Nilotinib (AMN-107) 化学構造
分子量: 529.52

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Quality Control & MSDS

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 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWXmS4FsUUN3ME2wMlAxODF2NDFOwG0> M1nUW3NCVkeHUh?=
KU812 NH75UpRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGXw[45KSzVyPUCuNFAzPDhizszN NF3HPJdUSU6JRWK=
EM-2 M{\pbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoP0TWM2OD1yLkCwOFEh|ryP NWHLc|hHW0GQR1XS
LAMA-84 MnTkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVrvSm5zUUN3ME2wMlAxPDlizszN MYXTRW5ITVJ?
MEG-01 NFzYZolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2DCdWlEPTB;MD6wNFgzQCEQvF2= MnjDV2FPT0WU
BV-173 NYPkUoI5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYTJR|UxRTBwMEGwPFkh|ryP MljuV2FPT0WU
KASUMI-1 M4\vSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MluyTWM2OD1yLkCyOFE{KM7:TR?= Mk\2V2FPT0WU
NB7 NYLQSJQxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVPiN4NOUUN3ME2wMlE{PDN7IN88US=> NYPWWJVpW0GQR1XS
BHT-101 NV;NO3ZRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVHJR|UxRTBwNkSyOlMh|ryP MV;TRW5ITVJ?
CGTH-W-1 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2jWbmlEPTB;MD62OFg4KM7:TR?= MX7TRW5ITVJ?
HMV-II MlX6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3XENWlEPTB;MD63OFg4PCEQvF2= Mn7jV2FPT0WU
NKM-1 NX3wVJVqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXrJR|UxRTBwOUCxOUDPxE1? NVi2doMyW0GQR1XS
LB2241-RCC NUnxOHZYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYPJR|UxRTFwMEKyNlgh|ryP NF;SNZVUSU6JRWK=
NCI-H1703 Mnm1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2i2W2lEPTB;MT6xPFg4KM7:TR?= NXX5flNyW0GQR1XS
BE-13 NHfsTo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3jZVmlEPTB;MT6yO|QyPiEQvF2= NWD6WFZyW0GQR1XS
ACN NGHvc4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkP4TWM2OD1zLkW1NFc4KM7:TR?= MmDiV2FPT0WU
A204 MoezS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3LVV2lEPTB;MT61O|IxPSEQvF2= M3rmWHNCVkeHUh?=
HOP-62 M{XpNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVix[VZFUUN3ME2xMlgzODd5IN88US=> M13XcnNCVkeHUh?=
H9 M3vycWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4jRdmlEPTB;Mj63N|c6OyEQvF2= NFXZSpJUSU6JRWK=
HCC1806 MljpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFzJWHZKSzVyPUKuO|Q{OjdizszN NXLGRnRWW0GQR1XS
NOS-1 NXPSNXpsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX;JR|UxRTJwOEexNFIh|ryP NWSyVXo1W0GQR1XS
RS4-11 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV\KRYZ3UUN3ME2yMlkxPjJ|IN88US=> MkTHV2FPT0WU
JAR M4\qNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXjU[5Q5UUN3ME2yMlkzODh2IN88US=> MU\TRW5ITVJ?
T98G MlSyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV\JR|UxRTNwMEGzNVMh|ryP NXTsU2kzW0GQR1XS
NCI-SNU-1 M2X4UWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoLrTWM2OD1|LkSwNFkzKM7:TR?= MWXTRW5ITVJ?
SK-MEL-1 MnPyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV;JR|UxRTNwNEOwNlkh|ryP NUHCVJY{W0GQR1XS
L-363 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoHBTWM2OD1|Lk[xNVA4KM7:TR?= NU\hcGxkW0GQR1XS
SW982 NETBOmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MorLTWM2OD1|Lk[0NVY6KM7:TR?= NEjCS2dUSU6JRWK=
HT-1080 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXXJR|UxRTNwOUG3O|Uh|ryP MY\TRW5ITVJ?
G-402 NW\wNoRPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYLJR|UxRTRwM{GyNFMh|ryP M4P1UHNCVkeHUh?=
HOS NULnUG1PT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV;JR|UxRTRwOECyPFIh|ryP MnT1V2FPT0WU
SK-NEP-1 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4fFdmlEPTB;ND64N|E6OSEQvF2= M2fiVXNCVkeHUh?=
HAL-01 MnrJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYfJR|UxRTRwOEiyOFIh|ryP M{Xjd3NCVkeHUh?=
SBC-1 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWDWdHl1UUN3ME20MlkxQTB5IN88US=> NYLDVpRvW0GQR1XS
CTV-1 NHX5U4JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXHJR|UxRTVwNEi5N|gh|ryP MmKwV2FPT0WU
LCLC-103H M1iySmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH7NNIRKSzVyPUWuO|c1PzFizszN NYj5XHZOW0GQR1XS
RVH-421 NIrhcZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUPJR|UxRTVwN{e1N|Yh|ryP NXTrRpdSW0GQR1XS
K-562 M4C0cWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M37QVWlEPTB;NT65NFM3KM7:TR?= MWjTRW5ITVJ?
CAL-33 NUnBbVJsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH;nPItKSzVyPU[uN|E{PTlizszN MoXQV2FPT0WU
MDA-MB-361 MmrLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYDJR|UxRTZwM{O2PVkh|ryP MYrTRW5ITVJ?
IGROV-1 M3XkcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4L2fWlEPTB;Nj60O|E6OSEQvF2= MnnGV2FPT0WU
NY Ml[4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFTzZXJKSzVyPU[uOVM2QTlizszN NIP3bnhUSU6JRWK=
Ramos-2G6-4C10 MonaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmLUTWM2OD14Lk[2PVMyKM7:TR?= MorsV2FPT0WU
HuO9 NUHUdY96T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUnaVJg4UUN3ME22Mlc{QTZ2IN88US=> NFvVOVdUSU6JRWK=
MS-1 NHv5V4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{PlemlEPTB;Nz6xNVk2OyEQvF2= M{HJcnNCVkeHUh?=
RPMI-8226 M2DjcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnLMTWM2OD15LkK4Nlg4KM7:TR?= M2f4dHNCVkeHUh?=
HDLM-2 M2r3O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoT4TWM2OD15LkSwNVQ6KM7:TR?= NV22cpZCW0GQR1XS
D-566MG MnrsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MknBTWM2OD15LkS3NVU2KM7:TR?= M{XTZ3NCVkeHUh?=
SK-MEL-24 M17UVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHW0[lNKSzVyPUeuOlM{QTJizszN MWDTRW5ITVJ?
COLO-679 NXToTo55T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3q5T2lEPTB;Nz65PFY4OSEQvF2= MXXTRW5ITVJ?
EW-13 NHn1[lRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXzJR|UxRThwM{KwOVQh|ryP NH;xdI1USU6JRWK=
A388 MoHRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVy2UXZRUUN3ME24MlM5PDhzIN88US=> NETSN2NUSU6JRWK=
UM-UC-3 NGDvbYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVfJR|UxRThwNEO5OVYh|ryP MnXlV2FPT0WU
NUGC-3 M2i2cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MULJR|UxRThwNUO1PFIh|ryP MnTJV2FPT0WU
COLO-668 Mn3CS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV3JR|UxRThwNUm0PVEh|ryP Mnm3V2FPT0WU
MOLT-4 NH;Lc2ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX;Gc4tiUUN3ME24MlYzOzV|IN88US=> MkjoV2FPT0WU
D-423MG M3XMUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX23[2JuUUN3ME24Mlg{PzV4IN88US=> NY\vPHBKW0GQR1XS
CTB-1 NFvOe5BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnvqTWM2OD16Lki3NVI5KM7:TR?= MkTWV2FPT0WU
BCPAP MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3ToUGlEPTB;OT6wNlU3OiEQvF2= MV\TRW5ITVJ?
GCT MkHTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHrIdG1KSzVyPUmuNFk5OzFizszN NYezT4pJW0GQR1XS
ACHN M2PHd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWTJR|UxRTlwMkO2N|Ih|ryP NUS4fHRFW0GQR1XS
KYSE-520 NVexNZQ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4[xXmlEPTB;OT6zN|Q5OiEQvF2= MofxV2FPT0WU
LB771-HNC M3flRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1vhemlEPTB;OT63OlQ6PyEQvF2= NFfh[2xUSU6JRWK=
MLMA NFfMV|hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NY[2bYFtUUN3ME2xNE4xOTN{IN88US=> Mn3tV2FPT0WU
HEC-1 M2jF[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFfBOo5KSzVyPUGwMlI5ODRizszN Mn\0V2FPT0WU
HL-60 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUizfnRrUUN3ME2xNE43QDV|IN88US=> NYnzd2VqW0GQR1XS
A101D NYfWO3NXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIfPR|ZKSzVyPUGwMlg6OjNizszN MUPTRW5ITVJ?
A2058 NE\5c|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF7SToVKSzVyPUGwMlkzPDVizszN NFrFb|hUSU6JRWK=
KARPAS-45 M{Dybmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnTpTWM2OD1zMT6wOlM2KM7:TR?= M3HwNHNCVkeHUh?=
697 MnzJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXf1WHdCUUN3ME2xNU4zOTBzIN88US=> MYrTRW5ITVJ?
NCI-N87 NETpeYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHS5U4tKSzVyPUGxMlc4OzFizszN M1v3WHNCVkeHUh?=
DSH1 MmiwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1XlbGlEPTB;MUGuO|k2OyEQvF2= NV7lNlA3W0GQR1XS
HLE MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1[yb2lEPTB;MUGuPFg{QSEQvF2= MmTKV2FPT0WU
NCI-H720 NILD[3lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2D6UGlEPTB;MUKuOlgxOSEQvF2= NUXMbnFPW0GQR1XS
EW-3 NGP3folIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGjjdmFKSzVyPUGyMlk{ODdizszN NFnPTYJUSU6JRWK=
AGS NY[0bI1vT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUX5XGJvUUN3ME2xN{4xOzVzIN88US=> MlXmV2FPT0WU
ES5 NXPpTos2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVHJR|UxRTF|LkC1NVIh|ryP MU\TRW5ITVJ?
DB M17pVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3zMSmlEPTB;MUOuN|I2PiEQvF2= MYLTRW5ITVJ?
A4-Fuk NF3LUmdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2HXSmlEPTB;MUOuOFExOiEQvF2= NW\1bFRDW0GQR1XS
A427 Mkf3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NU\rc3lVUUN3ME2xN{41QTd{IN88US=> MYTTRW5ITVJ?
MN-60 Mm\5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWnJR|UxRTF|LkW4OFMh|ryP MmrrV2FPT0WU
HCC2218 NWO3UnFGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWfkSGVKUUN3ME2xN{42QDV4IN88US=> MVnTRW5ITVJ?
MV-4-11 M1f3VWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NE\qd4RKSzVyPUGzMlgyOzdizszN MX3TRW5ITVJ?
GI-1 NVjnXGZ2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmfZTWM2OD1zND6xNVg1KM7:TR?= MljsV2FPT0WU
JVM-3 M3TtUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NInu[VVKSzVyPUG0MlI3PTZizszN MXTTRW5ITVJ?
NCI-H2029 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWSxS41HUUN3ME2xOE4zPzJ5IN88US=> M1PPS3NCVkeHUh?=
TE-12 MlXPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX\JR|UxRTF2Lk[wOFYh|ryP NEL2N3NUSU6JRWK=
WM-115 M1;afGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2\PdGlEPTB;MUWuOVY5OyEQvF2= NYjKb25bW0GQR1XS
BB65-RCC MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHvrOm9KSzVyPUG2MlAzPDFizszN M1nuVXNCVkeHUh?=
NCI-H1693 NXzUd5BzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEXaR4tKSzVyPUG2MlM5ODJizszN M374ZXNCVkeHUh?=
KARPAS-299 NUTTTVNoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2\PN2lEPTB;MU[uOlIxOyEQvF2= NGHTTFlUSU6JRWK=
UACC-257 MlX4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXixSY93UUN3ME2xO{4xPTh{IN88US=> M3HPd3NCVkeHUh?=
RKO NHjsdoZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYjJR|UxRTF5Lk[0N|Mh|ryP NF7ieo5USU6JRWK=
HT-29 MmLjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVPJR|UxRTF5Lke4PFkh|ryP M4fkcnNCVkeHUh?=
ES7 NIK2PFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUnJR|UxRTF6LkGxNlIh|ryP M3T4XHNCVkeHUh?=
DEL NEDQU4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYSzUFdnUUN3ME2xPE4{OTd{IN88US=> NWm3V2JKW0GQR1XS
BT-549 NF;kb4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH[2VHpKSzVyPUG4MlQxQTJizszN M1nSOnNCVkeHUh?=
NCI-H1755 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVfJR|UxRTF6LkW3NlMh|ryP M2rRXXNCVkeHUh?=
HCE-T NFH6fG1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NG\1[JpKSzVyPUG4Mlg{PDFizszN M1fXOHNCVkeHUh?=
LU-139 NHLp[IFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3:3emlEPTB;MUmuNFQ2QCEQvF2= MVHTRW5ITVJ?
ECC10 NVS3XHF7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkW3TWM2OD1zOT6yOFc2KM7:TR?= MUTTRW5ITVJ?
769-P NHnFUFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1PBZmlEPTB;MUmuOlM{PSEQvF2= M1rnTHNCVkeHUh?=
BALL-1 MmnlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUTvZnJHUUN3ME2xPU43Pzd3IN88US=> NUD2OItOW0GQR1XS
LXF-289 NWjxXmNjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHX5ZWpKSzVyPUG5Mlg6PzlizszN MUXTRW5ITVJ?
TYK-nu NYnYbXNTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1v4cGlEPTB;MUmuPVMyPSEQvF2= M4jMTnNCVkeHUh?=
NCI-H630 M1nFeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1\McGlEPTB;MUmuPVM4QCEQvF2= MVzTRW5ITVJ?
EW-18 MoLoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mlv4TWM2OD1{MD6zPFAzKM7:TR?= MXHTRW5ITVJ?
KYSE-150 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnnvTWM2OD1{MD63NFQ4KM7:TR?= MXXTRW5ITVJ?
LOXIMVI MnPrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3zVZWlEPTB;MkCuO|U5PiEQvF2= NWTIcWw5W0GQR1XS
HuP-T3 Mlr6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoDUTWM2OD1{MT6wPFUzKM7:TR?= MW\TRW5ITVJ?
MFE-280 M2nHUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVnJR|UxRTJzLkW2O|kh|ryP NEWwXoVUSU6JRWK=
SK-OV-3 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M37qSmlEPTB;MkGuPFQxQCEQvF2= NIrTNIVUSU6JRWK=
QIMR-WIL M2X6dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX;JR|UxRTJ{LkC0O|gh|ryP M3KzRnNCVkeHUh?=
NCI-H69 NYfZNnloT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUTJR|UxRTJ{LkSyPVkh|ryP NYj3coZWW0GQR1XS
TE-5 MlTvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXTIeoFMUUN3ME2yNk41QTZ3IN88US=> NWPueph1W0GQR1XS
NCI-H1993 NIK4elVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWrzUXFEUUN3ME2yNk41QTdzIN88US=> NH\zSGJUSU6JRWK=
NCI-H1092 M1SzWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUPJR|UxRTJ|LkK4OFMh|ryP M3TQSnNCVkeHUh?=
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NCI-H1792 M1n6Tmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4S0bWlEPTB;NEmuPFUyQCEQvF2= M3;jRXNCVkeHUh?=

... 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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