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)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。

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)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。
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 M3ri[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXvzVFR5UUN3ME2wMlAxODF2NDFOwG0> M2Tle3NCVkeHUh?=
KU812 M1;iTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXP5Xog6UUN3ME2wMlAxOjR6IN88US=> MlLzV2FPT0WU
EM-2 NVnhVXFIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHjhb|BKSzVyPUCuNFA1OSEQvF2= NEDkPHlUSU6JRWK=
LAMA-84 M4XK[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGKz[WZKSzVyPUCuNFA1QSEQvF2= M1TnZnNCVkeHUh?=
MEG-01 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWDJR|UxRTBwMEC4Nlgh|ryP Ml2wV2FPT0WU
BV-173 MkewS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{XVXmlEPTB;MD6wNVA5QSEQvF2= MWTTRW5ITVJ?
KASUMI-1 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3P3TWlEPTB;MD6wNlQyOyEQvF2= NXLuOYFtW0GQR1XS
NB7 NEXjb2ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M13memlEPTB;MD6xN|Q{QSEQvF2= MmKyV2FPT0WU
BHT-101 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2HxbmlEPTB;MD62OFI3OyEQvF2= NYPjdlh[W0GQR1XS
CGTH-W-1 NV[1TGNIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3LQd2lEPTB;MD62OFg4KM7:TR?= MVTTRW5ITVJ?
HMV-II MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWTJR|UxRTBwN{S4O|Qh|ryP NIPxcpZUSU6JRWK=
NKM-1 MnvjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGfSR4tKSzVyPUCuPVAyPSEQvF2= NEWxSlhUSU6JRWK=
LB2241-RCC MoLmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NILqe5NKSzVyPUGuNFIzOjhizszN NXvQem0xW0GQR1XS
NCI-H1703 M3zJfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml;NTWM2OD1zLkG4PFch|ryP MULTRW5ITVJ?
BE-13 NVLiWY9oT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX\VPZdOUUN3ME2xMlI4PDF4IN88US=> MV3TRW5ITVJ?
ACN NFTTbJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{LrXWlEPTB;MT61OVA4PyEQvF2= NWT6[WtiW0GQR1XS
A204 Ml3JS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFjNS3JKSzVyPUGuOVczODVizszN MUDTRW5ITVJ?
HOP-62 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUf1TIFHUUN3ME2xMlgzODd5IN88US=> MWHTRW5ITVJ?
H9 M4jWfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWjJR|UxRTJwN{O3PVMh|ryP NWrmO4hDW0GQR1XS
HCC1806 M1O5[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3zqdGlEPTB;Mj63OFMzPyEQvF2= M2PBVnNCVkeHUh?=
NOS-1 NXSyfWxxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4\SPWlEPTB;Mj64O|ExOiEQvF2= NVzUVllKW0GQR1XS
RS4-11 Ml:3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NE\hRZhKSzVyPUKuPVA3OjNizszN MYXTRW5ITVJ?
JAR M{fDOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MojRTWM2OD1{LkmyNFg1KM7:TR?= M1LLOXNCVkeHUh?=
T98G MknWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYfJR|UxRTNwMEGzNVMh|ryP NIXhRXNUSU6JRWK=
NCI-SNU-1 NXLtPI1{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUTJR|UxRTNwNECwPVIh|ryP MWPTRW5ITVJ?
SK-MEL-1 NEG5OWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NW[0WI5QUUN3ME2zMlQ{ODJ7IN88US=> NVr4dIU3W0GQR1XS
L-363 MoDhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH[5[mdKSzVyPUOuOlEyODdizszN MYLTRW5ITVJ?
SW982 NH;keHdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUTUd3dLUUN3ME2zMlY1OTZ7IN88US=> M130THNCVkeHUh?=
HT-1080 M4\n[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIHWZZdKSzVyPUOuPVE4PzVizszN MUfTRW5ITVJ?
G-402 MorOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2izNWlEPTB;ND6zNVIxOyEQvF2= MnjqV2FPT0WU
HOS NUDINmpIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWLJR|UxRTRwOECyPFIh|ryP NIHIfGlUSU6JRWK=
SK-NEP-1 M{\Ldmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnX4TWM2OD12LkizNVkyKM7:TR?= NICyVIxUSU6JRWK=
HAL-01 NFP6[JFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYLHR3MzUUN3ME20Mlg5OjR{IN88US=> M2\5VXNCVkeHUh?=
SBC-1 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEPJNm5KSzVyPUSuPVA6ODdizszN MX\TRW5ITVJ?
CTV-1 M3Kzemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHnTd4hKSzVyPUWuOFg6OzhizszN M3;LbXNCVkeHUh?=
LCLC-103H NE[4VndIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVfJVIVMUUN3ME21Mlc4PDdzIN88US=> MliwV2FPT0WU
RVH-421 NIrP[2ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV;J[nlRUUN3ME21Mlc4PTN4IN88US=> NFXrbWdUSU6JRWK=
K-562 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NY\LVGhCUUN3ME21MlkxOzZizszN MmHyV2FPT0WU
CAL-33 NYn1bnQ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4D0NGlEPTB;Nj6zNVM2QSEQvF2= Mk[2V2FPT0WU
MDA-MB-361 NIXTNm1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2nRSmlEPTB;Nj6zN|Y6QSEQvF2= NHXiZo9USU6JRWK=
IGROV-1 Ml\MS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3vhWmlEPTB;Nj60O|E6OSEQvF2= M2ruenNCVkeHUh?=
NY NFfEPWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnrLTWM2OD14LkWzOVk6KM7:TR?= MnXwV2FPT0WU
Ramos-2G6-4C10 M120[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmDDTWM2OD14Lk[2PVMyKM7:TR?= NH7EOZNUSU6JRWK=
HuO9 NU\DSnhST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4T3UWlEPTB;Nj63N|k3PCEQvF2= NXXqVVJQW0GQR1XS
MS-1 NWCybFJXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVft[HJjUUN3ME23MlEyQTV|IN88US=> MnnIV2FPT0WU
RPMI-8226 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWrZNGd3UUN3ME23MlI5Ojh5IN88US=> MXzTRW5ITVJ?
HDLM-2 NEDCO2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX36TGJLUUN3ME23MlQxOTR7IN88US=> MXnTRW5ITVJ?
D-566MG MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF[0UFhKSzVyPUeuOFcyPTVizszN NF\6VVVUSU6JRWK=
SK-MEL-24 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4T0XWlEPTB;Nz62N|M6OiEQvF2= MmXTV2FPT0WU
COLO-679 Mn35S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVPRZ|V{UUN3ME23Mlk5PjdzIN88US=> NUfJWndHW0GQR1XS
EW-13 Mn;sS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1TTXWlEPTB;OD6zNlA2PCEQvF2= Mk\sV2FPT0WU
A388 NHLObnJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NE[xOWJKSzVyPUiuN|g1QDFizszN MlL3V2FPT0WU
UM-UC-3 M1H3O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1fa[GlEPTB;OD60N|k2PiEQvF2= MV3TRW5ITVJ?
NUGC-3 MoD3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2\MUWlEPTB;OD61N|U5OiEQvF2= Mn7aV2FPT0WU
COLO-668 M{nkd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmTxTWM2OD16LkW5OFkyKM7:TR?= NHPVcGNUSU6JRWK=
MOLT-4 NXz6T4tlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUjjRplPUUN3ME24MlYzOzV|IN88US=> MnW3V2FPT0WU
D-423MG MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{LwOWlEPTB;OD64N|c2PiEQvF2= MWDTRW5ITVJ?
CTB-1 M{\peWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3LaPWlEPTB;OD64O|EzQCEQvF2= NY\3c4VUW0GQR1XS
BCPAP NFXXU3JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4nkSmlEPTB;OT6wNlU3OiEQvF2= MkniV2FPT0WU
GCT MlG4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{nZOGlEPTB;OT6wPVg{OSEQvF2= MWTTRW5ITVJ?
ACHN M13se2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXnJR|UxRTlwMkO2N|Ih|ryP M2TGZ3NCVkeHUh?=
KYSE-520 M{n5PGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVHOUFJ1UUN3ME25MlM{PDh{IN88US=> MnviV2FPT0WU
LB771-HNC MlX5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGDCWplKSzVyPUmuO|Y1QTdizszN M1HrbXNCVkeHUh?=
MLMA NGn4eGdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF7FR21KSzVyPUGwMlAyOzJizszN MnLVV2FPT0WU
HEC-1 Ml3nS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmTCTWM2OD1zMD6yPFA1KM7:TR?= NH;GUnhUSU6JRWK=
HL-60 M4j4Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIfLc4dKSzVyPUGwMlY5PTNizszN M3\vS3NCVkeHUh?=
A101D MlrQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX3NZW9FUUN3ME2xNE45QTJ|IN88US=> MXLTRW5ITVJ?
A2058 Mnu5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlvZTWM2OD1zMD65NlQ2KM7:TR?= NYHEfG9nW0GQR1XS
KARPAS-45 NVPCUW9iT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYHJR|UxRTFzLkC2N|Uh|ryP NYW1dlZsW0GQR1XS
697 M2PLdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVzJR|UxRTFzLkKxNFEh|ryP MYHTRW5ITVJ?
NCI-N87 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1rsfGlEPTB;MUGuO|c{OSEQvF2= M{G1RXNCVkeHUh?=
DSH1 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFXTVmJKSzVyPUGxMlc6PTNizszN MoPPV2FPT0WU
HLE MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIHLOXhKSzVyPUGxMlg5OzlizszN NHXsVINUSU6JRWK=
NCI-H720 NFvudYNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4W4SWlEPTB;MUKuOlgxOSEQvF2= NHviSXlUSU6JRWK=
EW-3 M2\ORmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{DUdGlEPTB;MUKuPVMxPyEQvF2= M{TKNHNCVkeHUh?=
AGS NXvB[GhmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn3ZTWM2OD1zMz6wN|UyKM7:TR?= NGPKPWZUSU6JRWK=
ES5 NV\OWYI{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUXJR|UxRTF|LkC1NVIh|ryP MmfLV2FPT0WU
DB NF\GR5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4\ucWlEPTB;MUOuN|I2PiEQvF2= MkTxV2FPT0WU
A4-Fuk Ml;JS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWTR[XcyUUN3ME2xN{41OTB{IN88US=> M133W3NCVkeHUh?=
A427 NEHlfphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoPpTWM2OD1zMz60PVczKM7:TR?= MnXKV2FPT0WU
MN-60 NUjyNVBiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGXIXm9KSzVyPUGzMlU5PDNizszN NXLab5JDW0GQR1XS
HCC2218 NXW0Zno2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYjJR|UxRTF|LkW4OVYh|ryP M2jRZnNCVkeHUh?=
MV-4-11 M2nT[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIjqfY5KSzVyPUGzMlgyOzdizszN MYjTRW5ITVJ?
GI-1 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH74TpBKSzVyPUG0MlEyQDRizszN NV7yPZNVW0GQR1XS
JVM-3 M37aNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXG5RVdXUUN3ME2xOE4zPjV4IN88US=> MlL6V2FPT0WU
NCI-H2029 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWfaT2I4UUN3ME2xOE4zPzJ5IN88US=> MWfTRW5ITVJ?
TE-12 NHLaPXBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWfQOIVuUUN3ME2xOE43ODR4IN88US=> MWDTRW5ITVJ?
WM-115 NFPPNYhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVniOHA1UUN3ME2xOU42Pjh|IN88US=> NVjaUWVrW0GQR1XS
BB65-RCC M3f1RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGPpcItKSzVyPUG2MlAzPDFizszN NWTucWwyW0GQR1XS
NCI-H1693 NX;oZmN6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXTLe3gxUUN3ME2xOk4{QDB{IN88US=> NFP1RnpUSU6JRWK=
KARPAS-299 NHLUNZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mnm2TWM2OD1zNj62NlA{KM7:TR?= NWW0S2c6W0GQR1XS
UACC-257 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYjJR|UxRTF5LkC1PFIh|ryP NW[zSm9KW0GQR1XS
RKO M4nGbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVvJR|UxRTF5Lk[0N|Mh|ryP NGXKSnJUSU6JRWK=
HT-29 NXvE[nVkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmXLTWM2OD1zNz63PFg6KM7:TR?= MkTWV2FPT0WU
ES7 NUm4RVJRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4fJUmlEPTB;MUiuNVEzOiEQvF2= MlfuV2FPT0WU
DEL MnfwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIXuWZVKSzVyPUG4MlMyPzJizszN M1PXXnNCVkeHUh?=
BT-549 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGHyZ3dKSzVyPUG4MlQxQTJizszN M3T2Z3NCVkeHUh?=
NCI-H1755 M3\ZRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFLKR2tKSzVyPUG4MlU4OjNizszN Mmn4V2FPT0WU
HCE-T NHuyZ4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NILaZYlKSzVyPUG4Mlg{PDFizszN MoDhV2FPT0WU
LU-139 NFzmPFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYnJR|UxRTF7LkC0OVgh|ryP NWi1N3hDW0GQR1XS
ECC10 NGj4PG5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{nyS2lEPTB;MUmuNlQ4PSEQvF2= MWrTRW5ITVJ?
769-P M2rXcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoHQTWM2OD1zOT62N|M2KM7:TR?= NX\KT2xvW0GQR1XS
BALL-1 NELIcFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnPqTWM2OD1zOT62O|c2KM7:TR?= Mkf1V2FPT0WU
LXF-289 M3HiVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX3JR|UxRTF7Lki5O|kh|ryP NX;jNFJmW0GQR1XS
TYK-nu MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlraTWM2OD1zOT65N|E2KM7:TR?= NUTwc3B[W0GQR1XS
NCI-H630 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlTETWM2OD1zOT65N|c5KM7:TR?= NWXqRWJsW0GQR1XS
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COR-L88 M{DPXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFzT[XRKSzVyPUO0MlA4PDFizszN MXvTRW5ITVJ?
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COLO-684 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnzqTWM2OD1|ND6zOFA1KM7:TR?= NIHHOGNUSU6JRWK=
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NCI-H1770 MoPCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVzJR|UxRTN2Lkm2NUDPxE1? NFHNPGNUSU6JRWK=
NCI-H1666 NHXseI1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXLRTY9HUUN3ME2zOU45OjV|IN88US=> NV[1dIR2W0GQR1XS
YH-13 NILscVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUjJR|UxRTN3LkmyJO69VQ>? MVnTRW5ITVJ?
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GP5d MmPrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2jX[GlEPTB;M{iuPFY2OyEQvF2= MV\TRW5ITVJ?
SW1116 NGTNSG5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWnyWGJLUUN3ME2zPU4zQDB3IN88US=> M1\pfnNCVkeHUh?=
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RD NHm1[YNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M33qb2lEPTB;M{muOVI2QCEQvF2= M1e3cnNCVkeHUh?=
NCI-SNU-5 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml;MTWM2OD1|OT62PVE3KM7:TR?= MkHyV2FPT0WU
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SK-MEL-3 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3i0d2lEPTB;NECuOVk{OiEQvF2= NIGzV5lUSU6JRWK=
SK-MEL-28 NYjaR3BOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlXxTWM2OD12MD62OFM2KM7:TR?= NYXtNodsW0GQR1XS
SCC-4 NFvzVY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXzYeplyUUN3ME20NU4zOTN5IN88US=> MU\TRW5ITVJ?
no-11 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NELRVm5KSzVyPUSxMlc{PTRizszN MX3TRW5ITVJ?
HT-144 NFXEOlJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4TwNGlEPTB;NEKuNFU3PyEQvF2= M3;jc3NCVkeHUh?=
MFM-223 NXPxcnd7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NG\aS3NKSzVyPUSyMlQxOiEQvF2= NWLVVJRpW0GQR1XS
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GAMG MlmwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2LCUmlEPTB;NEOuOFUyPyEQvF2= NG[zdGJUSU6JRWK=
LU-135 Mn3tS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmDMTWM2OD12ND6wPVI{KM7:TR?= NG\lfG5USU6JRWK=
HCC1187 MkXIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4rnOmlEPTB;NESuPFI3OiEQvF2= NHW2XYRUSU6JRWK=
TE-1 Ml3mS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4XTSGlEPTB;NEWuNVY2PCEQvF2= Ml3TV2FPT0WU
J-RT3-T3-5 M1;jeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2fid2lEPTB;NEWuOFMyPSEQvF2= MnPTV2FPT0WU
GI-ME-N NImzUFFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlfNTWM2OD12NT64PVUzKM7:TR?= M2LsTHNCVkeHUh?=
D-392MG MoPrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFzxdlhKSzVyPUS1MlkzPTZizszN M4XvU3NCVkeHUh?=
KALS-1 M3;qeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYfOeZluUUN3ME20Ok44OjV5IN88US=> NVTldmtDW0GQR1XS
MMAC-SF Mme1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGC1NYtKSzVyPUS2Mlk6PTJizszN MVTTRW5ITVJ?
HSC-3 M{jyVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWXudXJiUUN3ME20O{4{PjB6IN88US=> MYDTRW5ITVJ?
KM-H2 NFXaU45Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVPQSIc4UUN3ME20O{43ODB5IN88US=> NGj5NpRUSU6JRWK=
LoVo MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3vubmlEPTB;NEiuNVAxOiEQvF2= MX7TRW5ITVJ?
NCI-H510A NWHt[I05T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmDGTWM2OD12OD6xPFcyKM7:TR?= NUX0SlJyW0GQR1XS
EW-11 NV;oeIx3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4DSS2lEPTB;NEiuNlM1QCEQvF2= NV7S[ZloW0GQR1XS
HCC2998 MkHUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnnsTWM2OD12OD62NlM3KM7:TR?= MVvTRW5ITVJ?
J82 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUXJR|UxRTR6LkeyOFIh|ryP NWXadW9SW0GQR1XS
ML-2 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFLHR2tKSzVyPUS5MlQ3ODVizszN M2[xdnNCVkeHUh?=
NCI-H2030 NEnHeJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF[xR4VKSzVyPUS5MlcyOTdizszN NF\W[HpUSU6JRWK=
NCI-H1792 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1XZfGlEPTB;NEmuPFUyQCEQvF2= Mn;jV2FPT0WU

多くの細胞株試験データを見る場合、クリックしてください

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 順序で溶剤を入れること:
4% DMSO+30% PEG 300+5% Tween 80+ddH2O
3mg/mL

* 溶解度検測はSelleck技術部門によって行いますので、文献より提供された溶解度と差異がある可能性がありますが、生産工芸と不同ロット(lot)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
別名 N/A

便利ツール

モル濃度計算器

モル濃度計算器

解決のために必要とされるマス、ボリュームまたは濃度を計算してください。

マス (g) = 濃度 (mol/L) x ボリューム (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • マス
    濃度
    ボリューム
    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

貯蔵液を準備することを要求される希釈剤を計算してください. セレック希釈計算器は、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 ( 輸入 輸出 )

  • 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

マス 濃度 ボリューム 分子量

臨床試験

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02973711 Not yet recruiting Leukemia, Chronic Myeloid University of Michigan Cancer Center February 2017 Phase 1|Phase 2
NCT02954978 Recruiting Parkinson Disease|Parkinsons Disease With Dementia Georgetown University January 2017 Phase 2
NCT02947893 Recruiting Alzheimers Disease Georgetown University January 2017 Phase 2
NCT02602314 Not yet recruiting Chronyc Myeloid Leukemia Gruppo Italiano Malattie EMatologiche dellAdulto December 2016 Phase 4
NCT02709083 Recruiting Chronic Myelogenous Leukemia|Chronic Myeloid Leukemia|Leukemia Emory University October 2016 Phase 2
NCT02917720 Not yet recruiting Chronic Myeloid Leukemia European LeukemiaNet|Heidelberg University|Ludwig-Maximilians - University of Munich October 2016 Phase 2

技術サポート

ストックの作り方、阻害剤の保管する方法、細胞実験や動物実験に注意すべきな点を全部含めており、製品を取扱う時よくあった質問に対して取扱説明書でお答えいたします。

Handling Instructions

他の質問がある場合は、お気軽くお問合せください。

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Bcr-Abl信号経路図

Bcr-Abl Inhibitors with Unique Features

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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