Nilotinib (AMN-107) 化学構造
分子量: 529.52

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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、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 NF;ZU3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX;JR|UxRTBwMECwNVQ1KM7:TR?= NIXZfJhUSU6JRWK=
KU812 MmTiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4nHTGlEPTB;MD6wNFI1QCEQvF2= M1LxPHNCVkeHUh?=
EM-2 NUTjXXRtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXzVUpNrUUN3ME2wMlAxPDFizszN M{n1R3NCVkeHUh?=
LAMA-84 M1y4SGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NITyeFJKSzVyPUCuNFA1QSEQvF2= NGrr[W1USU6JRWK=
MEG-01 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGDveVFKSzVyPUCuNFA5OjhizszN NVzDb4ZTW0GQR1XS
BV-173 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnewTWM2OD1yLkCxNFg6KM7:TR?= NXfxfoFTW0GQR1XS
KASUMI-1 MkTFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4LR[2lEPTB;MD6wNlQyOyEQvF2= NV7yWmU3W0GQR1XS
NB7 MoHkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1XRU2lEPTB;MD6xN|Q{QSEQvF2= NXy5fW5rW0GQR1XS
BHT-101 NHyyNWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXr1emNpUUN3ME2wMlY1OjZ|IN88US=> MWPTRW5ITVJ?
CGTH-W-1 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmryTWM2OD1yLk[0PFch|ryP Mlz0V2FPT0WU
HMV-II M{O0V2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVXJR|UxRTBwN{S4O|Qh|ryP NXPGWFBOW0GQR1XS
NKM-1 M3XkdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M13sbWlEPTB;MD65NFE2KM7:TR?= NG\ReHFUSU6JRWK=
LB2241-RCC M{LLUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmfzTWM2OD1zLkCyNlI5KM7:TR?= MXjTRW5ITVJ?
NCI-H1703 M1vC[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1HR[2lEPTB;MT6xPFg4KM7:TR?= Mlv6V2FPT0WU
BE-13 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlflTWM2OD1zLkK3OFE3KM7:TR?= MlH5V2FPT0WU
ACN NGTI[VBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1LBUmlEPTB;MT61OVA4PyEQvF2= NXLxRpExW0GQR1XS
A204 NIPWWnFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVPJR|UxRTFwNUeyNFUh|ryP M{nRb3NCVkeHUh?=
HOP-62 MonVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2PMTGlEPTB;MT64NlA4PyEQvF2= MnP3V2FPT0WU
H9 NYi3PW93T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWLZO3QzUUN3ME2yMlc{Pzl|IN88US=> M{fETXNCVkeHUh?=
HCC1806 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M33SRWlEPTB;Mj63OFMzPyEQvF2= MnjyV2FPT0WU
NOS-1 NEXkNotIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYnvSWp7UUN3ME2yMlg4OTB{IN88US=> NFHjcndUSU6JRWK=
RS4-11 NXPYN4hyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3TWbmlEPTB;Mj65NFYzOyEQvF2= NH;5WopUSU6JRWK=
JAR NF3PepdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWXBXFRDUUN3ME2yMlkzODh2IN88US=> NHXNb5ZUSU6JRWK=
T98G NUjGe3FzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2\TWWlEPTB;Mz6wNVMyOyEQvF2= MUXTRW5ITVJ?
NCI-SNU-1 NH7O[pRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYXiWXZ[UUN3ME2zMlQxODl{IN88US=> MormV2FPT0WU
SK-MEL-1 NFLKNHhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3r4NGlEPTB;Mz60N|AzQSEQvF2= MmP4V2FPT0WU
L-363 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlTCTWM2OD1|Lk[xNVA4KM7:TR?= NXHpcFA{W0GQR1XS
SW982 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWnJR|UxRTNwNkSxOlkh|ryP MnfFV2FPT0WU
HT-1080 Ml[2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUjJR|UxRTNwOUG3O|Uh|ryP M{TEZ3NCVkeHUh?=
G-402 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHHoboZKSzVyPUSuN|EzODNizszN NVHPTHhWW0GQR1XS
HOS MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkPRTWM2OD12LkiwNlgzKM7:TR?= NHraV|BUSU6JRWK=
SK-NEP-1 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXjJR|UxRTRwOEOxPVEh|ryP M4jXPXNCVkeHUh?=
HAL-01 M1;CXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUnMNXJGUUN3ME20Mlg5OjR{IN88US=> NGT0bINUSU6JRWK=
SBC-1 M125fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NImwZWFKSzVyPUSuPVA6ODdizszN NFTzR21USU6JRWK=
CTV-1 NXXkPGxkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUPVPGIyUUN3ME21MlQ5QTN6IN88US=> MX;TRW5ITVJ?
LCLC-103H M2LEfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUjJR|UxRTVwN{e0O|Eh|ryP NIrqb2RUSU6JRWK=
RVH-421 M4q2NGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mle2TWM2OD13Lke3OVM3KM7:TR?= NYnYWld{W0GQR1XS
K-562 M4PtV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV\JR|UxRTVwOUCzOkDPxE1? M2rBcHNCVkeHUh?=
CAL-33 M{XXdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXHaVZpMUUN3ME22MlMyOzV7IN88US=> M4O5ZnNCVkeHUh?=
MDA-MB-361 MmLjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2ToOmlEPTB;Nj6zN|Y6QSEQvF2= MUPTRW5ITVJ?
IGROV-1 M2PCNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFjtfHdKSzVyPU[uOFcyQTFizszN MkfBV2FPT0WU
NY M2DOOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUnJR|UxRTZwNUO1PVkh|ryP MUjTRW5ITVJ?
Ramos-2G6-4C10 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmrUTWM2OD14Lk[2PVMyKM7:TR?= MXfTRW5ITVJ?
HuO9 NUPWPGdlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml7XTWM2OD14LkezPVY1KM7:TR?= MYjTRW5ITVJ?
MS-1 NX3w[oQzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1OycWlEPTB;Nz6xNVk2OyEQvF2= NYTpblVNW0GQR1XS
RPMI-8226 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlLZTWM2OD15LkK4Nlg4KM7:TR?= MUfTRW5ITVJ?
HDLM-2 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYnJR|UxRTdwNECxOFkh|ryP NWjLeWdtW0GQR1XS
D-566MG MlPDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmqzTWM2OD15LkS3NVU2KM7:TR?= NYjH[4ZiW0GQR1XS
SK-MEL-24 NG\2cGhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVvJR|UxRTdwNkOzPVIh|ryP NE[1VmhUSU6JRWK=
COLO-679 NInSfJlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH:yRmFKSzVyPUeuPVg3PzFizszN MUHTRW5ITVJ?
EW-13 NX[2ZXk{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml3tTWM2OD16LkOyNFU1KM7:TR?= M{TxbnNCVkeHUh?=
A388 MkLZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnTKTWM2OD16LkO4OFgyKM7:TR?= NYjGeFRFW0GQR1XS
UM-UC-3 NVnOd3ZqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEXSOZBKSzVyPUiuOFM6PTZizszN NIXYV3RUSU6JRWK=
NUGC-3 MlL6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVPJR|UxRThwNUO1PFIh|ryP Mn7oV2FPT0WU
COLO-668 NXqxR|BbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3rXdGlEPTB;OD61PVQ6OSEQvF2= NHXLb|dUSU6JRWK=
MOLT-4 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmThTWM2OD16Lk[yN|U{KM7:TR?= MmPDV2FPT0WU
D-423MG M1v1[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4TiZ2lEPTB;OD64N|c2PiEQvF2= NFvGV29USU6JRWK=
CTB-1 M3fO[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mli3TWM2OD16Lki3NVI5KM7:TR?= MknGV2FPT0WU
BCPAP NXG4dlBmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEXPe2tKSzVyPUmuNFI2PjJizszN M{\mSXNCVkeHUh?=
GCT M3f0SGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXjvZYw1UUN3ME25MlA6QDNzIN88US=> M2Swb3NCVkeHUh?=
ACHN NEHtOnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1XYc2lEPTB;OT6yN|Y{OiEQvF2= M363d3NCVkeHUh?=
KYSE-520 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2jYXGlEPTB;OT6zN|Q5OiEQvF2= M4jlWXNCVkeHUh?=
LB771-HNC MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXXSTHlbUUN3ME25Mlc3PDl5IN88US=> Mmq4V2FPT0WU
MLMA NXTzfXZ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXfWSo42UUN3ME2xNE4xOTN{IN88US=> M2[zc3NCVkeHUh?=
HEC-1 Ml7nS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGXmOGlKSzVyPUGwMlI5ODRizszN NE\WNIRUSU6JRWK=
HL-60 NIHKSphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYrMcGJkUUN3ME2xNE43QDV|IN88US=> M1PrZnNCVkeHUh?=
A101D NV2w[oNVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoezTWM2OD1zMD64PVI{KM7:TR?= MXrTRW5ITVJ?
A2058 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYnJR|UxRTFyLkmyOFUh|ryP NUXufnZWW0GQR1XS
KARPAS-45 MoTCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXvUdZNvUUN3ME2xNU4xPjN3IN88US=> NGLY[W9USU6JRWK=
697 M2nhT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX;JR|UxRTFzLkKxNFEh|ryP MkPBV2FPT0WU
NCI-N87 MljWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYH2d4l7UUN3ME2xNU44PzNzIN88US=> MWfTRW5ITVJ?
DSH1 M4[2RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUTNSWFWUUN3ME2xNU44QTV|IN88US=> MUjTRW5ITVJ?
HLE NVLwclF5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVW1OVBnUUN3ME2xNU45QDN7IN88US=> NV\3NJN{W0GQR1XS
NCI-H720 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX[2W2h4UUN3ME2xNk43QDBzIN88US=> NFHQTYZUSU6JRWK=
EW-3 NGnvWJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1nKc2lEPTB;MUKuPVMxPyEQvF2= M{Swe3NCVkeHUh?=
AGS MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnHBTWM2OD1zMz6wN|UyKM7:TR?= MmLOV2FPT0WU
ES5 MnrCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NInwdY9KSzVyPUGzMlA2OTJizszN NFn0VJFUSU6JRWK=
DB M4LaXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NU\lfVcyUUN3ME2xN{4{OjV4IN88US=> M3fySnNCVkeHUh?=
A4-Fuk MkXpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWDJR|UxRTF|LkSxNFIh|ryP M2WycnNCVkeHUh?=
A427 NYjMPVFwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1foUmlEPTB;MUOuOFk4OiEQvF2= MUjTRW5ITVJ?
MN-60 MkiyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NILkS4tKSzVyPUGzMlU5PDNizszN MmrlV2FPT0WU
HCC2218 NEfud4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M13JRmlEPTB;MUOuOVg2PiEQvF2= NV;4WHlTW0GQR1XS
MV-4-11 NYfPR41ST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUfJR|UxRTF|LkixN|ch|ryP NH;FSotUSU6JRWK=
GI-1 NF;WXZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFz5W5VKSzVyPUG0MlEyQDRizszN NVPLd2k4W0GQR1XS
JVM-3 NHfLRXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIjT[5dKSzVyPUG0MlI3PTZizszN MlP6V2FPT0WU
NCI-H2029 M1X1cGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mle3TWM2OD1zND6yO|I4KM7:TR?= M1i1S3NCVkeHUh?=
TE-12 NELONG9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX\JR|UxRTF2Lk[wOFYh|ryP MX\TRW5ITVJ?
WM-115 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{mzZ2lEPTB;MUWuOVY5OyEQvF2= MmjtV2FPT0WU
BB65-RCC MlPQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoXxTWM2OD1zNj6wNlQyKM7:TR?= NHLsepNUSU6JRWK=
NCI-H1693 MmLTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF\ZTHlKSzVyPUG2MlM5ODJizszN MWHTRW5ITVJ?
KARPAS-299 NVfxe3ZHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWm1cGtkUUN3ME2xOk43OjB|IN88US=> MWTTRW5ITVJ?
UACC-257 MoDYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWP0SpVbUUN3ME2xO{4xPTh{IN88US=> NHyyblhUSU6JRWK=
RKO NXjjT2FCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYrJR|UxRTF5Lk[0N|Mh|ryP M1vMVXNCVkeHUh?=
HT-29 M2LVRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4D5PGlEPTB;MUeuO|g5QSEQvF2= M3i0cnNCVkeHUh?=
ES7 M2XQeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmrPTWM2OD1zOD6xNVIzKM7:TR?= NWKxTFhHW0GQR1XS
DEL NUjadnZ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV7JR|UxRTF6LkOxO|Ih|ryP M4fnVHNCVkeHUh?=
BT-549 NY\oTlliT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{CyWGlEPTB;MUiuOFA6OiEQvF2= Mnf5V2FPT0WU
NCI-H1755 NETrelNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmfNTWM2OD1zOD61O|I{KM7:TR?= M{fpOHNCVkeHUh?=
HCE-T NXrKSJBLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmrUTWM2OD1zOD64N|QyKM7:TR?= M2q5[HNCVkeHUh?=
LU-139 NF7uVXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX;LVndvUUN3ME2xPU4xPDV6IN88US=> MnTaV2FPT0WU
ECC10 M{L3bGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2jVZ2lEPTB;MUmuNlQ4PSEQvF2= MVvTRW5ITVJ?
769-P Mki0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYTnZpEzUUN3ME2xPU43OzN3IN88US=> NFzGZZFUSU6JRWK=
BALL-1 NWrO[|U6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWTJR|UxRTF7Lk[3O|Uh|ryP MkDwV2FPT0WU
LXF-289 NUC2T5ZLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1rHcWlEPTB;MUmuPFk4QSEQvF2= MYXTRW5ITVJ?
TYK-nu M2Xn[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmKzTWM2OD1zOT65N|E2KM7:TR?= MYTTRW5ITVJ?
NCI-H630 Mnq2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIW1VJpKSzVyPUG5Mlk{PzhizszN M2fse3NCVkeHUh?=
EW-18 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVOw[45kUUN3ME2yNE4{QDB{IN88US=> MmHTV2FPT0WU
KYSE-150 M163dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4PXVWlEPTB;MkCuO|A1PyEQvF2= NVfiPZAxW0GQR1XS
LOXIMVI NHn0XmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXLJR|UxRTJyLke1PFYh|ryP MlWxV2FPT0WU
HuP-T3 M1PTXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXTJR|UxRTJzLkC4OVIh|ryP MlTDV2FPT0WU
MFE-280 NXnNbolIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYLJR|UxRTJzLkW2O|kh|ryP NWLnPJRmW0GQR1XS
SK-OV-3 M2HrWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVHoWJFxUUN3ME2yNU45PDB6IN88US=> NEDsd|hUSU6JRWK=
QIMR-WIL Mki2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlrsTWM2OD1{Mj6wOFc5KM7:TR?= NIjVOGpUSU6JRWK=
NCI-H69 Mm\3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHLFXVBKSzVyPUKyMlQzQTlizszN MlLuV2FPT0WU
TE-5 MojYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmjjTWM2OD1{Mj60PVY2KM7:TR?= M3q1b3NCVkeHUh?=
NCI-H1993 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1jQfGlEPTB;MkKuOFk4OSEQvF2= NWS2OZo4W0GQR1XS
NCI-H1092 NV3WTpR7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUXrVlQ1UUN3ME2yN{4zQDR|IN88US=> M3nsWnNCVkeHUh?=
RH-1 NVfpfWNtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHuy[IJKSzVyPUKzMlU{PTdizszN MU\TRW5ITVJ?
DBTRG-05MG MkHtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFWxXIJKSzVyPUKzMlg1PzJizszN NYn3VnlFW0GQR1XS
Mo-T M3jhZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGfSc|BKSzVyPUKzMlkh|ryP M4qyUHNCVkeHUh?=
HD-MY-Z MnzRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmPUTWM2OD1{ND6yN|YzKM7:TR?= Mn31V2FPT0WU
NCI-H2342 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWXJR|UxRTJ2Lk[3Olch|ryP NULqcIRMW0GQR1XS
C32 NX[3WJFRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIS1OGRKSzVyPUK0Mlk2PzZizszN M4C4PHNCVkeHUh?=
HTC-C3 NGDOe5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3TwVGlEPTB;MkWuN|U4PyEQvF2= NInofXpUSU6JRWK=
NCI-H358 M1\1XWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mm\hTWM2OD1{NT6zPVQ{KM7:TR?= M2n3d3NCVkeHUh?=
CAL-85-1 NHzEV|RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWrIT2ZUUUN3ME2yOU41PTd5IN88US=> MljBV2FPT0WU
HT-1197 M2\kOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1LITGlEPTB;MkWuOVMyQSEQvF2= NI\WXWdUSU6JRWK=
A172 NVL1bHh{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmO2TWM2OD1{NT63NVM3KM7:TR?= NFm1cpZUSU6JRWK=
SW1573 M1n1[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn\oTWM2OD1{NT63O|g2KM7:TR?= MWPTRW5ITVJ?
EW-24 NIGxeVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUTPSVREUUN3ME2yOU46PjJizszN MljHV2FPT0WU
SK-MEL-2 NITwZpZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml\KTWM2OD1{Nj6wN|EzKM7:TR?= NYGzXHQ2W0GQR1XS
LU-65 NVPKbmg4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1r6TWlEPTB;Mk[uNFQ2OiEQvF2= MWTTRW5ITVJ?
KMOE-2 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXHJR|UxRTJ4LkC5NVUh|ryP M3\UWHNCVkeHUh?=
H-EMC-SS M4TKN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmfLTWM2OD1{Nj60NVE1KM7:TR?= NGHSTIdUSU6JRWK=
H4 NHry[mFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mm\MTWM2OD1{Nj60NlQ{KM7:TR?= NEDYc2VUSU6JRWK=
DU-4475 MnLwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXHJR|UxRTJ5LkG4O|Ih|ryP NV3GU2RoW0GQR1XS
HCT-116 MlzrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoixTWM2OD1{Nz60N|Q6KM7:TR?= MoPRV2FPT0WU
MSTO-211H NEn4VYNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1;YRmlEPTB;MkeuOlI2PSEQvF2= M2nhNXNCVkeHUh?=
NCI-H292 MoW3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVnqepV6UUN3ME2yO{46PjF5IN88US=> NFziNW5USU6JRWK=
NCI-H446 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXfJR|UxRTJ6LkKxNFUh|ryP MWTTRW5ITVJ?
NCI-H2009 NInJVGJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUfJR|UxRTJ7LkG0N|Eh|ryP NFf2T2lUSU6JRWK=
MHH-ES-1 NIjSN3hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV7JR|UxRTJ7LkO2PFUh|ryP M4PhOHNCVkeHUh?=
TI-73 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYD2fm5qUUN3ME2yPU41ODBzIN88US=> NXfkRmk1W0GQR1XS
NCI-H2228 NUTIS|AyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHfP[YtKSzVyPUK5MlQ2QCEQvF2= NH\mPWJUSU6JRWK=
MHH-PREB-1 M1\wd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEDKdo9KSzVyPUK5MlU2ODVizszN NUT6[FV7W0GQR1XS
ChaGo-K-1 NFfRc2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MonVTWM2OD1{OT62NFk4KM7:TR?= MmXXV2FPT0WU
KY821 M3PHdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUHYRnpvUUN3ME2yPU43PDN|IN88US=> M3PZR3NCVkeHUh?=
NCI-H209 NFLJSnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn\XTWM2OD1{OT64N|Y3KM7:TR?= NGDKfGFUSU6JRWK=
NBsusSR NF\VNXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYHJR|UxRTJ7Lkm5NFQh|ryP M{TlUXNCVkeHUh?=
NCI-H1304 NW\sbVFyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYjzNZpSUUN3ME2zNE42PzF4IN88US=> MWnTRW5ITVJ?
NB14 MojUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmPDTWM2OD1|MT6wOFQ3KM7:TR?= NUO5THV2W0GQR1XS
HCC1419 NYXWOZlQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVvWUI9yUUN3ME2zNU4zPCEQvF2= NFrUcFBUSU6JRWK=
KG-1 NIrPZ2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYjJR|UxRTNzLke0Nlkh|ryP NXjHRVRtW0GQR1XS
A2780 NILVNnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1uz[mlEPTB;M{GuPFM2QCEQvF2= M1vUUHNCVkeHUh?=
NCI-H28 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnW1TWM2OD1|MT65PFYyKM7:TR?= NHm0OW5USU6JRWK=
C2BBe1 M3PySGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NE\Mb2hKSzVyPUOyMlI3OzRizszN MmPFV2FPT0WU
VA-ES-BJ NF;Y[3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2ezXWlEPTB;M{KuN|Eh|ryP MWrTRW5ITVJ?
SBC-5 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MojzTWM2OD1|Mj64OVEyKM7:TR?= NILNTnlUSU6JRWK=
OVCAR-4 NF3ZSXBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3XWbWlEPTB;M{OuOFg1QCEQvF2= MYfTRW5ITVJ?
COR-L88 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFjpNotKSzVyPUO0MlA4PDFizszN NYPPSpVXW0GQR1XS
SW954 NWfjUWVZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX;UVotVUUN3ME2zOE4xPzV{IN88US=> Mm\OV2FPT0WU
COLO-684 NV20dph[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHn6ToVKSzVyPUO0MlM1ODRizszN NXTyb4JiW0GQR1XS
HCC70 NIHIWWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX\Gc2pPUUN3ME2zOE46PTF2IN88US=> MYLTRW5ITVJ?
NCI-H1770 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2fuV2lEPTB;M{SuPVYyKM7:TR?= M1;nbnNCVkeHUh?=
NCI-H1666 M{DBb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1GyXGlEPTB;M{WuPFI2OyEQvF2= MkPBV2FPT0WU
YH-13 NILoXWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFnCNpZKSzVyPUO1MlkzKM7:TR?= MXHTRW5ITVJ?
DJM-1 NHHZfoJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MofCTWM2OD1|Nj64NFQ6KM7:TR?= MXLTRW5ITVJ?
KNS-62 MoG2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGHafWlKSzVyPUO2Mlk1OzhizszN MXTTRW5ITVJ?
SK-MEL-30 Mne3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWPJR|UxRTN5Lki3N|ch|ryP MWrTRW5ITVJ?
SJRH30 MmPOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUTJR|UxRTN6LkezOFEh|ryP MXvTRW5ITVJ?
GP5d NInBN5pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYrL[4pqUUN3ME2zPE45PjV|IN88US=> MnXMV2FPT0WU
SW1116 NVTD[HJOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NG[zb5pKSzVyPUO5MlI5ODVizszN MmT6V2FPT0WU
COLO-800 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX\aU|NmUUN3ME2zPU4{PjN6IN88US=> M3TxTHNCVkeHUh?=
RD NFK5ZlNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWjXZXVFUUN3ME2zPU42OjV6IN88US=> MWTTRW5ITVJ?
NCI-SNU-5 NILnc4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUnJR|UxRTN7Lk[5NVYh|ryP NUfqPHB5W0GQR1XS
HuO-3N1 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3HacGlEPTB;NECuNVA5KM7:TR?= M{DQWnNCVkeHUh?=
SK-UT-1 M3fiOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWTRU4tWUUN3ME20NE42Pjd2IN88US=> MVHTRW5ITVJ?
SK-MEL-3 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlLaTWM2OD12MD61PVMzKM7:TR?= MkG0V2FPT0WU
SK-MEL-28 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXjJR|UxRTRyLk[0N|Uh|ryP MXjTRW5ITVJ?
SCC-4 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGmwcWpKSzVyPUSxMlIyOzdizszN MkS0V2FPT0WU
no-11 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFfvRotKSzVyPUSxMlc{PTRizszN MWjTRW5ITVJ?
HT-144 MmDHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXzHRm5ZUUN3ME20Nk4xPTZ5IN88US=> MXLTRW5ITVJ?
MFM-223 NGfVVINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NW\KWoRkUUN3ME20Nk41ODJizszN NFfvV45USU6JRWK=
ONS-76 NV3mVIZbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmX2TWM2OD12Mj64NFE5KM7:TR?= M1KybHNCVkeHUh?=
ES8 M{jYXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXzxXXdMUUN3ME20N{4{Pjl6IN88US=> NVzabmJzW0GQR1XS
T-24 NUPwV2FZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2fXfGlEPTB;NEOuOFM3QSEQvF2= NVf3fGRtW0GQR1XS
GAMG MnvFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWf2V2I6UUN3ME20N{41PTF5IN88US=> MYPTRW5ITVJ?
LU-135 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1\q[GlEPTB;NESuNFkzOyEQvF2= MWnTRW5ITVJ?
HCC1187 NH36bpJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2Lmb2lEPTB;NESuPFI3OiEQvF2= NEjvdmtUSU6JRWK=
TE-1 M1;KRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M17RPWlEPTB;NEWuNVY2PCEQvF2= NEDMfJlUSU6JRWK=
J-RT3-T3-5 NWXITYdHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3\3[WlEPTB;NEWuOFMyPSEQvF2= NYnoRmxZW0GQR1XS
GI-ME-N M1fseGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYLmeGhvUUN3ME20OU45QTV{IN88US=> M3G3W3NCVkeHUh?=
D-392MG NXz0dHRbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVfB[pBnUUN3ME20OU46OjV4IN88US=> MkjyV2FPT0WU
KALS-1 NXTreYRTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWm1PY56UUN3ME20Ok44OjV5IN88US=> NXPTVodOW0GQR1XS
MMAC-SF MnPOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHjuZoVKSzVyPUS2Mlk6PTJizszN MoXJV2FPT0WU
HSC-3 NHnYbm1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXvJR|UxRTR5LkO2NFgh|ryP MnTuV2FPT0WU
KM-H2 NITjd|RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFHtZYdKSzVyPUS3MlYxODdizszN M3WyRnNCVkeHUh?=
LoVo NVy5UWEyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIPaO2pKSzVyPUS4MlExODJizszN Mnv3V2FPT0WU
NCI-H510A NYDOfpA6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX3JR|UxRTR6LkG4O|Eh|ryP NYfKfItHW0GQR1XS
EW-11 NGjEXZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUL4[IpXUUN3ME20PE4zOzR6IN88US=> MXnTRW5ITVJ?
HCC2998 NGTaPI5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml2xTWM2OD12OD62NlM3KM7:TR?= NETGPXlUSU6JRWK=
J82 NXewVI9pT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUTJR|UxRTR6LkeyOFIh|ryP NYD0NYNPW0GQR1XS
ML-2 M3z4V2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NI\IRolKSzVyPUS5MlQ3ODVizszN NIDnVFdUSU6JRWK=
NCI-H2030 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGLRS|lKSzVyPUS5MlcyOTdizszN NIL0TlRUSU6JRWK=
NCI-H1792 M4TFUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWnIRmU1UUN3ME20PU45PTF6IN88US=> NH;FVG5USU6JRWK=

... 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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