Nilotinib (AMN-107) 化学構造
分子量: 529.52

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Quality Control & MSDS

製品説明

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    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 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVnJR|UxRTBwMECwNVQ1KM7:TR?= NITZcWhUSU6JRWK=
KU812 NF\4d5VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnX1TWM2OD1yLkCwNlQ5KM7:TR?= MnfUV2FPT0WU
EM-2 NGfhV3BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmjmTWM2OD1yLkCwOFEh|ryP M3P3WXNCVkeHUh?=
LAMA-84 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV\JR|UxRTBwMEC0PUDPxE1? NUDEbpY2W0GQR1XS
MEG-01 NGizOHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1;PXmlEPTB;MD6wNFgzQCEQvF2= MUPTRW5ITVJ?
BV-173 NEPaVYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlW1TWM2OD1yLkCxNFg6KM7:TR?= MULTRW5ITVJ?
KASUMI-1 NYPGW2FST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NU\lRW1CUUN3ME2wMlAzPDF|IN88US=> MlzWV2FPT0WU
NB7 M1jlcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmnaTWM2OD1yLkGzOFM6KM7:TR?= M4T0UXNCVkeHUh?=
BHT-101 MonVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnTPTWM2OD1yLk[0NlY{KM7:TR?= NWDKempFW0GQR1XS
CGTH-W-1 M{foWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXvn[pRVUUN3ME2wMlY1QDdizszN MULTRW5ITVJ?
HMV-II NIj2SWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWrVcHlXUUN3ME2wMlc1QDd2IN88US=> Ml3SV2FPT0WU
NKM-1 NVLCepc6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF7vZVVKSzVyPUCuPVAyPSEQvF2= NF3G[mFUSU6JRWK=
LB2241-RCC M4H4RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1TqcWlEPTB;MT6wNlIzQCEQvF2= NIS3S5hUSU6JRWK=
NCI-H1703 MmK4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWDRboRsUUN3ME2xMlE5QDdizszN NXvReHlvW0GQR1XS
BE-13 NHfxPHdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXvJR|UxRTFwMke0NVYh|ryP Mnf0V2FPT0WU
ACN NHHIZopIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEHrWWZKSzVyPUGuOVUxPzdizszN NGThZXBUSU6JRWK=
A204 M4jkRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWXJR|UxRTFwNUeyNFUh|ryP NYnnV3pVW0GQR1XS
HOP-62 NUjtPWExT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEHTVJVKSzVyPUGuPFIxPzdizszN MUfTRW5ITVJ?
H9 NXv3NIxET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYfJR|UxRTJwN{O3PVMh|ryP MoDsV2FPT0WU
HCC1806 NHTDXoVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUeyV|RUUUN3ME2yMlc1OzJ5IN88US=> M2LXTnNCVkeHUh?=
NOS-1 NWDPcIFET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NU[xZ2g5UUN3ME2yMlg4OTB{IN88US=> M3y1[HNCVkeHUh?=
RS4-11 NILEU4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmXjTWM2OD1{LkmwOlI{KM7:TR?= MVjTRW5ITVJ?
JAR MlHCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{fpfWlEPTB;Mj65NlA5PCEQvF2= NYLwTmRkW0GQR1XS
T98G MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYHVNHVXUUN3ME2zMlAyOzF|IN88US=> NGrw[W9USU6JRWK=
NCI-SNU-1 NVfUV|VlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{DtcGlEPTB;Mz60NFA6OiEQvF2= M{f2fnNCVkeHUh?=
SK-MEL-1 M{iybmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXvJR|UxRTNwNEOwNlkh|ryP M3\Sb3NCVkeHUh?=
L-363 M16ze2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXXJR|UxRTNwNkGxNFch|ryP M2DPXnNCVkeHUh?=
SW982 NWfa[WJUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYm2SHJxUUN3ME2zMlY1OTZ7IN88US=> Mm\2V2FPT0WU
HT-1080 NHL6VFFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVzJR|UxRTNwOUG3O|Uh|ryP M3OyUXNCVkeHUh?=
G-402 M1uwfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXvJR|UxRTRwM{GyNFMh|ryP MUHTRW5ITVJ?
HOS NGj1W|FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXvJR|UxRTRwOECyPFIh|ryP NET1fnNUSU6JRWK=
SK-NEP-1 M1H1dGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV7JR|UxRTRwOEOxPVEh|ryP MkDtV2FPT0WU
HAL-01 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGXjOWNKSzVyPUSuPFgzPDJizszN M2nteXNCVkeHUh?=
SBC-1 NXjnbZU1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWnNOnJTUUN3ME20MlkxQTB5IN88US=> M1G3THNCVkeHUh?=
CTV-1 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWjZclQ5UUN3ME21MlQ5QTN6IN88US=> MmfIV2FPT0WU
LCLC-103H MorZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmjsTWM2OD13Lke3OFcyKM7:TR?= M{PuPHNCVkeHUh?=
RVH-421 M3e3Omdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoX1TWM2OD13Lke3OVM3KM7:TR?= NFjWPI1USU6JRWK=
K-562 NYPXfJpXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml\5TWM2OD13LkmwN|Yh|ryP M2m5bXNCVkeHUh?=
CAL-33 Ml;iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWS1UVRPUUN3ME22MlMyOzV7IN88US=> M2G1RnNCVkeHUh?=
MDA-MB-361 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYrJR|UxRTZwM{O2PVkh|ryP NIHsSJdUSU6JRWK=
IGROV-1 NUHibWxVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUjafZRGUUN3ME22MlQ4OTlzIN88US=> MX;TRW5ITVJ?
NY NXnCb2xxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUPJR|UxRTZwNUO1PVkh|ryP NEX2VHJUSU6JRWK=
Ramos-2G6-4C10 NHvuXHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlLETWM2OD14Lk[2PVMyKM7:TR?= Mn75V2FPT0WU
HuO9 MlWwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1m5XWlEPTB;Nj63N|k3PCEQvF2= M3zlPHNCVkeHUh?=
MS-1 MoLDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlzlTWM2OD15LkGxPVU{KM7:TR?= M2W3T3NCVkeHUh?=
RPMI-8226 MljJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4LENWlEPTB;Nz6yPFI5PyEQvF2= MkS4V2FPT0WU
HDLM-2 M3LNSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHvSR3lKSzVyPUeuOFAyPDlizszN M1nhZnNCVkeHUh?=
D-566MG M4LQVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmH6TWM2OD15LkS3NVU2KM7:TR?= NIPBPHZUSU6JRWK=
SK-MEL-24 M{XzWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mmj0TWM2OD15Lk[zN|kzKM7:TR?= MYjTRW5ITVJ?
COLO-679 Mof0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHLvUmNKSzVyPUeuPVg3PzFizszN MWjTRW5ITVJ?
EW-13 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWi3cFVwUUN3ME24MlMzODV2IN88US=> M3PvUXNCVkeHUh?=
A388 M3zFNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV3JR|UxRThwM{i0PFEh|ryP Ml7qV2FPT0WU
UM-UC-3 NHfIeWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NULwTGJvUUN3ME24MlQ{QTV4IN88US=> M2\CPXNCVkeHUh?=
NUGC-3 NGnFW5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUPJR|UxRThwNUO1PFIh|ryP M4jCbHNCVkeHUh?=
COLO-668 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkfTTWM2OD16LkW5OFkyKM7:TR?= NWT2UnRUW0GQR1XS
MOLT-4 MlP5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX7SOYVEUUN3ME24MlYzOzV|IN88US=> NH21WG9USU6JRWK=
D-423MG NGnCOlRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnG5TWM2OD16LkizO|U3KM7:TR?= M33je3NCVkeHUh?=
CTB-1 M2HVeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIPKNWNKSzVyPUiuPFcyOjhizszN MnjyV2FPT0WU
BCPAP MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFfJblhKSzVyPUmuNFI2PjJizszN MXnTRW5ITVJ?
GCT MkHnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFjqXFVKSzVyPUmuNFk5OzFizszN M2\XOHNCVkeHUh?=
ACHN M2H3eGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoXpTWM2OD17LkKzOlMzKM7:TR?= MUDTRW5ITVJ?
KYSE-520 NYXMOW9xT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3G2V2lEPTB;OT6zN|Q5OiEQvF2= MWjTRW5ITVJ?
LB771-HNC NF23e4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWXJR|UxRTlwN{[0PVch|ryP NF71WJlUSU6JRWK=
MLMA MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGrNfVlKSzVyPUGwMlAyOzJizszN NWTENFBEW0GQR1XS
HEC-1 NXfKWnR5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVf3cJN7UUN3ME2xNE4zQDB2IN88US=> NHHTVGdUSU6JRWK=
HL-60 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX\JR|UxRTFyLk[4OVMh|ryP MUfTRW5ITVJ?
A101D NHvHZXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYDJR|UxRTFyLki5NlMh|ryP Ml;xV2FPT0WU
A2058 NHvMTJVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnnBTWM2OD1zMD65NlQ2KM7:TR?= NVvsTmNUW0GQR1XS
KARPAS-45 NE\3[ohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUDJR|UxRTFzLkC2N|Uh|ryP M3;6Z3NCVkeHUh?=
697 M{HnfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NES4Z4ZKSzVyPUGxMlIyODFizszN Mlq0V2FPT0WU
NCI-N87 NF3xemlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEfLS5hKSzVyPUGxMlc4OzFizszN NELvd3ZUSU6JRWK=
DSH1 NGT5cI5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1TBXmlEPTB;MUGuO|k2OyEQvF2= MX\TRW5ITVJ?
HLE NXTZV|JZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3L5RWlEPTB;MUGuPFg{QSEQvF2= MYfTRW5ITVJ?
NCI-H720 MkXaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX\zR|RQUUN3ME2xNk43QDBzIN88US=> MkLCV2FPT0WU
EW-3 MnzVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYrRVnNkUUN3ME2xNk46OzB5IN88US=> M4XN[3NCVkeHUh?=
AGS NYXkbWo6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnTiTWM2OD1zMz6wN|UyKM7:TR?= NFexbm9USU6JRWK=
ES5 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn74TWM2OD1zMz6wOVEzKM7:TR?= M3\5fXNCVkeHUh?=
DB NFHhT29Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVnobHJHUUN3ME2xN{4{OjV4IN88US=> NFnZ[lRUSU6JRWK=
A4-Fuk MkHWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYrJR|UxRTF|LkSxNFIh|ryP MnTzV2FPT0WU
A427 NILMRY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUDESHBUUUN3ME2xN{41QTd{IN88US=> M1jRV3NCVkeHUh?=
MN-60 NGHRZndIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3nSRWlEPTB;MUOuOVg1OyEQvF2= NUHBOFFRW0GQR1XS
HCC2218 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnTwTWM2OD1zMz61PFU3KM7:TR?= NUDhZm57W0GQR1XS
MV-4-11 MlrjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVHJR|UxRTF|LkixN|ch|ryP NVHa[IhCW0GQR1XS
GI-1 NHHqRZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MULJR|UxRTF2LkGxPFQh|ryP M{\0XnNCVkeHUh?=
JVM-3 NXi1[phbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1vve2lEPTB;MUSuNlY2PiEQvF2= NYHXNWpoW0GQR1XS
NCI-H2029 NGD3VIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2r5[2lEPTB;MUSuNlczPyEQvF2= NWf5OYVNW0GQR1XS
TE-12 Mke0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnPwTWM2OD1zND62NFQ3KM7:TR?= NGjWZY1USU6JRWK=
WM-115 NVGxWppMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVz5b2trUUN3ME2xOU42Pjh|IN88US=> MYPTRW5ITVJ?
BB65-RCC M3jDbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYC2fY5bUUN3ME2xOk4xOjRzIN88US=> NYqySJhNW0GQR1XS
NCI-H1693 NFnMSVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWfJR|UxRTF4LkO4NFIh|ryP M2HPZ3NCVkeHUh?=
KARPAS-299 MoLES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4rDSGlEPTB;MU[uOlIxOyEQvF2= NH7DeYVUSU6JRWK=
UACC-257 NVr5TnZkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmfuTWM2OD1zNz6wOVgzKM7:TR?= NXnDV|d3W0GQR1XS
RKO NFn3UJJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWjJR|UxRTF5Lk[0N|Mh|ryP MmKwV2FPT0WU
HT-29 M1POTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3m1VWlEPTB;MUeuO|g5QSEQvF2= NYjzS29TW0GQR1XS
ES7 NIG5U4JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX;JR|UxRTF6LkGxNlIh|ryP MmX0V2FPT0WU
DEL NFeyWnBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX;JR|UxRTF6LkOxO|Ih|ryP MVrTRW5ITVJ?
BT-549 NITwXnRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mo\RTWM2OD1zOD60NFkzKM7:TR?= MkD2V2FPT0WU
NCI-H1755 NHnGNIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlOzTWM2OD1zOD61O|I{KM7:TR?= MXTTRW5ITVJ?
HCE-T Mmn2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH3xeYFKSzVyPUG4Mlg{PDFizszN MnrHV2FPT0WU
LU-139 NFTaU2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml;tTWM2OD1zOT6wOFU5KM7:TR?= M33xO3NCVkeHUh?=
ECC10 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MorWTWM2OD1zOT6yOFc2KM7:TR?= M1HKZ3NCVkeHUh?=
769-P MlTNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmfZTWM2OD1zOT62N|M2KM7:TR?= NWDEUmNEW0GQR1XS
BALL-1 M2j6bWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYnEToJzUUN3ME2xPU43Pzd3IN88US=> M2X6RXNCVkeHUh?=
LXF-289 NGTzOW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmHXTWM2OD1zOT64PVc6KM7:TR?= NEfkUYdUSU6JRWK=
TYK-nu MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYLJXVVbUUN3ME2xPU46OzF3IN88US=> NYPyb|B5W0GQR1XS
NCI-H630 MlvkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFnNZpBKSzVyPUG5Mlk{PzhizszN NYHOXZlzW0GQR1XS
EW-18 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MU\JR|UxRTJyLkO4NFIh|ryP Mmn3V2FPT0WU
KYSE-150 NXrzeXJTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX;Xe4Z4UUN3ME2yNE44ODR5IN88US=> NF3GU29USU6JRWK=
LOXIMVI MlHiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX3JR|UxRTJyLke1PFYh|ryP MoHYV2FPT0WU
HuP-T3 M1LUZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUDJR|UxRTJzLkC4OVIh|ryP M2nU[XNCVkeHUh?=
MFE-280 M3vGUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIH4[4VKSzVyPUKxMlU3PzlizszN NYTPbmJqW0GQR1XS
SK-OV-3 NV2wb|NmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFSzOWxKSzVyPUKxMlg1ODhizszN M4DoZXNCVkeHUh?=
QIMR-WIL MnXIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIfZd4VKSzVyPUKyMlA1PzhizszN NFXab45USU6JRWK=
NCI-H69 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV\6d|RUUUN3ME2yNk41Ojl7IN88US=> NHX6NWZUSU6JRWK=
TE-5 MmrrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXjnXFhpUUN3ME2yNk41QTZ3IN88US=> MkjFV2FPT0WU
NCI-H1993 Mo\3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXf3[5JXUUN3ME2yNk41QTdzIN88US=> Mm\HV2FPT0WU
NCI-H1092 NYSybnByT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX7EW|JMUUN3ME2yN{4zQDR|IN88US=> MlK3V2FPT0WU
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NCI-H1666 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXjJR|UxRTN3LkiyOVMh|ryP MoLEV2FPT0WU
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SJRH30 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnjTTWM2OD1|OD63N|QyKM7:TR?= NYWzemxnW0GQR1XS
GP5d MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3j6S2lEPTB;M{iuPFY2OyEQvF2= M3L2O3NCVkeHUh?=
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COLO-800 M374fmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH:1WIRKSzVyPUO5MlM3OzhizszN Mn[0V2FPT0WU
RD MljWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2L4emlEPTB;M{muOVI2QCEQvF2= M2m0TnNCVkeHUh?=
NCI-SNU-5 MofZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoTZTWM2OD1|OT62PVE3KM7:TR?= NGPGdmJUSU6JRWK=
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SK-MEL-3 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYrJR|UxRTRyLkW5N|Ih|ryP NFfOZoFUSU6JRWK=
SK-MEL-28 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MofJTWM2OD12MD62OFM2KM7:TR?= MkPkV2FPT0WU
SCC-4 M2rQUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVjJR|UxRTRzLkKxN|ch|ryP M1;hUnNCVkeHUh?=
no-11 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGrhUWFKSzVyPUSxMlc{PTRizszN M1vh[nNCVkeHUh?=
HT-144 NEDGVppIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnSzTWM2OD12Mj6wOVY4KM7:TR?= NYjZW4V{W0GQR1XS
MFM-223 M4fBNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXS1NIJpUUN3ME20Nk41ODJizszN NFz3cHdUSU6JRWK=
ONS-76 NXnLWm4{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3PBWGlEPTB;NEKuPFAyQCEQvF2= M3fuSXNCVkeHUh?=
ES8 NHrmTmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX;iSXJzUUN3ME20N{4{Pjl6IN88US=> M3;LOXNCVkeHUh?=
T-24 M17mWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1[xXmlEPTB;NEOuOFM3QSEQvF2= NHv3dG5USU6JRWK=
GAMG M37RT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlXuTWM2OD12Mz60OVE4KM7:TR?= NGHQT49USU6JRWK=
LU-135 MkSzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGDKNIJKSzVyPUS0MlA6OjNizszN M{fuU3NCVkeHUh?=
HCC1187 NVntNoczT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1nMemlEPTB;NESuPFI3OiEQvF2= MVHTRW5ITVJ?
TE-1 NFjIbnFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MknWTWM2OD12NT6xOlU1KM7:TR?= M2f4bHNCVkeHUh?=
J-RT3-T3-5 M1rxXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUnJR|UxRTR3LkSzNVUh|ryP MX;TRW5ITVJ?
GI-ME-N M3W5U2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn;tTWM2OD12NT64PVUzKM7:TR?= M4HJR3NCVkeHUh?=
D-392MG MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlnITWM2OD12NT65NlU3KM7:TR?= M{XlbHNCVkeHUh?=
KALS-1 MlS5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHy0TGxKSzVyPUS2MlczPTdizszN NXjYRYJEW0GQR1XS
MMAC-SF MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1i5UGlEPTB;NE[uPVk2OiEQvF2= MmrhV2FPT0WU
HSC-3 MoHnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV7JR|UxRTR5LkO2NFgh|ryP M4TTe3NCVkeHUh?=
KM-H2 NIPzUHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVHJR|UxRTR5Lk[wNFch|ryP MVvTRW5ITVJ?
LoVo NXTmb5RLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXrJR|UxRTR6LkGwNFIh|ryP Mn\KV2FPT0WU
NCI-H510A MkfLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkHsTWM2OD12OD6xPFcyKM7:TR?= NXi5eJpTW0GQR1XS
EW-11 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2DRSWlEPTB;NEiuNlM1QCEQvF2= NVHie4RsW0GQR1XS
HCC2998 M3nLVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYrJR|UxRTR6Lk[yN|Yh|ryP MoG4V2FPT0WU
J82 M1j1emdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWfJR|UxRTR6LkeyOFIh|ryP MnnnV2FPT0WU
ML-2 NF3SO5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXXCblRxUUN3ME20PU41PjB3IN88US=> NVrjeGtlW0GQR1XS
NCI-H2030 NUL0XWpkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVLJR|UxRTR7LkexNVch|ryP NFHuS5BUSU6JRWK=
NCI-H1792 MljDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWHJR|UxRTR7Lki1NVgh|ryP MUnTRW5ITVJ?

... 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 2年-20℃
6月-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 27 mg/mL (50.98 mM)
<1 mg/mL (<1 mM)
エタノール <1 mg/mL (<1 mM)
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

カスタマーフィードバック (5)


Click to enlarge
Rating
Source FASEB J , 2011, 25, 3661-3673. Nilotinib (AMN-107) purchased from Selleck
Method Analyzing cell apoptosis
Cell Lines Ba/F3-p210T315I cells
Concentrations 0-5 μM
Incubation Time 24 h
Results In a parallel study using imatinib/PDMP or nilotinib/PDMP combinations, to our surprise, similar significant synergy in Ba/F3-p210T315I cells was observed.

Click to enlarge
Rating
Source Molecules, 2014, 19, 3356-75. Nilotinib (AMN-107) purchased from Selleck
Method Western blot
Cell Lines K562, CD34+CD38- cells
Concentrations 0, 0.01, 0.1, 1 uM
Incubation Time 12 h
Results Since nilotinib targets the Bcr-Abl kinase in CML cells, we evaluated its ability to inhibit kinase activity in ABCB1- and ABCG2-overexpressing CD34+CD38- cells. In K562 cells, nilotinib effectively inhibited the phosphorylation of Bcr-Abl and CrkL (a surrogate marker of Bcr-Abl activity) at a concentration of 0.1 umol/L. However, in CD34+CD38- cells, nilotinib failed to completely inhibit the phosphorylation of Bcr-Abl and CrkL even when cells were exposed to concentration up to 1.0 umol/L.

Click to enlarge
Rating
Source Leukemia Res, 2012, 36, 1311-1314. Nilotinib (AMN-107) purchased from Selleck
Method Thymidine uptake Uptake assay
Cell Lines K562, MEG-01 cells
Concentrations 0.1-10uM
Incubation Time 20 min
Results Nilotinib was much more potent than imatinib to inhibit nucleoside transport. It prevented the uptake of thymidine in K562 cells by 97% at 10 uM, a level that was similar to the one obtained with the vasodilatator molecule dipyridamole. Nilotinib was also very efficient at 1 and 0.1 uM; it blocked the entry of thymidine by 90 and 74%, respectively (Fig. 2a). With the MEG-01 cell line, nilotinib was also extremely potent and blocked the entry of thymidine by 96, 92 and 60% with 10, 1 and 0.1 uM nilotinib, respectively (Fig. 2b).

Click to enlarge
Rating
Source Urol Oncol, 2014, 0.1016/j.urolonc.2014.06.001. Nilotinib (AMN-107) purchased from Selleck
Method Immunoblot analyses
Cell Lines LNCaP, PC-3, DU-145 cells
Concentrations 10 uM
Incubation Time 24 h
Results It shows a robust overexpression of phospho-ERK1/2 T202/Y204 in nilotinib-treated DU-145 cells (B). An up-regulation of phospho-ERK1/2 T202/Y204 was also detectable in nilotinib-treated LNCaP cells, albeit at a lower level, and was not found in PC-3 cells (C).

Click to enlarge
Rating
Source Urol Oncol, 2014, 0.1016/j.urolonc.2014.06.001. Nilotinib (AMN-107) purchased from Selleck
Method Immunohistochemical staining
Cell Lines Xenografted DU-145 cells
Concentrations 5 mg/kg/d
Incubation Time 21 days
Results Accoding to published animals experiments, DU-145 xenografts from a representative experiment in which nilotinib was used at a 75-mg/kg/d concentration. It's found a significant increase of phospho-ERK-positive residual tumor cells from a mean of 67.5 cells per high-powerfield in controls to 131.1 cells per high-powerfield in DU-145 xenografts treated for 21 days with nilotinib (P< 0.0005).

文献中の引用 (18)

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Related Bcr-Abl 阻害剤

  • PX-478 2HCl

    PX-478 2HCl is an orally active, and selective hypoxia-inducible factor-1α (HIF-1α) inhibitor. Phase 1.

  • Defactinib (VS-6063, PF-04554878)

    Defactinib (VS-6063, PF-04554878) is a selective, and orally active FAK inhibitor. Phase 2.

  • SU6656

    SU 6656 is a selective Src family kinase inhibitor with IC50 of 280 nM, 20 nM, 130 nM, and 170 nM for Src, Yes, Lyn, and Fyn, respectively.

  • Dasatinib Monohydrate

    Dasatinib Monohydrate is a novel, potent and multi-targeted inhibitor that targets Abl, Src and c-Kit, with IC50 of <1 nM, 0.8 nM and 79 nM, respectively.

  • Imatinib Mesylate (STI571)

    Imatinib Mesylate (STI571) は口でImatinibの生物学的利用能メシラート塩です。そして、それは v-Ablc-KitPDGFRのマルチターゲット阻害剤で、IC50 がそれぞれ 0.6 μM、 0.1 μM、 0.1 μMです。

  • Ponatinib (AP24534)

    Ponatinib (AP24534) は、PI3KγとPI4KIIIβの新しくて強力な阻害剤で、IC50 がそれぞれ16 nM と 19 nMになる。

  • Bafetinib (INNO-406)

    Bafetinib(INNO-406)は、5.8nMと19nMのIC50による強力で選択的な二重Bcr-Abl/リン・チロシン・キナーゼ阻害剤です

    Features:Dual Bcr-Abl/Lyn inhibitor.

  • Degrasyn (WP1130)

    Degrasyn (WP1130)は、選択的な非ユビキチンアーゼ(DUB)阻害剤です。WP1130は、5人のダブズを妨げます:USP5、UCH-L1、USP9x、USP14とUCH37。

    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、Abl1とT315I Abl1の構造的な支配阻害剤で、IC50 がそれぞれ 0.8 nM と 4 nMです。

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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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