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 M2\ySGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlzwTWM2OD1yLkCwNFE1PCEQvF2= MXHTRW5ITVJ?
KU812 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVzJR|UxRTBwMECyOFgh|ryP MWXTRW5ITVJ?
EM-2 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXfydG1HUUN3ME2wMlAxPDFizszN MVHTRW5ITVJ?
LAMA-84 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHrUVWNKSzVyPUCuNFA1QSEQvF2= M2\FXHNCVkeHUh?=
MEG-01 NHvLUHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXXJR|UxRTBwMEC4Nlgh|ryP NWOwc4xOW0GQR1XS
BV-173 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3zvSmlEPTB;MD6wNVA5QSEQvF2= MmPmV2FPT0WU
KASUMI-1 NFjjfphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn\BTWM2OD1yLkCyOFE{KM7:TR?= NEjCb3BUSU6JRWK=
NB7 M{\hc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHTDXFhKSzVyPUCuNVM1OzlizszN MYXTRW5ITVJ?
BHT-101 M3fCeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH;sR21KSzVyPUCuOlQzPjNizszN M{\ZXXNCVkeHUh?=
CGTH-W-1 Mn\ZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWL6boRUUUN3ME2wMlY1QDdizszN NUTTdVN5W0GQR1XS
HMV-II MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVPJR|UxRTBwN{S4O|Qh|ryP NVm4fJU1W0GQR1XS
NKM-1 NEXBOlNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkXCTWM2OD1yLkmwNVUh|ryP MWDTRW5ITVJ?
LB2241-RCC NHu5d|FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoewTWM2OD1zLkCyNlI5KM7:TR?= MYLTRW5ITVJ?
NCI-H1703 NFPhb5pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlvhTWM2OD1zLkG4PFch|ryP NH\EfIlUSU6JRWK=
BE-13 MorOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NULHRmN4UUN3ME2xMlI4PDF4IN88US=> NVTDOWtnW0GQR1XS
ACN NF;M[GJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYPJR|UxRTFwNUWwO|ch|ryP NUDwfnpCW0GQR1XS
A204 NGnUTmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUDweFRmUUN3ME2xMlU4OjB3IN88US=> MkTLV2FPT0WU
HOP-62 NYm4NJFZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH3LSJNKSzVyPUGuPFIxPzdizszN NWfXbXlXW0GQR1XS
H9 MknvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MU\JR|UxRTJwN{O3PVMh|ryP MlHZV2FPT0WU
HCC1806 MoG1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlrCTWM2OD1{Lke0N|I4KM7:TR?= M4fnZ3NCVkeHUh?=
NOS-1 M4C1O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkPUTWM2OD1{Lki3NVAzKM7:TR?= NEnvb21USU6JRWK=
RS4-11 NYfjdoZbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnfFTWM2OD1{LkmwOlI{KM7:TR?= M1HzVHNCVkeHUh?=
JAR MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYP5SIZ1UUN3ME2yMlkzODh2IN88US=> NVX0NJhyW0GQR1XS
T98G M17tVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NULIVmhtUUN3ME2zMlAyOzF|IN88US=> M1zrcXNCVkeHUh?=
NCI-SNU-1 NFLlOVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkPaTWM2OD1|LkSwNFkzKM7:TR?= NWHIOHREW0GQR1XS
SK-MEL-1 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIroXWNKSzVyPUOuOFMxOjlizszN NH6xZXZUSU6JRWK=
L-363 NUDXeIJ[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M37VUWlEPTB;Mz62NVExPyEQvF2= MVrTRW5ITVJ?
SW982 MlXNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXTRVo8{UUN3ME2zMlY1OTZ7IN88US=> NV6zUJpyW0GQR1XS
HT-1080 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml7ETWM2OD1|LkmxO|c2KM7:TR?= MkfrV2FPT0WU
G-402 M{TtUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIrHb4lKSzVyPUSuN|EzODNizszN MoLiV2FPT0WU
HOS MmXMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYjJR|UxRTRwOECyPFIh|ryP M3XB[XNCVkeHUh?=
SK-NEP-1 NWTCcWZTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYPJWWlsUUN3ME20Mlg{OTlzIN88US=> NFK4eVBUSU6JRWK=
HAL-01 M3fIVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYHJem1[UUN3ME20Mlg5OjR{IN88US=> NHvpUlVUSU6JRWK=
SBC-1 M3;WZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkLVTWM2OD12LkmwPVA4KM7:TR?= NHXYT|RUSU6JRWK=
CTV-1 M33Wemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{DNW2lEPTB;NT60PFk{QCEQvF2= M4fnWHNCVkeHUh?=
LCLC-103H M4rXPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEHtVGJKSzVyPUWuO|c1PzFizszN NX\Pb4Z5W0GQR1XS
RVH-421 MlTWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnzwTWM2OD13Lke3OVM3KM7:TR?= NH7UbYlUSU6JRWK=
K-562 M{Dm[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEWxUHNKSzVyPUWuPVA{PiEQvF2= MUHTRW5ITVJ?
CAL-33 MlXaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{HNV2lEPTB;Nj6zNVM2QSEQvF2= NVXuOIpzW0GQR1XS
MDA-MB-361 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{ezXWlEPTB;Nj6zN|Y6QSEQvF2= MVfTRW5ITVJ?
IGROV-1 MoDXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWDrOVJmUUN3ME22MlQ4OTlzIN88US=> M{PvNHNCVkeHUh?=
NY MoLiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYL6cpl1UUN3ME22MlU{PTl7IN88US=> NFTvdIRUSU6JRWK=
Ramos-2G6-4C10 M1GycGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MljYTWM2OD14Lk[2PVMyKM7:TR?= MXnTRW5ITVJ?
HuO9 M1rtZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MknjTWM2OD14LkezPVY1KM7:TR?= NIHaOZJUSU6JRWK=
MS-1 NWjj[YdCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1;FfmlEPTB;Nz6xNVk2OyEQvF2= M3;ScXNCVkeHUh?=
RPMI-8226 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGXYdnhKSzVyPUeuNlgzQDdizszN NYPsPYZsW0GQR1XS
HDLM-2 Mn;HS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1PuNWlEPTB;Nz60NFE1QSEQvF2= M1XCbnNCVkeHUh?=
D-566MG NVG2Z3J{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYnJR|UxRTdwNEexOVUh|ryP M2WzcHNCVkeHUh?=
SK-MEL-24 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXTJR|UxRTdwNkOzPVIh|ryP NFrsVIVUSU6JRWK=
COLO-679 NGT3OWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2DwPWlEPTB;Nz65PFY4OSEQvF2= NXnDNI1pW0GQR1XS
EW-13 MmLKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWflc497UUN3ME24MlMzODV2IN88US=> M{DsUnNCVkeHUh?=
A388 MknzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWrJR|UxRThwM{i0PFEh|ryP NGGzfYJUSU6JRWK=
UM-UC-3 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmLxTWM2OD16LkSzPVU3KM7:TR?= M121UXNCVkeHUh?=
NUGC-3 NI[3NYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NW\obIpQUUN3ME24MlU{PTh{IN88US=> NHr5endUSU6JRWK=
COLO-668 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF23WZVKSzVyPUiuOVk1QTFizszN NVfFXGpSW0GQR1XS
MOLT-4 M2DXWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3TqT2lEPTB;OD62NlM2OyEQvF2= MkXHV2FPT0WU
D-423MG MknTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGDp[lJKSzVyPUiuPFM4PTZizszN NULUSGg5W0GQR1XS
CTB-1 NF;pXlFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUDWfpZCUUN3ME24Mlg4OTJ6IN88US=> MVvTRW5ITVJ?
BCPAP M3Px[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVPCOGQxUUN3ME25MlAzPTZ{IN88US=> M3TaeHNCVkeHUh?=
GCT MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlfWTWM2OD17LkC5PFMyKM7:TR?= NVXwfZcxW0GQR1XS
ACHN MlHIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVHJR|UxRTlwMkO2N|Ih|ryP MnPKV2FPT0WU
KYSE-520 NG\FXXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEXVbGlKSzVyPUmuN|M1QDJizszN MmDkV2FPT0WU
LB771-HNC NFvLTmVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2PG[GlEPTB;OT63OlQ6PyEQvF2= Ml3FV2FPT0WU
MLMA NWeyfVZvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mkn1TWM2OD1zMD6wNVMzKM7:TR?= MUTTRW5ITVJ?
HEC-1 M2DCSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEDGXXpKSzVyPUGwMlI5ODRizszN MUPTRW5ITVJ?
HL-60 NXv5[4lvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFHkT3NKSzVyPUGwMlY5PTNizszN MXHTRW5ITVJ?
A101D NUTBPVZmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFvzfJdKSzVyPUGwMlg6OjNizszN MVTTRW5ITVJ?
A2058 M4DmOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4fJd2lEPTB;MUCuPVI1PSEQvF2= MnmzV2FPT0WU
KARPAS-45 M4i2cWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWDJR|UxRTFzLkC2N|Uh|ryP Mm\UV2FPT0WU
697 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlPYTWM2OD1zMT6yNVAyKM7:TR?= MojKV2FPT0WU
NCI-N87 Mn3hS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4G4WGlEPTB;MUGuO|c{OSEQvF2= NWjEPWc1W0GQR1XS
DSH1 NUTxN4w2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXL1dJdoUUN3ME2xNU44QTV|IN88US=> NWPUS4gzW0GQR1XS
HLE MnXuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVfNbGl[UUN3ME2xNU45QDN7IN88US=> NYjNdmtkW0GQR1XS
NCI-H720 M2PPcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGXNTplKSzVyPUGyMlY5ODFizszN NHfXb5hUSU6JRWK=
EW-3 NG\WOHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3;MTWlEPTB;MUKuPVMxPyEQvF2= MnjMV2FPT0WU
AGS M3:yOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4\CV2lEPTB;MUOuNFM2OSEQvF2= NELj[nBUSU6JRWK=
ES5 MnLyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4nDPWlEPTB;MUOuNFUyOiEQvF2= MWLTRW5ITVJ?
DB MneyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M33KUGlEPTB;MUOuN|I2PiEQvF2= M3;ENnNCVkeHUh?=
A4-Fuk M1XaUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MojJTWM2OD1zMz60NVAzKM7:TR?= MYjTRW5ITVJ?
A427 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{npdGlEPTB;MUOuOFk4OiEQvF2= M3ewOXNCVkeHUh?=
MN-60 MlTWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2HXUGlEPTB;MUOuOVg1OyEQvF2= MWrTRW5ITVJ?
HCC2218 M17pVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXflZZp7UUN3ME2xN{42QDV4IN88US=> NV;reFFEW0GQR1XS
MV-4-11 NUHORZJ3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4TPfmlEPTB;MUOuPFE{PyEQvF2= NYfC[XE4W0GQR1XS
GI-1 NIjHbmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2TJXmlEPTB;MUSuNVE5PCEQvF2= MVTTRW5ITVJ?
JVM-3 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGHTbWxKSzVyPUG0MlI3PTZizszN M3;1OnNCVkeHUh?=
NCI-H2029 M3fTc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mlv6TWM2OD1zND6yO|I4KM7:TR?= NF7ifpdUSU6JRWK=
TE-12 Mn;1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MljwTWM2OD1zND62NFQ3KM7:TR?= MX7TRW5ITVJ?
WM-115 NH:wN4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MY\JR|UxRTF3LkW2PFMh|ryP NX\uVoNjW0GQR1XS
BB65-RCC NUHhcGc2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NELhS5RKSzVyPUG2MlAzPDFizszN M{HSPHNCVkeHUh?=
NCI-H1693 MkTBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIHqfVhKSzVyPUG2MlM5ODJizszN NX3xXVV6W0GQR1XS
KARPAS-299 MnP2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV7GTGZtUUN3ME2xOk43OjB|IN88US=> Ml;zV2FPT0WU
UACC-257 M37xUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mm[1TWM2OD1zNz6wOVgzKM7:TR?= MYjTRW5ITVJ?
RKO MmPsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVXJR|UxRTF5Lk[0N|Mh|ryP NGPp[XFUSU6JRWK=
HT-29 M{flRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2TzO2lEPTB;MUeuO|g5QSEQvF2= M3vrNHNCVkeHUh?=
ES7 M4XLbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlfQTWM2OD1zOD6xNVIzKM7:TR?= NFfNUY1USU6JRWK=
DEL M{PvOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWThSmRCUUN3ME2xPE4{OTd{IN88US=> NXOxOXJ4W0GQR1XS
BT-549 M3LtXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEnXbJlKSzVyPUG4MlQxQTJizszN MWHTRW5ITVJ?
NCI-H1755 M{PKWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGH4fHRKSzVyPUG4MlU4OjNizszN MW\TRW5ITVJ?
HCE-T NH;GcIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXHJR|UxRTF6LkizOFEh|ryP M2rqd3NCVkeHUh?=
LU-139 NH;ZXItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXfXSIdyUUN3ME2xPU4xPDV6IN88US=> MUTTRW5ITVJ?
ECC10 NGHZTmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYLJcFh4UUN3ME2xPU4zPDd3IN88US=> MXXTRW5ITVJ?
769-P MkGzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF;vOlRKSzVyPUG5MlY{OzVizszN NVTac4FGW0GQR1XS
BALL-1 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV3vPJVnUUN3ME2xPU43Pzd3IN88US=> NWS4c|YxW0GQR1XS
LXF-289 M2nE[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFjJWVRKSzVyPUG5Mlg6PzlizszN MWfTRW5ITVJ?
TYK-nu MmjUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF36OnhKSzVyPUG5Mlk{OTVizszN MmfkV2FPT0WU
NCI-H630 NUT5N|R[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2fqfWlEPTB;MUmuPVM4QCEQvF2= MXTTRW5ITVJ?
EW-18 NGew[FlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkPYTWM2OD1{MD6zPFAzKM7:TR?= M2TMenNCVkeHUh?=
KYSE-150 MmDkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NELIfINKSzVyPUKwMlcxPDdizszN NXLYRWhLW0GQR1XS
LOXIMVI MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWHWfpdLUUN3ME2yNE44PTh4IN88US=> MojMV2FPT0WU
HuP-T3 MoG2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml:0TWM2OD1{MT6wPFUzKM7:TR?= NWThd5lWW0GQR1XS
MFE-280 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnXYTWM2OD1{MT61Olc6KM7:TR?= NGDae3FUSU6JRWK=
SK-OV-3 M4TIOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M374UmlEPTB;MkGuPFQxQCEQvF2= MmDPV2FPT0WU
QIMR-WIL M2qwbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHjIVHVKSzVyPUKyMlA1PzhizszN NWXWfpVOW0GQR1XS
NCI-H69 NVzrO4tCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYDJR|UxRTJ{LkSyPVkh|ryP NUHiTpFYW0GQR1XS
TE-5 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4fNbWlEPTB;MkKuOFk3PSEQvF2= M2LZdnNCVkeHUh?=
NCI-H1993 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH\JbmpKSzVyPUKyMlQ6PzFizszN MV\TRW5ITVJ?
NCI-H1092 NVWyVmJCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGi2WHpKSzVyPUKzMlI5PDNizszN MnK4V2FPT0WU
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HD-MY-Z M2XvOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX22V2NLUUN3ME2yOE4zOzZ{IN88US=> NFnvVYRUSU6JRWK=
NCI-H2342 Ml;CS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWPp[|ZCUUN3ME2yOE43PzZ5IN88US=> MnfLV2FPT0WU
C32 MnrMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYHZTm9vUUN3ME2yOE46PTd4IN88US=> NWHBN2t2W0GQR1XS
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NCI-H358 NX3lc|BKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{HnRWlEPTB;MkWuN|k1OyEQvF2= MmnTV2FPT0WU
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NCI-H292 NETEN2RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWTJR|UxRTJ5Lkm2NVch|ryP NVjRUJlUW0GQR1XS
NCI-H446 M4PFUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVjJRpR3UUN3ME2yPE4zOTB3IN88US=> NFfGbIZUSU6JRWK=
NCI-H2009 M3vqWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkXCTWM2OD1{OT6xOFMyKM7:TR?= M{f6XnNCVkeHUh?=
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TI-73 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVKzOoJOUUN3ME2yPU41ODBzIN88US=> NIrKUnlUSU6JRWK=
NCI-H2228 NWfo[JlZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFL4bFJKSzVyPUK5MlQ2QCEQvF2= NV:wS5ljW0GQR1XS
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NCI-H1304 NInhbIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX\YSHRJUUN3ME2zNE42PzF4IN88US=> NWW3fGFjW0GQR1XS
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KG-1 M3nvfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3nPc2lEPTB;M{GuO|QzQSEQvF2= NX:2WGZDW0GQR1XS
A2780 M4TodGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MULJR|UxRTNzLkizOVgh|ryP MnruV2FPT0WU
NCI-H28 MlLaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHfVXm1KSzVyPUOxMlk5PjFizszN MVLTRW5ITVJ?
C2BBe1 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVnNOpk5UUN3ME2zNk4zPjN2IN88US=> Mm\1V2FPT0WU
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SBC-5 NYHVVnZ{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2PCUGlEPTB;M{KuPFUyOSEQvF2= NX;pOo52W0GQR1XS
OVCAR-4 Mn;XS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEPRNphKSzVyPUOzMlQ5PDhizszN NE\EU5lUSU6JRWK=
COR-L88 NHvvcIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3j0XmlEPTB;M{SuNFc1OSEQvF2= MonaV2FPT0WU
SW954 M2noe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXjJR|UxRTN2LkC3OVIh|ryP MmPoV2FPT0WU
COLO-684 NF;xTm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXfJR|UxRTN2LkO0NFQh|ryP MojEV2FPT0WU
HCC70 MnPrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHvDR4hKSzVyPUO0Mlk2OTRizszN M33PWXNCVkeHUh?=
NCI-H1770 NXzpd4tqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1HXb2lEPTB;M{SuPVYyKM7:TR?= MmX4V2FPT0WU
NCI-H1666 MoDLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M37FfWlEPTB;M{WuPFI2OyEQvF2= MUXTRW5ITVJ?
YH-13 M{TqeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mk\TTWM2OD1|NT65NkDPxE1? NEXhNYdUSU6JRWK=
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KNS-62 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M13xfWlEPTB;M{[uPVQ{QCEQvF2= MmHBV2FPT0WU
SK-MEL-30 NXj0e2RJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M33VZWlEPTB;M{euPFc{PyEQvF2= NEna[GhUSU6JRWK=
SJRH30 M1;YZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mmm5TWM2OD1|OD63N|QyKM7:TR?= MVHTRW5ITVJ?
GP5d NGTpTlBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGK1RnlKSzVyPUO4Mlg3PTNizszN MlfiV2FPT0WU
SW1116 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MljBTWM2OD1|OT6yPFA2KM7:TR?= NYXzbXpZW0GQR1XS
COLO-800 MnjuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYXKcmxkUUN3ME2zPU4{PjN6IN88US=> NHi4dYFUSU6JRWK=
RD M3:4TGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlnwTWM2OD1|OT61NlU5KM7:TR?= MoTzV2FPT0WU
NCI-SNU-5 NH;uOnhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUXNR2VrUUN3ME2zPU43QTF4IN88US=> M1LUWXNCVkeHUh?=
HuO-3N1 Mnm4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYnJR|UxRTRyLkGwPEDPxE1? Mo\wV2FPT0WU
SK-UT-1 NUfEN2pyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NY\TU45UUUN3ME20NE42Pjd2IN88US=> MVjTRW5ITVJ?
SK-MEL-3 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M13OSGlEPTB;NECuOVk{OiEQvF2= MULTRW5ITVJ?
SK-MEL-28 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEKyRYVKSzVyPUSwMlY1OzVizszN NWDWeWtsW0GQR1XS
SCC-4 NVHiSGRXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlW0TWM2OD12MT6yNVM4KM7:TR?= M{TKUHNCVkeHUh?=
no-11 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkjFTWM2OD12MT63N|U1KM7:TR?= MljxV2FPT0WU
HT-144 NVHpeZVKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIrqV4FKSzVyPUSyMlA2PjdizszN NV\ZVlNWW0GQR1XS
MFM-223 M{PmRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mlf6TWM2OD12Mj60NFIh|ryP NV7xOFhtW0GQR1XS
ONS-76 NWXaN29kT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWPJR|UxRTR{LkiwNVgh|ryP NIroRoFUSU6JRWK=
ES8 M2DjWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYjJR|UxRTR|LkO2PVgh|ryP M4jvT3NCVkeHUh?=
T-24 M13ucWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWrJR|UxRTR|LkSzOlkh|ryP M2\Nc3NCVkeHUh?=
GAMG M4HmVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGHNZZJKSzVyPUSzMlQ2OTdizszN NWfleoMxW0GQR1XS
LU-135 MojrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{HZNmlEPTB;NESuNFkzOyEQvF2= MXnTRW5ITVJ?
HCC1187 M1z1VGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFHtblNKSzVyPUS0MlgzPjJizszN Mn7hV2FPT0WU
TE-1 NV:5e404T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnXQTWM2OD12NT6xOlU1KM7:TR?= NV7jOJRYW0GQR1XS
J-RT3-T3-5 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoSzTWM2OD12NT60N|E2KM7:TR?= NWDTOlBMW0GQR1XS
GI-ME-N NUHPNlZHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{\LeWlEPTB;NEWuPFk2OiEQvF2= MoDZV2FPT0WU
D-392MG NYfZUpFUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1;iTmlEPTB;NEWuPVI2PiEQvF2= Mn[wV2FPT0WU
KALS-1 M1jyTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnLjTWM2OD12Nj63NlU4KM7:TR?= NE\YfYlUSU6JRWK=
MMAC-SF M4LoNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoTKTWM2OD12Nj65PVUzKM7:TR?= M1fHO3NCVkeHUh?=
HSC-3 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVnLXnBPUUN3ME20O{4{PjB6IN88US=> MmW0V2FPT0WU
KM-H2 NVLBWYVCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXm5bHJYUUN3ME20O{43ODB5IN88US=> M4XoXnNCVkeHUh?=
LoVo MmO1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHrLUplKSzVyPUS4MlExODJizszN M3;5U3NCVkeHUh?=
NCI-H510A M1TVTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NImwe5hKSzVyPUS4MlE5PzFizszN MmnXV2FPT0WU
EW-11 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEjRcHFKSzVyPUS4MlI{PDhizszN NGnuO3VUSU6JRWK=
HCC2998 M2PKNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVLqWZZFUUN3ME20PE43OjN4IN88US=> MU\TRW5ITVJ?
J82 M3TX[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1nwTmlEPTB;NEiuO|I1OiEQvF2= NGWwR49USU6JRWK=
ML-2 NHzLbGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{L4fGlEPTB;NEmuOFYxPSEQvF2= MUTTRW5ITVJ?
NCI-H2030 NYDxU4toT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEPjNXNKSzVyPUS5MlcyOTdizszN M2LFSnNCVkeHUh?=
NCI-H1792 NYDnPHVIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXzSWo51UUN3ME20PU45PTF6IN88US=> MVLTRW5ITVJ?

... 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

文献中の引用 (19)

技術サポート&よくある質問(FAQ)

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