Nilotinib (AMN-107)

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。

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Nilotinib (AMN-107) 化学構造
分子量: 529.52

高品質保証

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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。
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 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWDDUow4UUN3ME2wMlAxODF2NDFOwG0> NULleJNKW0GQR1XS
KU812 NVq0T5FIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4T4U2lEPTB;MD6wNFI1QCEQvF2= Mmq1V2FPT0WU
EM-2 M1m4fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXjlNZY{UUN3ME2wMlAxPDFizszN MUnTRW5ITVJ?
LAMA-84 NHrYRZZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MofsTWM2OD1yLkCwOFkh|ryP NWjtNHZEW0GQR1XS
MEG-01 M1vm[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEDvfGhKSzVyPUCuNFA5OjhizszN M4PSeXNCVkeHUh?=
BV-173 M4rvVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlqzTWM2OD1yLkCxNFg6KM7:TR?= M1PPTnNCVkeHUh?=
KASUMI-1 M{XlWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEXEZ4pKSzVyPUCuNFI1OTNizszN NIG1RlNUSU6JRWK=
NB7 NXnFVZJOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYjJR|UxRTBwMUO0N|kh|ryP NE[2fG5USU6JRWK=
BHT-101 M1\iUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmWxTWM2OD1yLk[0NlY{KM7:TR?= NG\ISGlUSU6JRWK=
CGTH-W-1 NGTGNVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGnQcJBKSzVyPUCuOlQ5PyEQvF2= M3qzNHNCVkeHUh?=
HMV-II NHTje4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1TrS2lEPTB;MD63OFg4PCEQvF2= NHPiZmNUSU6JRWK=
NKM-1 MlLYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVOzPI9yUUN3ME2wMlkxOTVizszN MWLTRW5ITVJ?
LB2241-RCC MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGjoRW5KSzVyPUGuNFIzOjhizszN M{HsU3NCVkeHUh?=
NCI-H1703 MoDKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnnUTWM2OD1zLkG4PFch|ryP MVTTRW5ITVJ?
BE-13 NXnTPGcyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mmr6TWM2OD1zLkK3OFE3KM7:TR?= NVzwOI5qW0GQR1XS
ACN NFj0[YhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn;ETWM2OD1zLkW1NFc4KM7:TR?= NF7mbIdUSU6JRWK=
A204 MlLJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NInRW|hKSzVyPUGuOVczODVizszN MVvTRW5ITVJ?
HOP-62 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn75TWM2OD1zLkiyNFc4KM7:TR?= M3e0WnNCVkeHUh?=
H9 NFvsVFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGmw[GlKSzVyPUKuO|M4QTNizszN M13ERnNCVkeHUh?=
HCC1806 NH7WUG5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX7JR|UxRTJwN{SzNlch|ryP MnHFV2FPT0WU
NOS-1 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFj2VXdKSzVyPUKuPFcyODJizszN M{TwUXNCVkeHUh?=
RS4-11 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGTRSJhKSzVyPUKuPVA3OjNizszN M4TaT3NCVkeHUh?=
JAR NHnPW|RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUj2Rm1{UUN3ME2yMlkzODh2IN88US=> MVzTRW5ITVJ?
T98G NHrQWYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NITs[WxKSzVyPUOuNFE{OTNizszN Ml25V2FPT0WU
NCI-SNU-1 NEPOVGRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVzJR|UxRTNwNECwPVIh|ryP MnPCV2FPT0WU
SK-MEL-1 NH;YNHFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NE\odZZKSzVyPUOuOFMxOjlizszN NHK0S5lUSU6JRWK=
L-363 NGTSN2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoW1TWM2OD1|Lk[xNVA4KM7:TR?= NH22bnhUSU6JRWK=
SW982 NWHRZWdqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml\MTWM2OD1|Lk[0NVY6KM7:TR?= MUHTRW5ITVJ?
HT-1080 NXPmS294T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIS0fHZKSzVyPUOuPVE4PzVizszN NVvXXml3W0GQR1XS
G-402 M3jiNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWfkdGZmUUN3ME20MlMyOjB|IN88US=> MlLHV2FPT0WU
HOS M2G2Wmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1jKWGlEPTB;ND64NFI5OiEQvF2= NIDkeWdUSU6JRWK=
SK-NEP-1 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1HT[2lEPTB;ND64N|E6OSEQvF2= MoXlV2FPT0WU
HAL-01 M33uSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NETJVYxKSzVyPUSuPFgzPDJizszN NYm3SWZSW0GQR1XS
SBC-1 MojGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGn5[YVKSzVyPUSuPVA6ODdizszN MYrTRW5ITVJ?
CTV-1 MkfWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{PwfGlEPTB;NT60PFk{QCEQvF2= NXXnNXh2W0GQR1XS
LCLC-103H NFzrNmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUjJR|UxRTVwN{e0O|Eh|ryP MVnTRW5ITVJ?
RVH-421 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MonDTWM2OD13Lke3OVM3KM7:TR?= Mn3sV2FPT0WU
K-562 NInzbYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnSxTWM2OD13LkmwN|Yh|ryP MV\TRW5ITVJ?
CAL-33 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWnJR|UxRTZwM{GzOVkh|ryP NGD1c29USU6JRWK=
MDA-MB-361 M1niWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYfXS5V6UUN3ME22MlM{Pjl7IN88US=> NXvzN5N7W0GQR1XS
IGROV-1 MnzRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYnJR|UxRTZwNEexPVEh|ryP MY\TRW5ITVJ?
NY NHjYVI9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH\6NHJKSzVyPU[uOVM2QTlizszN MknEV2FPT0WU
Ramos-2G6-4C10 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVvFR4VlUUN3ME22MlY3QTNzIN88US=> MnfwV2FPT0WU
HuO9 NGfuOI1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlvUTWM2OD14LkezPVY1KM7:TR?= NEWydHhUSU6JRWK=
MS-1 MlLyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlS4TWM2OD15LkGxPVU{KM7:TR?= M1PtcnNCVkeHUh?=
RPMI-8226 NUG0N5N[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVPjbFZzUUN3ME23MlI5Ojh5IN88US=> NGTBS3FUSU6JRWK=
HDLM-2 M1rjfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEjmZnhKSzVyPUeuOFAyPDlizszN NEPITodUSU6JRWK=
D-566MG MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXnq[IxFUUN3ME23MlQ4OTV3IN88US=> MVLTRW5ITVJ?
SK-MEL-24 NITRSItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXrLe4tnUUN3ME23MlY{Ozl{IN88US=> NIXTbYRUSU6JRWK=
COLO-679 M{i3emdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHviUGFKSzVyPUeuPVg3PzFizszN NGi0W|VUSU6JRWK=
EW-13 M2e4d2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX;JR|UxRThwM{KwOVQh|ryP M3XldXNCVkeHUh?=
A388 NYj3VGtPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoXKTWM2OD16LkO4OFgyKM7:TR?= NELRTWpUSU6JRWK=
UM-UC-3 NUWzXm5kT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFSw[3lKSzVyPUiuOFM6PTZizszN NGTlblJUSU6JRWK=
NUGC-3 NEP3WYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGXYW5BKSzVyPUiuOVM2QDJizszN MU\TRW5ITVJ?
COLO-668 M4q2[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoLpTWM2OD16LkW5OFkyKM7:TR?= NEL1R5RUSU6JRWK=
MOLT-4 NH;zRopIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWfJR|UxRThwNkKzOVMh|ryP M3;Bb3NCVkeHUh?=
D-423MG NXL6VGVyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MknQTWM2OD16LkizO|U3KM7:TR?= MXLTRW5ITVJ?
CTB-1 M{HqWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXvJR|UxRThwOEexNlgh|ryP NX\3U3pEW0GQR1XS
BCPAP NUTtVXJRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVfJR|UxRTlwMEK1OlIh|ryP NVXnc|NPW0GQR1XS
GCT MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlfCTWM2OD17LkC5PFMyKM7:TR?= NFS2PIdUSU6JRWK=
ACHN NH\HOI1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWeySpF2UUN3ME25MlI{PjN{IN88US=> MY\TRW5ITVJ?
KYSE-520 NH;6[ZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHPHe4VKSzVyPUmuN|M1QDJizszN MlrTV2FPT0WU
LB771-HNC MlrRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEjCW4RKSzVyPUmuO|Y1QTdizszN NUTuc|h3W0GQR1XS
MLMA M2HsUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVXJR|UxRTFyLkCxN|Ih|ryP M{jYbHNCVkeHUh?=
HEC-1 NIDHOYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NI\uSWpKSzVyPUGwMlI5ODRizszN MnXUV2FPT0WU
HL-60 M3LPemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mkm5TWM2OD1zMD62PFU{KM7:TR?= M{H6VXNCVkeHUh?=
A101D MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlKyTWM2OD1zMD64PVI{KM7:TR?= M3vEfnNCVkeHUh?=
A2058 M3HUemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmH4TWM2OD1zMD65NlQ2KM7:TR?= NWLVd2x1W0GQR1XS
KARPAS-45 MkTUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3jlZ2lEPTB;MUGuNFY{PSEQvF2= M1v5U3NCVkeHUh?=
697 NECzZmNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml:3TWM2OD1zMT6yNVAyKM7:TR?= MlfUV2FPT0WU
NCI-N87 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkfYTWM2OD1zMT63O|MyKM7:TR?= M3q5TXNCVkeHUh?=
DSH1 NFTOTHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUnJR|UxRTFzLke5OVMh|ryP MUHTRW5ITVJ?
HLE M2XWSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MULJR|UxRTFzLki4N|kh|ryP M1X6U3NCVkeHUh?=
NCI-H720 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV;JR|UxRTF{Lk[4NFEh|ryP NEny[JlUSU6JRWK=
EW-3 Mle1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUezU|YzUUN3ME2xNk46OzB5IN88US=> MnPrV2FPT0WU
AGS NIryPHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2\FVGlEPTB;MUOuNFM2OSEQvF2= MUjTRW5ITVJ?
ES5 M{TwfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4HG[mlEPTB;MUOuNFUyOiEQvF2= NXnYPYRRW0GQR1XS
DB M1frS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHvZR|hKSzVyPUGzMlMzPTZizszN MYLTRW5ITVJ?
A4-Fuk MoXjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUXJR|UxRTF|LkSxNFIh|ryP M3KwXXNCVkeHUh?=
A427 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGXFelhKSzVyPUGzMlQ6PzJizszN MmfSV2FPT0WU
MN-60 NFzpU4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXzJR|UxRTF|LkW4OFMh|ryP M4r4[XNCVkeHUh?=
HCC2218 MmTnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVXJR|UxRTF|LkW4OVYh|ryP MVjTRW5ITVJ?
MV-4-11 NUC0cZRWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXjyfFJDUUN3ME2xN{45OTN5IN88US=> M4nObnNCVkeHUh?=
GI-1 MmPkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M135TGlEPTB;MUSuNVE5PCEQvF2= MmezV2FPT0WU
JVM-3 MmXiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH3JXoVKSzVyPUG0MlI3PTZizszN NEi4WFBUSU6JRWK=
NCI-H2029 M3nyZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3PiUmlEPTB;MUSuNlczPyEQvF2= M1jMRXNCVkeHUh?=
TE-12 NUXJVVRGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUXJR|UxRTF2Lk[wOFYh|ryP MkXXV2FPT0WU
WM-115 M3TrWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWrJR|UxRTF3LkW2PFMh|ryP MUPTRW5ITVJ?
BB65-RCC M17KRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVLZNldWUUN3ME2xOk4xOjRzIN88US=> MlzNV2FPT0WU
NCI-H1693 M4TWRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYTtdVZEUUN3ME2xOk4{QDB{IN88US=> NV\KdWd4W0GQR1XS
KARPAS-299 M4jG[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHXFfJlKSzVyPUG2MlYzODNizszN MUDTRW5ITVJ?
UACC-257 Ml3KS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX;3fphZUUN3ME2xO{4xPTh{IN88US=> NITLS4ZUSU6JRWK=
RKO NHfReIFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmWyTWM2OD1zNz62OFM{KM7:TR?= MnOwV2FPT0WU
HT-29 M1jyWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYLJR|UxRTF5Lke4PFkh|ryP M4fBZXNCVkeHUh?=
ES7 M3rLcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYfJR|UxRTF6LkGxNlIh|ryP M{T1R3NCVkeHUh?=
DEL NF7wNo5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoCzTWM2OD1zOD6zNVczKM7:TR?= NG\sTW1USU6JRWK=
BT-549 NWfxVY5DT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFewSIZKSzVyPUG4MlQxQTJizszN NH;zNJhUSU6JRWK=
NCI-H1755 NWjh[3FHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYjvdpN2UUN3ME2xPE42PzJ|IN88US=> NIDQ[oxUSU6JRWK=
HCE-T MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHLkRW1KSzVyPUG4Mlg{PDFizszN NXjzWINwW0GQR1XS
LU-139 NWnYW4pET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4LnXmlEPTB;MUmuNFQ2QCEQvF2= MmT2V2FPT0WU
ECC10 M1HTXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGfT[mtKSzVyPUG5MlI1PzVizszN MnzhV2FPT0WU
769-P Mmr0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV3XT3FsUUN3ME2xPU43OzN3IN88US=> MV3TRW5ITVJ?
BALL-1 Mki1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX3ucXNMUUN3ME2xPU43Pzd3IN88US=> M2jwU3NCVkeHUh?=
LXF-289 MnnjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4TWS2lEPTB;MUmuPFk4QSEQvF2= NVjsSXYyW0GQR1XS
TYK-nu MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mon5TWM2OD1zOT65N|E2KM7:TR?= NXnZcmlSW0GQR1XS
NCI-H630 NX[4R5plT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkfKTWM2OD1zOT65N|c5KM7:TR?= NHz4NolUSU6JRWK=
EW-18 M{G0d2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVnJR|UxRTJyLkO4NFIh|ryP NUn5e2F4W0GQR1XS
KYSE-150 MmPLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGP6fnVKSzVyPUKwMlcxPDdizszN NUnWUZZEW0GQR1XS
LOXIMVI M4j4VGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGHTbZVKSzVyPUKwMlc2QDZizszN MUHTRW5ITVJ?
HuP-T3 NXj6eFBiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWnJR|UxRTJzLkC4OVIh|ryP MVjTRW5ITVJ?
MFE-280 NEW0PGlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXqyWFBVUUN3ME2yNU42Pjd7IN88US=> NWG4eoVGW0GQR1XS
SK-OV-3 MnvPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV\JR|UxRTJzLki0NFgh|ryP MYjTRW5ITVJ?
QIMR-WIL M{H0RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1fhSGlEPTB;MkKuNFQ4QCEQvF2= NWjXOlhbW0GQR1XS
NCI-H69 NECzeZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIfYb2xKSzVyPUKyMlQzQTlizszN MY\TRW5ITVJ?
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NCI-H2228 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mke1TWM2OD1{OT60OVgh|ryP NGm2fJpUSU6JRWK=
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MFM-223 NHK3ZnVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHjxRYJKSzVyPUSyMlQxOiEQvF2= M{fLWXNCVkeHUh?=
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GAMG MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYPJR|UxRTR|LkS1NVch|ryP NWmwcXFTW0GQR1XS
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NCI-H2030 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXHJR|UxRTR7LkexNVch|ryP NHvR[GdUSU6JRWK=
NCI-H1792 M1vzV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{HDPWlEPTB;NEmuPFUyQCEQvF2= NHHNZ2hUSU6JRWK=

... 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 3年-20℃
2年-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 27 mg/mL (50.98 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
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 (19)

技術サポート&よくある質問(FAQ)

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    Features:Dual Bcr-Abl/Lyn inhibitor.

  • Degrasyn (WP1130)

    Degrasyn (WP1130)は一種の選択性的なdeubiquitinase(DUB: USP5、UCH-L1、USP9x、USP14と UCH37)阻害剤ですが、Bcr/Ablを抑制する作用があります。Degrasyn (WP1130)も一種のJAK2トランスデューサ(20Sプロテアソームに影響を与えない)と転写活性剤(STAT)です。

    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)は一種のBcr-Abl阻害剤で、Abl1(WT)とAbl1(T315I)に作用する時のIC50値が0.8 nMと4 nMです。DCC-2036 (Rebastinib)はSRC、LYN、FGR、HCK、KDR、FLT3とTie-2も抑制しますが、c-Kitに低い抑制活性を表します。臨床1期。

    Features:A conformational control inhibitor of Abl1 and T315I Abl1.

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Tags: Nilotinib (AMN-107)を買う | 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)代理店
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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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