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 NY\hdlVjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHnoTpRKSzVyPUCuNFAxOTR2IN88US=> NHvIVYFUSU6JRWK=
KU812 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHfsToFKSzVyPUCuNFAzPDhizszN NF7YeIpUSU6JRWK=
EM-2 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYPoRYdTUUN3ME2wMlAxPDFizszN NGOxcmhUSU6JRWK=
LAMA-84 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkjETWM2OD1yLkCwOFkh|ryP NWfBcIs2W0GQR1XS
MEG-01 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEDo[otKSzVyPUCuNFA5OjhizszN MnPzV2FPT0WU
BV-173 MoLZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlLwTWM2OD1yLkCxNFg6KM7:TR?= MlfxV2FPT0WU
KASUMI-1 NVLYNWFVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFn3PGVKSzVyPUCuNFI1OTNizszN NWLvdZRtW0GQR1XS
NB7 M4\EOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVvJR|UxRTBwMUO0N|kh|ryP NVn6b2lHW0GQR1XS
BHT-101 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmLMTWM2OD1yLk[0NlY{KM7:TR?= MnW0V2FPT0WU
CGTH-W-1 NF7CbJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmHWTWM2OD1yLk[0PFch|ryP MWjTRW5ITVJ?
HMV-II M1v2cGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHmze|lKSzVyPUCuO|Q5PzRizszN M{joXXNCVkeHUh?=
NKM-1 M3zOUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUPobnJKUUN3ME2wMlkxOTVizszN NHPuenpUSU6JRWK=
LB2241-RCC MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXzJR|UxRTFwMEKyNlgh|ryP M17EVHNCVkeHUh?=
NCI-H1703 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmnxTWM2OD1zLkG4PFch|ryP M3LtWnNCVkeHUh?=
BE-13 NIjXOIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{fsdWlEPTB;MT6yO|QyPiEQvF2= MV;TRW5ITVJ?
ACN NI\ZOFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVPzTJIxUUN3ME2xMlU2ODd5IN88US=> M3nNUnNCVkeHUh?=
A204 NWXlVJF1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYTJWW83UUN3ME2xMlU4OjB3IN88US=> NY[yXYxnW0GQR1XS
HOP-62 NXf3UpZqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoHWTWM2OD1zLkiyNFc4KM7:TR?= MmrSV2FPT0WU
H9 M4HGSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mon1TWM2OD1{LkezO|k{KM7:TR?= MlvLV2FPT0WU
HCC1806 M2\FW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml;PTWM2OD1{Lke0N|I4KM7:TR?= M2jDenNCVkeHUh?=
NOS-1 MoDvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NID5[pVKSzVyPUKuPFcyODJizszN MmDtV2FPT0WU
RS4-11 M4LFPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWPHTWFyUUN3ME2yMlkxPjJ|IN88US=> M{P4XnNCVkeHUh?=
JAR M{PQWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEnJW3RKSzVyPUKuPVIxQDRizszN MVXTRW5ITVJ?
T98G M1r3Wmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWrmd3dzUUN3ME2zMlAyOzF|IN88US=> NHjBUm1USU6JRWK=
NCI-SNU-1 M1G1NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NULzdmZbUUN3ME2zMlQxODl{IN88US=> Mo[yV2FPT0WU
SK-MEL-1 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlnXTWM2OD1|LkSzNFI6KM7:TR?= MnH0V2FPT0WU
L-363 M4P6b2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGH2SmFKSzVyPUOuOlEyODdizszN M3;rN3NCVkeHUh?=
SW982 M1XTcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3nremlEPTB;Mz62OFE3QSEQvF2= NWHDSHVmW0GQR1XS
HT-1080 M{CyPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{LYOWlEPTB;Mz65NVc4PSEQvF2= MlW4V2FPT0WU
G-402 NFvhUoZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NI\zV4JKSzVyPUSuN|EzODNizszN NI\FSJVUSU6JRWK=
HOS M4nUbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmLPTWM2OD12LkiwNlgzKM7:TR?= MmPYV2FPT0WU
SK-NEP-1 NX;VN2xVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXP2cWo2UUN3ME20Mlg{OTlzIN88US=> MlW3V2FPT0WU
HAL-01 NIq4PWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{DvS2lEPTB;ND64PFI1OiEQvF2= MWDTRW5ITVJ?
SBC-1 NVf2XGJET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVHnWphGUUN3ME20MlkxQTB5IN88US=> MnrTV2FPT0WU
CTV-1 NEnwfHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXjmS5lXUUN3ME21MlQ5QTN6IN88US=> NXi4R2xSW0GQR1XS
LCLC-103H M1PuNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIHTVYRKSzVyPUWuO|c1PzFizszN NUCzeo54W0GQR1XS
RVH-421 Moe5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXzJR|UxRTVwN{e1N|Yh|ryP MlXLV2FPT0WU
K-562 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX3JR|UxRTVwOUCzOkDPxE1? M17UOXNCVkeHUh?=
CAL-33 NFrIcoRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmKxTWM2OD14LkOxN|U6KM7:TR?= NYnzfVN6W0GQR1XS
MDA-MB-361 NUHFWoY2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2rwc2lEPTB;Nj6zN|Y6QSEQvF2= M{XxenNCVkeHUh?=
IGROV-1 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mni2TWM2OD14LkS3NVkyKM7:TR?= Mm\5V2FPT0WU
NY MljYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHfW[oxKSzVyPU[uOVM2QTlizszN M2DjNnNCVkeHUh?=
Ramos-2G6-4C10 NXLDTHU2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYrETpJyUUN3ME22MlY3QTNzIN88US=> MmToV2FPT0WU
HuO9 MlHGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{PkRmlEPTB;Nj63N|k3PCEQvF2= MVvTRW5ITVJ?
MS-1 NUHjR4pOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUPJR|UxRTdwMUG5OVMh|ryP M2jhe3NCVkeHUh?=
RPMI-8226 NHjrfoVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFLBUGlKSzVyPUeuNlgzQDdizszN MX;TRW5ITVJ?
HDLM-2 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn7CTWM2OD15LkSwNVQ6KM7:TR?= M37qTXNCVkeHUh?=
D-566MG NXPSXoxZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnLlTWM2OD15LkS3NVU2KM7:TR?= NXPHVYNJW0GQR1XS
SK-MEL-24 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX3CfFJsUUN3ME23MlY{Ozl{IN88US=> NFfDWo5USU6JRWK=
COLO-679 M2TDSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYeyOFh7UUN3ME23Mlk5PjdzIN88US=> MXzTRW5ITVJ?
EW-13 Ml;OS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlzlTWM2OD16LkOyNFU1KM7:TR?= NVrXeHBQW0GQR1XS
A388 NVrHNHlkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVzJR|UxRThwM{i0PFEh|ryP MX\TRW5ITVJ?
UM-UC-3 MlPnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHu2UJNKSzVyPUiuOFM6PTZizszN MlX3V2FPT0WU
NUGC-3 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NInpSmhKSzVyPUiuOVM2QDJizszN NYPV[2w1W0GQR1XS
COLO-668 M{ewV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlzhTWM2OD16LkW5OFkyKM7:TR?= M3jJbnNCVkeHUh?=
MOLT-4 MnXtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2rVbmlEPTB;OD62NlM2OyEQvF2= NIjMd2RUSU6JRWK=
D-423MG NVLHUGh3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVrJR|UxRThwOEO3OVYh|ryP NV\zTJFHW0GQR1XS
CTB-1 NH3pdFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXzze4wyUUN3ME24Mlg4OTJ6IN88US=> MnvMV2FPT0WU
BCPAP NUfzXmlET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmXKTWM2OD17LkCyOVYzKM7:TR?= M3rvR3NCVkeHUh?=
GCT NWnRWGRMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3f3PGlEPTB;OT6wPVg{OSEQvF2= MUDTRW5ITVJ?
ACHN NXrWUndYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn3uTWM2OD17LkKzOlMzKM7:TR?= MXrTRW5ITVJ?
KYSE-520 M{Pldmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlfNTWM2OD17LkOzOFgzKM7:TR?= NFPQenVUSU6JRWK=
LB771-HNC MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFK3VHJKSzVyPUmuO|Y1QTdizszN NXrDb2V1W0GQR1XS
MLMA M{\VbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXy0NGtDUUN3ME2xNE4xOTN{IN88US=> NYfiWWw4W0GQR1XS
HEC-1 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVzIRpVjUUN3ME2xNE4zQDB2IN88US=> MUPTRW5ITVJ?
HL-60 M3HBOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3;V[mlEPTB;MUCuOlg2OyEQvF2= NFjQXoZUSU6JRWK=
A101D MmXyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXLJR|UxRTFyLki5NlMh|ryP NWToc5FXW0GQR1XS
A2058 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVzrOodwUUN3ME2xNE46OjR3IN88US=> M2DDeHNCVkeHUh?=
KARPAS-45 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVnOWFVkUUN3ME2xNU4xPjN3IN88US=> NE\VTY1USU6JRWK=
697 NFPTbmNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2\CWGlEPTB;MUGuNlExOSEQvF2= M3TTbXNCVkeHUh?=
NCI-N87 NVr3XVZPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MULJR|UxRTFzLke3N|Eh|ryP MYDTRW5ITVJ?
DSH1 M4XhUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlLsTWM2OD1zMT63PVU{KM7:TR?= NETBd45USU6JRWK=
HLE NYnY[IFFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUPJR|UxRTFzLki4N|kh|ryP M3TM[HNCVkeHUh?=
NCI-H720 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVLlOWxmUUN3ME2xNk43QDBzIN88US=> MVXTRW5ITVJ?
EW-3 MlHZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3TWPWlEPTB;MUKuPVMxPyEQvF2= MV\TRW5ITVJ?
AGS NFjHOppIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX;JR|UxRTF|LkCzOVEh|ryP NXPnWJdJW0GQR1XS
ES5 NWO2[FVrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4m4TWlEPTB;MUOuNFUyOiEQvF2= NYjCdWNKW0GQR1XS
DB NETORYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFz5S|FKSzVyPUGzMlMzPTZizszN NVfvdWdqW0GQR1XS
A4-Fuk MlzjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVXQN5pWUUN3ME2xN{41OTB{IN88US=> MmL1V2FPT0WU
A427 NIrBT5BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV;JR|UxRTF|LkS5O|Ih|ryP NULVfoNTW0GQR1XS
MN-60 NEHU[2RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1ntd2lEPTB;MUOuOVg1OyEQvF2= MV7TRW5ITVJ?
HCC2218 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYjqU2o2UUN3ME2xN{42QDV4IN88US=> M1fH[3NCVkeHUh?=
MV-4-11 NYjx[IoxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3zq[WlEPTB;MUOuPFE{PyEQvF2= NVrZc2RlW0GQR1XS
GI-1 NFfwSppIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHO2NWdKSzVyPUG0MlEyQDRizszN NIe5UphUSU6JRWK=
JVM-3 M3KzTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV3JR|UxRTF2LkK2OVYh|ryP MWLTRW5ITVJ?
NCI-H2029 Mnj0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXjJR|UxRTF2LkK3Nlch|ryP MUnTRW5ITVJ?
TE-12 M{nXXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{\tNGlEPTB;MUSuOlA1PiEQvF2= M3PQRnNCVkeHUh?=
WM-115 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH70fHlKSzVyPUG1MlU3QDNizszN MmjrV2FPT0WU
BB65-RCC Mk\HS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIXlW3lKSzVyPUG2MlAzPDFizszN Mon6V2FPT0WU
NCI-H1693 MnvNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnrBTWM2OD1zNj6zPFAzKM7:TR?= NIe0PIFUSU6JRWK=
KARPAS-299 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUPJR|UxRTF4Lk[yNFMh|ryP Mn;nV2FPT0WU
UACC-257 M3H0SGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV7JR|UxRTF5LkC1PFIh|ryP MWHTRW5ITVJ?
RKO NWLye|BtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVXJR|UxRTF5Lk[0N|Mh|ryP M2D0TXNCVkeHUh?=
HT-29 Mon0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlzCTWM2OD1zNz63PFg6KM7:TR?= MYXTRW5ITVJ?
ES7 MoDHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NE\s[HdKSzVyPUG4MlEyOjJizszN NHznSFBUSU6JRWK=
DEL M1XvS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{nneGlEPTB;MUiuN|E4OiEQvF2= M1LzZ3NCVkeHUh?=
BT-549 M2HRbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUDNdldrUUN3ME2xPE41ODl{IN88US=> MX\TRW5ITVJ?
NCI-H1755 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFTzXXBKSzVyPUG4MlU4OjNizszN NF\4eXVUSU6JRWK=
HCE-T NGDucoxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXPJR|UxRTF6LkizOFEh|ryP M2n2[nNCVkeHUh?=
LU-139 NEKzT5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHew[ZZKSzVyPUG5MlA1PThizszN MYfTRW5ITVJ?
ECC10 M{\MNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUXJR|UxRTF7LkK0O|Uh|ryP MnfVV2FPT0WU
769-P MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MonvTWM2OD1zOT62N|M2KM7:TR?= Ml3CV2FPT0WU
BALL-1 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmHUTWM2OD1zOT62O|c2KM7:TR?= M4DTZnNCVkeHUh?=
LXF-289 NEfyboxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUfySm5VUUN3ME2xPU45QTd7IN88US=> M1fOVHNCVkeHUh?=
TYK-nu MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NULYNIlFUUN3ME2xPU46OzF3IN88US=> NX74T3dRW0GQR1XS
NCI-H630 NX\X[nNNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnLETWM2OD1zOT65N|c5KM7:TR?= NEjTc4dUSU6JRWK=
EW-18 NF;zfWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmLHTWM2OD1{MD6zPFAzKM7:TR?= NF3aRVRUSU6JRWK=
KYSE-150 NILCTpVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4LU[GlEPTB;MkCuO|A1PyEQvF2= MmG0V2FPT0WU
LOXIMVI M1HpdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGi3XXpKSzVyPUKwMlc2QDZizszN MYjTRW5ITVJ?
HuP-T3 NU\xSJpnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVrJR|UxRTJzLkC4OVIh|ryP MXjTRW5ITVJ?
MFE-280 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{G1emlEPTB;MkGuOVY4QSEQvF2= NX;ZcJAyW0GQR1XS
SK-OV-3 NXLtTIp[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWrqWnV5UUN3ME2yNU45PDB6IN88US=> NGm4NYRUSU6JRWK=
QIMR-WIL NEHrdFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYHJR|UxRTJ{LkC0O|gh|ryP NFjWeYFUSU6JRWK=
NCI-H69 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUTTUVBKUUN3ME2yNk41Ojl7IN88US=> NYHIWHVyW0GQR1XS
TE-5 Mli1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXPJR|UxRTJ{LkS5OlUh|ryP MXnTRW5ITVJ?
NCI-H1993 MlHwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmTKTWM2OD1{Mj60PVcyKM7:TR?= MUHTRW5ITVJ?
NCI-H1092 M4Tkfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnTtTWM2OD1{Mz6yPFQ{KM7:TR?= NWLXVWlwW0GQR1XS
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... 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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