQR1XS
A101D MoDZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUnwTlc3UUN3ME2xNE45QTJ|IN88US=> NHLtbWRUSU6JRWK=
A2058 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1e3XGlEPTB;MUCuPVI1PSEQvF2= NGXtfllUSU6JRWK=
KARPAS-45 Mlq2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3fYR2lEPTB;MUGuNFY{PSEQvF2= MWjTRW5ITVJ?
697 M17SVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFq3TYZKSzVyPUGxMlIyODFizszN MXLTRW5ITVJ?
NCI-N87 NEXxT5pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4XtU2lEPTB;MUGuO|c{OSEQvF2= MorlV2FPT0WU
DSH1 NHHoSIdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUPndIYzUUN3ME2xNU44QTV|IN88US=> M33EWnNCVkeHUh?=
HLE NX\wPZV6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmS4TWM2OD1zMT64PFM6KM7:TR?= MVPTRW5ITVJ?
NCI-H720 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEDnPJpKSzVyPUGyMlY5ODFizszN M2r0dXNCVkeHUh?=
EW-3 M37acGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3T3fGlEPTB;MUKuPVMxPyEQvF2= MoXjV2FPT0WU
AGS NHHCdG1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGDYO49KSzVyPUGzMlA{PTFizszN NUm0TVJwW0GQR1XS
ES5 MkLtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoDpTWM2OD1zMz6wOVEzKM7:TR?= M{DMNnNCVkeHUh?=
DB MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF25NJFKSzVyPUGzMlMzPTZizszN M{jaTHNCVkeHUh?=
A4-Fuk Ml;nS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmfnTWM2OD1zMz60NVAzKM7:TR?= Mn\2V2FPT0WU
A427 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mon2TWM2OD1zMz60PVczKM7:TR?= NFTO[2RUSU6JRWK=
MN-60 NV;JT4t2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEDDWmVKSzVyPUGzMlU5PDNizszN MWrTRW5ITVJ?
HCC2218 MorKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4DvPGlEPTB;MUOuOVg2PiEQvF2= NU\leldmW0GQR1XS
MV-4-11 NVfX[lhQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmjETWM2OD1zMz64NVM4KM7:TR?= MXTTRW5ITVJ?
GI-1 NVG1TGVzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFLFfoRKSzVyPUG0MlEyQDRizszN NH\LT|hUSU6JRWK=
JVM-3 NUPQRnBXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4naRmlEPTB;MUSuNlY2PiEQvF2= M4TsO3NCVkeHUh?=
NCI-H2029 M3GxZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{nST2lEPTB;MUSuNlczPyEQvF2= M331V3NCVkeHUh?=
TE-12 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXfJR|UxRTF2Lk[wOFYh|ryP NID6eFJUSU6JRWK=
WM-115 MmrBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUHRS4E{UUN3ME2xOU42Pjh|IN88US=> NEXhZZVUSU6JRWK=
BB65-RCC M{\xUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVnJR|UxRTF4LkCyOFEh|ryP NY\OSnd5W0GQR1XS
NCI-H1693 NYn5OolMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV7JR|UxRTF4LkO4NFIh|ryP Mn3PV2FPT0WU
KARPAS-299 NILjbG9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYnJR|UxRTF4Lk[yNFMh|ryP MorkV2FPT0WU
UACC-257 NV7WOm5ET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWP0bGN5UUN3ME2xO{4xPTh{IN88US=> NIHBTlFUSU6JRWK=
RKO MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVLrVm1uUUN3ME2xO{43PDN|IN88US=> MWfTRW5ITVJ?
HT-29 M3HUbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWDJR|UxRTF5Lke4PFkh|ryP NUj4cGJOW0GQR1XS
ES7 MoL5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX\K[VBuUUN3ME2xPE4yOTJ{IN88US=> MlvXV2FPT0WU
DEL MnzFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXf0SJdqUUN3ME2xPE4{OTd{IN88US=> MXPTRW5ITVJ?
BT-549 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3zqR2lEPTB;MUiuOFA6OiEQvF2= Mn73V2FPT0WU
NCI-H1755 M4TvfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2i4d2lEPTB;MUiuOVczOyEQvF2= NWXMZo5iW0GQR1XS
HCE-T NXLHXnZWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX7JR|UxRTF6LkizOFEh|ryP M4\afXNCVkeHUh?=
LU-139 NUCzPWcyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnPBTWM2OD1zOT6wOFU5KM7:TR?= NI\DNVVUSU6JRWK=
ECC10 NIOy[otIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWHsWolTUUN3ME2xPU4zPDd3IN88US=> MUHTRW5ITVJ?
769-P M2TYVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NY[3N4psUUN3ME2xPU43OzN3IN88US=> Mn;vV2FPT0WU
BALL-1 NIfyZmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXrJR|UxRTF7Lk[3O|Uh|ryP M4CwSHNCVkeHUh?=
LXF-289 NUn6dolRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHzP[ZpKSzVyPUG5Mlg6PzlizszN NITUdpZUSU6JRWK=
TYK-nu NX;DOnFiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGm1c2lKSzVyPUG5Mlk{OTVizszN M1;wUnNCVkeHUh?=
NCI-H630 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYPMcpM4UUN3ME2xPU46Ozd6IN88US=> M4nyfXNCVkeHUh?=
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SCC-4 MlPKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlX1TWM2OD12MT6yNVM4KM7:TR?= M1vEWHNCVkeHUh?=
no-11 NY[2eXF7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1vYfmlEPTB;NEGuO|M2PCEQvF2= NYOwN4ZkW0GQR1XS
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MMAC-SF M4\aSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{jBU2lEPTB;NE[uPVk2OiEQvF2= MXPTRW5ITVJ?
HSC-3 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkjLTWM2OD12Nz6zOlA5KM7:TR?= M2rB[XNCVkeHUh?=
KM-H2 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3uzXWlEPTB;NEeuOlAxPyEQvF2= NX3lUFZyW0GQR1XS
LoVo NYTMVmh7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3;VbGlEPTB;NEiuNVAxOiEQvF2= NVfXSFl6W0GQR1XS
NCI-H510A NYPwXWRsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1;ONGlEPTB;NEiuNVg4OSEQvF2= NH[3RpdUSU6JRWK=
EW-11 NWfwVZhXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmTrTWM2OD12OD6yN|Q5KM7:TR?= MVrTRW5ITVJ?
HCC2998 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHP5[21KSzVyPUS4MlYzOzZizszN NVL1R4xmW0GQR1XS
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ML-2 M4fH[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH\GUWZKSzVyPUS5MlQ3ODVizszN M{S3bHNCVkeHUh?=
NCI-H2030 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFLCdm1KSzVyPUS5MlcyOTdizszN Mmm3V2FPT0WU
NCI-H1792 NVTobZNUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn2zTWM2OD12OT64OVE5KM7:TR?= NIHqToRUSU6JRWK=

他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

体内試験 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]

お薦めの試験操作(参考用のみ)

細胞試験: [4]
+ 展開
  • 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.
    (参考用のみ)
動物試験:[6]
+ 展開
  • 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
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 27 mg/mL (50.98 mM)
Water Insoluble
Ethanol Insoluble
体内 左から(NMPから)右の順に溶剤を製品に加えます(文献ではなく、Selleckの実験によるデータ):
4% DMSO+30% PEG 300+5% Tween 80+ddH2O
混合させたのち直ちに使用することを推奨します。
3mg/mL

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程で起きる正常な現象ですからご安心ください。

化学情報

分子量 529.52
化学式

C28H22F3N7O

CAS No. 641571-10-0
保管
in solvent
別名 N/A

便利ツール

モル濃度計算器

モル濃度計算器

求めたい質量、体積または濃度を計算してください。

質量 (g) = 濃度 (mol/L) x 体積 (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • 質量
    濃度
    体積
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備するために必要な希釈率を計算してください。Selleck希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 入力 出力 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

質量 濃度 体積 分子量

臨床試験

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03578367 Recruiting CML|Chronic Myelogenous Leukemia|Leukemia Myeloid Chronic|Hematologic Diseases Novartis Pharmaceuticals|Novartis November 12 2018 Phase 2
NCT03516279 Not yet recruiting Chronic Phase Chronic Myelogenous Leukemia BCR-ABL1 Positive|Minimal Residual Disease ECOG-ACRIN Cancer Research Group|National Cancer Institute (NCI)|Eastern Cooperative Oncology Group August 12 2018 Phase 2
NCT03654768 Recruiting Chronic Phase Chronic Myelogenous Leukemia BCR-ABL1 Positive Southwest Oncology Group|National Cancer Institute (NCI) July 20 2018 Phase 2
NCT03228303 Not yet recruiting Chronic Myeloid Leukemia Assiut University December 1 2017 Early Phase 1
NCT03205488 Recruiting Parkinson Disease Northwestern University|University of Rochester|University of Iowa|Michael J. Fox Foundation for Parkinson''s Research October 16 2017 Phase 2
NCT03079505 Recruiting Chronic Myeloid Leukemia - Chronic Phase Hamad Medical Corporation August 3 2017 Phase 3

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

  • * 必須

よくある質問(FAQ)

  • 質問1:

    I would like to use AMN-107 for in vivo studies in mice, can you give me some suggestions about the in vivo formulation?

  • 回答:

    For in vivo study, we recommend to use 4% DMSO+30% PEG 300+5% Tween 80+ddH2O up to 3mg/ml.

Bcr-Ablシグナル伝達経路

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Tags: Nilotinib (AMN-107)を買う | Nilotinib (AMN-107) ic50 | 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)化学構造 | Nilotinib (AMN-107)分子量 | Nilotinib (AMN-107)代理店
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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID