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 NX;3[oQ2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoHJTWM2OD1yLkCwNFE1PCEQvF2= M3:1UXNCVkeHUh?=
KU812 M1P5dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1fFdWlEPTB;MD6wNFI1QCEQvF2= NEGzW|FUSU6JRWK=
EM-2 M2LEcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEHsc3dKSzVyPUCuNFA1OSEQvF2= MV3TRW5ITVJ?
LAMA-84 M1PoVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVfB[JZVUUN3ME2wMlAxPDlizszN M4TWWXNCVkeHUh?=
MEG-01 NVfieW5jT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1rHdGlEPTB;MD6wNFgzQCEQvF2= NILJcGpUSU6JRWK=
BV-173 NUXhSJpXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NW\3UXcxUUN3ME2wMlAyODh7IN88US=> NIPKT4JUSU6JRWK=
KASUMI-1 M1rwO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoPXTWM2OD1yLkCyOFE{KM7:TR?= NF\PUW5USU6JRWK=
NB7 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFiyd3RKSzVyPUCuNVM1OzlizszN MXnTRW5ITVJ?
BHT-101 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX7iRYZMUUN3ME2wMlY1OjZ|IN88US=> MkHvV2FPT0WU
CGTH-W-1 MojDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFf1c5RKSzVyPUCuOlQ5PyEQvF2= MXzTRW5ITVJ?
HMV-II Ml7hS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml3JTWM2OD1yLke0PFc1KM7:TR?= MlT4V2FPT0WU
NKM-1 NFTIWlRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYmyfo9zUUN3ME2wMlkxOTVizszN NET1c4VUSU6JRWK=
LB2241-RCC MmrXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXPTN|F2UUN3ME2xMlAzOjJ6IN88US=> MUDTRW5ITVJ?
NCI-H1703 MlfvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV3JR|UxRTFwMUi4O{DPxE1? MYjTRW5ITVJ?
BE-13 M{T4OWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHHKRXpKSzVyPUGuNlc1OTZizszN NFnhbpFUSU6JRWK=
ACN M1W4Omdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYrJR|UxRTFwNUWwO|ch|ryP NXzqNYU4W0GQR1XS
A204 NUPlSFF{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFXLUlNKSzVyPUGuOVczODVizszN MUTTRW5ITVJ?
HOP-62 NHT2SI9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUjJR|UxRTFwOEKwO|ch|ryP NVm0RXltW0GQR1XS
H9 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1fHfWlEPTB;Mj63N|c6OyEQvF2= M2rPPHNCVkeHUh?=
HCC1806 NUnvWmE6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFLl[3dKSzVyPUKuO|Q{OjdizszN Mn7uV2FPT0WU
NOS-1 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnrBTWM2OD1{Lki3NVAzKM7:TR?= NUPLSXVPW0GQR1XS
RS4-11 Mkj0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWHJR|UxRTJwOUC2NlMh|ryP MWLTRW5ITVJ?
JAR NWiydG9vT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYr6TYZPUUN3ME2yMlkzODh2IN88US=> MkXZV2FPT0WU
T98G MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmD4TWM2OD1|LkCxN|E{KM7:TR?= MVvTRW5ITVJ?
NCI-SNU-1 MknmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGq2SXlKSzVyPUOuOFAxQTJizszN MnvWV2FPT0WU
SK-MEL-1 NYDVVph4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mli3TWM2OD1|LkSzNFI6KM7:TR?= MmfOV2FPT0WU
L-363 M3Lxc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYP6TVVxUUN3ME2zMlYyOTB5IN88US=> M1O3UXNCVkeHUh?=
SW982 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEn1[JpKSzVyPUOuOlQyPjlizszN M2D5bnNCVkeHUh?=
HT-1080 M4TVTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1e5ZWlEPTB;Mz65NVc4PSEQvF2= NHjpVFlUSU6JRWK=
G-402 NEDPTYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkPvTWM2OD12LkOxNlA{KM7:TR?= MVHTRW5ITVJ?
HOS M3PacWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYPJR|UxRTRwOECyPFIh|ryP NInpXpJUSU6JRWK=
SK-NEP-1 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV;JR|UxRTRwOEOxPVEh|ryP NITzV2ZUSU6JRWK=
HAL-01 M3LCU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWLJR|UxRTRwOEiyOFIh|ryP Mn3hV2FPT0WU
SBC-1 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{G1cGlEPTB;ND65NFkxPyEQvF2= M1rxbHNCVkeHUh?=
CTV-1 NYfl[nE6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmjOTWM2OD13LkS4PVM5KM7:TR?= M4Lj[nNCVkeHUh?=
LCLC-103H NI\mdpZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NG\TZopKSzVyPUWuO|c1PzFizszN NF;wZYtUSU6JRWK=
RVH-421 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYW5OGpnUUN3ME21Mlc4PTN4IN88US=> MXfTRW5ITVJ?
K-562 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUj3bopYUUN3ME21MlkxOzZizszN NHXzVpFUSU6JRWK=
CAL-33 NED0NndIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MY\JR|UxRTZwM{GzOVkh|ryP NF;WSVZUSU6JRWK=
MDA-MB-361 NYDuO2F1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mny5TWM2OD14LkOzOlk6KM7:TR?= MXPTRW5ITVJ?
IGROV-1 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmTvTWM2OD14LkS3NVkyKM7:TR?= MnfGV2FPT0WU
NY NV\KSYJrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFzENWtKSzVyPU[uOVM2QTlizszN NGfpcWRUSU6JRWK=
Ramos-2G6-4C10 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWHjXZVDUUN3ME22MlY3QTNzIN88US=> NGjKeIhUSU6JRWK=
HuO9 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml:xTWM2OD14LkezPVY1KM7:TR?= MWLTRW5ITVJ?
MS-1 M2i5c2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF3MVIVKSzVyPUeuNVE6PTNizszN M2LEOXNCVkeHUh?=
RPMI-8226 Mn7ES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXvJR|UxRTdwMkiyPFch|ryP NHnPOHdUSU6JRWK=
HDLM-2 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3\SOWlEPTB;Nz60NFE1QSEQvF2= Moe1V2FPT0WU
D-566MG M3H1Rmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoPsTWM2OD15LkS3NVU2KM7:TR?= MkjoV2FPT0WU
SK-MEL-24 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFnSWlhKSzVyPUeuOlM{QTJizszN NHXWb3lUSU6JRWK=
COLO-679 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{\ZPGlEPTB;Nz65PFY4OSEQvF2= M{fF[3NCVkeHUh?=
EW-13 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml7OTWM2OD16LkOyNFU1KM7:TR?= M1\rbnNCVkeHUh?=
A388 NEn0VJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnzSTWM2OD16LkO4OFgyKM7:TR?= MlnzV2FPT0WU
UM-UC-3 NGXLWWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmjzTWM2OD16LkSzPVU3KM7:TR?= NFzvUJJUSU6JRWK=
NUGC-3 NHLGOXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NES0cpRKSzVyPUiuOVM2QDJizszN Mn\YV2FPT0WU
COLO-668 MkPYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3\qV2lEPTB;OD61PVQ6OSEQvF2= MkXiV2FPT0WU
MOLT-4 NEftTGZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkLqTWM2OD16Lk[yN|U{KM7:TR?= MnzlV2FPT0WU
D-423MG M{O0O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MljGTWM2OD16LkizO|U3KM7:TR?= MkDZV2FPT0WU
CTB-1 M1Kwbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGLzfoNKSzVyPUiuPFcyOjhizszN NGPJWmZUSU6JRWK=
BCPAP MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXjTSlVMUUN3ME25MlAzPTZ{IN88US=> NFO1boxUSU6JRWK=
GCT NETFOJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYjIPZVIUUN3ME25MlA6QDNzIN88US=> NXTN[VdKW0GQR1XS
ACHN M{Hmfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn7lTWM2OD17LkKzOlMzKM7:TR?= M3LsW3NCVkeHUh?=
KYSE-520 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHXF[WlKSzVyPUmuN|M1QDJizszN M{TmT3NCVkeHUh?=
LB771-HNC M2rjNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mm\TTWM2OD17Lke2OFk4KM7:TR?= NHfrblNUSU6JRWK=
MLMA M{jTPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmXDTWM2OD1zMD6wNVMzKM7:TR?= NXrkUJpSW0GQR1XS
HEC-1 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWfJR|UxRTFyLkK4NFQh|ryP MnvmV2FPT0WU
HL-60 M2LycGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVzJR|UxRTFyLk[4OVMh|ryP MYDTRW5ITVJ?
A101D MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mnv5TWM2OD1zMD64PVI{KM7:TR?= MoTuV2FPT0WU
A2058 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFuwOVFKSzVyPUGwMlkzPDVizszN NULBc4gyW0GQR1XS
KARPAS-45 NF:0eXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYnJR|UxRTFzLkC2N|Uh|ryP NVPuTWdSW0GQR1XS
697 NYTCfmJXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX7JR|UxRTFzLkKxNFEh|ryP MWLTRW5ITVJ?
NCI-N87 NWL1PYNRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnzNTWM2OD1zMT63O|MyKM7:TR?= MXXTRW5ITVJ?
DSH1 NV3hW|ZtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{O2Z2lEPTB;MUGuO|k2OyEQvF2= MnrOV2FPT0WU
HLE M{m2bmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2WxSWlEPTB;MUGuPFg{QSEQvF2= M2XvRnNCVkeHUh?=
NCI-H720 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoTSTWM2OD1zMj62PFAyKM7:TR?= NYPQeYhvW0GQR1XS
EW-3 Mn70S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGrzZVJKSzVyPUGyMlk{ODdizszN M4\mO3NCVkeHUh?=
AGS M3XZcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHTpeXVKSzVyPUGzMlA{PTFizszN NIrpRWVUSU6JRWK=
ES5 NWDBUXBiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX7JR|UxRTF|LkC1NVIh|ryP NYThVZVCW0GQR1XS
DB MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX\KWmd7UUN3ME2xN{4{OjV4IN88US=> M4G4UnNCVkeHUh?=
A4-Fuk Mn;US5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn;RTWM2OD1zMz60NVAzKM7:TR?= Mm\1V2FPT0WU
A427 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUnqR5l5UUN3ME2xN{41QTd{IN88US=> M2PIRXNCVkeHUh?=
MN-60 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlPPTWM2OD1zMz61PFQ{KM7:TR?= NWjs[pkxW0GQR1XS
HCC2218 NHLNeWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1jPbmlEPTB;MUOuOVg2PiEQvF2= NFPjdXhUSU6JRWK=
MV-4-11 M4frRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVzIRnZUUUN3ME2xN{45OTN5IN88US=> M3\Re3NCVkeHUh?=
GI-1 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYH5[XNzUUN3ME2xOE4yOTh2IN88US=> MlfrV2FPT0WU
JVM-3 NEXZVG5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoO1TWM2OD1zND6yOlU3KM7:TR?= MkLjV2FPT0WU
NCI-H2029 M1G5OGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1rxWGlEPTB;MUSuNlczPyEQvF2= M4HGN3NCVkeHUh?=
TE-12 NUDPeFI1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEjpcXVKSzVyPUG0MlYxPDZizszN NGnWTIxUSU6JRWK=
WM-115 MorBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlvMTWM2OD1zNT61Olg{KM7:TR?= MnLyV2FPT0WU
BB65-RCC MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4TTNmlEPTB;MU[uNFI1OSEQvF2= M2XvOXNCVkeHUh?=
NCI-H1693 M1PwdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVHJR|UxRTF4LkO4NFIh|ryP MoHxV2FPT0WU
KARPAS-299 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkXyTWM2OD1zNj62NlA{KM7:TR?= NFr5VpRUSU6JRWK=
UACC-257 M{\qOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoLXTWM2OD1zNz6wOVgzKM7:TR?= MoC0V2FPT0WU
RKO NEjQR5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGDD[phKSzVyPUG3MlY1OzNizszN MWnTRW5ITVJ?
HT-29 NGPIWlNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYPxfnp2UUN3ME2xO{44QDh7IN88US=> NWnX[2hLW0GQR1XS
ES7 NXTGeo9zT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2W2OWlEPTB;MUiuNVEzOiEQvF2= MoHqV2FPT0WU
DEL MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{ezRWlEPTB;MUiuN|E4OiEQvF2= NED3UGVUSU6JRWK=
BT-549 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXP2VmM1UUN3ME2xPE41ODl{IN88US=> Mkj4V2FPT0WU
NCI-H1755 M3z5PWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWnJR|UxRTF6LkW3NlMh|ryP MVnTRW5ITVJ?
HCE-T NUewVJRvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEfQRW5KSzVyPUG4Mlg{PDFizszN NIH6e3BUSU6JRWK=
LU-139 NVTCVYM1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGnvW4pKSzVyPUG5MlA1PThizszN MULTRW5ITVJ?
ECC10 M{fEZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUHJR|UxRTF7LkK0O|Uh|ryP Mn\IV2FPT0WU
769-P NYi5cmZtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGLHW5hKSzVyPUG5MlY{OzVizszN M3z5dXNCVkeHUh?=
BALL-1 M3\JRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NELido5KSzVyPUG5MlY4PzVizszN MV\TRW5ITVJ?
LXF-289 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGfhW2hKSzVyPUG5Mlg6PzlizszN MVfTRW5ITVJ?
TYK-nu M2nZ[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3vhTmlEPTB;MUmuPVMyPSEQvF2= NGTo[IJUSU6JRWK=
NCI-H630 NG\WWFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXLESZhqUUN3ME2xPU46Ozd6IN88US=> MXPTRW5ITVJ?
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HSC-3 MmO3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkCzTWM2OD12Nz6zOlA5KM7:TR?= M335V3NCVkeHUh?=
KM-H2 MmDMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWPJR|UxRTR5Lk[wNFch|ryP MXTTRW5ITVJ?
LoVo MojHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{XNSWlEPTB;NEiuNVAxOiEQvF2= M4TTcnNCVkeHUh?=
NCI-H510A NXPrVJNzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVPS[nBPUUN3ME20PE4yQDdzIN88US=> NU\kT5E4W0GQR1XS
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HCC2998 M2nZOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkDRTWM2OD12OD62NlM3KM7:TR?= M2TITXNCVkeHUh?=
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ML-2 MmXpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVTy[Y5HUUN3ME20PU41PjB3IN88US=> MYjTRW5ITVJ?
NCI-H2030 NGXiPWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUjkS3FoUUN3ME20PU44OTF5IN88US=> M4HQTHNCVkeHUh?=
NCI-H1792 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXrk[JNDUUN3ME20PU45PTF6IN88US=> NHHMcJlUSU6JRWK=

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