Nilotinib (AMN-107)

製品コードS1033

Nilotinib (AMN-107)化学構造

分子量(MW):529.52

Nilotinib (AMN-107)は一種のBcr-Abl阻害剤で、マウス類骨髄前駆細胞の中にIC50値が30 nM以下です。

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JPY 13102.90 あり
JPY 10079.16 あり
JPY 30237.48 あり
JPY 67674.36 あり

カスタマーフィードバック(5)

  • Ba/F3-p210T315I cells were treated with indicated concentrations of nilotinib with or without PDMP for 24 h. Apoptosis was determined as in A. Data are shown as percentage of sub-G1 for apoptosis in triplicate cultures. *P<0.05.

    FASEB J 2011 25, 3661-3673. Nilotinib (AMN-107) purchased from Selleck.

    Effect of nilotinib on Bcr-Abl kinase activity in ABCB1- and ABCG2- overexpressing CD34+CD38- cells. K562 parental cells and CD34+CD38- subpopulation isolated from K562 cells were treated with nilotinib at 0.01, 0.1 and 1.0 umol/L for 12 h. Equal amount of protein was loaded for western blot analysis as described in the Experimental section. The experiments were repeated at least three times independently, and a representative experiment is shown.

    Molecules 2014 19, 3356-75. Nilotinib (AMN-107) purchased from Selleck.

  •  

    Inhibition of thymidine (a and b) and cytarabine (c and d) uptake with nilotinib. The legend is similar to Fig. 1, except that imatinib was replaced by nilotinib.

    Leukemia Res 2012 36, 1311-1314. Nilotinib (AMN-107) purchased from Selleck.

    Nilotinib up-regulates the ERK survival signal in prostate cancer cells. (B and C) Immunoblot analyses of DU-145 cells (B) or DU-145 cells in comparison with LNCaP and PC-3 cells (C) treated with nilotinib for the expression of phospho-ERK1/2 T202/Y204 and total ERK. Immunoblot for GAPDH is shown as a loading control.

    Urol Oncol 2014 0.1016/j.urolonc.2014.06.001. Nilotinib (AMN-107) purchased from Selleck.

  • Immunohistochemical staining of xenografted DU-145 cells after 21 days of treatment with 75 mg/kg/d of nilotinib for phospho-ERK1/2 T202/Y204 expression. It can be noted that tumors explanted from vehicle-treated mice showed mostly positivity at the tumor periphery, whereas tumors explanted from nilotinib-treated mice showed a more evenly distributed phospho-ERK immunostaining (left panels). Quantification of phospho-ERK-positive DU-145 xenografts explanted after 21 days of treatment. Mean and standard errors of positive cells per high-power field (HPF; x40) from at least 3 tumors are given (right panel).

    Urol Oncol 2014 0.1016/j.urolonc.2014.06.001. Nilotinib (AMN-107) purchased from Selleck.

製品安全説明書

Bcr-Abl阻害剤の選択性比較

生物活性

製品説明 Nilotinib (AMN-107)は一種のBcr-Abl阻害剤で、マウス類骨髄前駆細胞の中にIC50値が30 nM以下です。
特性 A selective inhibitor of native and mutant Bcr-Abl.
ターゲット
Bcr-Abl [1]
(Murine myeloid progenitor cells)
<30 nM
体外試験

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]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
EoL-1-cell MlTxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4[zeWlEPTB;MD6wNFAyPDRizszN MXPTRW5ITVJ?
KU812 NHXHRm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF;jWmhKSzVyPUCuNFAzPDhizszN NELa[nRUSU6JRWK=
EM-2 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVzJR|UxRTBwMEC0NUDPxE1? MlzxV2FPT0WU
LAMA-84 M{PVT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn;STWM2OD1yLkCwOFkh|ryP MYfTRW5ITVJ?
MEG-01 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{TYTWlEPTB;MD6wNFgzQCEQvF2= M{WxXnNCVkeHUh?=
BV-173 NVP5V256T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmTETWM2OD1yLkCxNFg6KM7:TR?= NIjCOHdUSU6JRWK=
KASUMI-1 NIjhb|RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXPJR|UxRTBwMEK0NVMh|ryP NUeyXIJ5W0GQR1XS
NB7 NXX5WoZoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVrJR|UxRTBwMUO0N|kh|ryP MUXTRW5ITVJ?
BHT-101 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHvkcJRKSzVyPUCuOlQzPjNizszN NVv3SGFWW0GQR1XS
CGTH-W-1 M{ixfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWjDd2NxUUN3ME2wMlY1QDdizszN M1PXb3NCVkeHUh?=
HMV-II NF\OeVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NE\4TmdKSzVyPUCuO|Q5PzRizszN NXzSdWN3W0GQR1XS
NKM-1 M3\WW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIXKZpZKSzVyPUCuPVAyPSEQvF2= Ml62V2FPT0WU
LB2241-RCC M3O2O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHL6bWNKSzVyPUGuNFIzOjhizszN NHLQTYhUSU6JRWK=
NCI-H1703 M4SxZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3S1bGlEPTB;MT6xPFg4KM7:TR?= MV;TRW5ITVJ?
BE-13 MkXKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVflTodNUUN3ME2xMlI4PDF4IN88US=> NICxNHZUSU6JRWK=
ACN NXz1dWppT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX\JR|UxRTFwNUWwO|ch|ryP MVHTRW5ITVJ?
A204 NVLMWFhCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHfpV3BKSzVyPUGuOVczODVizszN MWXTRW5ITVJ?
HOP-62 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWPJR|UxRTFwOEKwO|ch|ryP M{f1PXNCVkeHUh?=
H9 NYfuSJBlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGnTc|hKSzVyPUKuO|M4QTNizszN NVPyTHZTW0GQR1XS
HCC1806 NUjTenJwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXX6V2VUUUN3ME2yMlc1OzJ5IN88US=> NFvDTYVUSU6JRWK=
NOS-1 NWDEc3BUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1HxfmlEPTB;Mj64O|ExOiEQvF2= Mn;CV2FPT0WU
RS4-11 NX;ze25bT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVvJR|UxRTJwOUC2NlMh|ryP MY\TRW5ITVJ?
JAR MlH0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1ThWmlEPTB;Mj65NlA5PCEQvF2= MY\TRW5ITVJ?
T98G MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFPEPWZKSzVyPUOuNFE{OTNizszN MXjTRW5ITVJ?
NCI-SNU-1 NFrEUYhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUfDWnB2UUN3ME2zMlQxODl{IN88US=> MoXEV2FPT0WU
SK-MEL-1 NIXSUopIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXLJR|UxRTNwNEOwNlkh|ryP NWHGfI1xW0GQR1XS
L-363 Mln2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NE\le5dKSzVyPUOuOlEyODdizszN M1LnWHNCVkeHUh?=
SW982 NFG5NplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2TTV2lEPTB;Mz62OFE3QSEQvF2= M{PmS3NCVkeHUh?=
HT-1080 M{fST2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVnJR|UxRTNwOUG3O|Uh|ryP MmG0V2FPT0WU
G-402 NX34RlVuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1jXbmlEPTB;ND6zNVIxOyEQvF2= MVnTRW5ITVJ?
HOS MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH;WUZRKSzVyPUSuPFAzQDJizszN M4\XOXNCVkeHUh?=
SK-NEP-1 M13zNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYHWcXZpUUN3ME20Mlg{OTlzIN88US=> MlzwV2FPT0WU
HAL-01 NVTq[HBPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn3KTWM2OD12Lki4NlQzKM7:TR?= NHHEfWdUSU6JRWK=
SBC-1 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXHJR|UxRTRwOUC5NFch|ryP MWrTRW5ITVJ?
CTV-1 M1XaPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHzyNHhKSzVyPUWuOFg6OzhizszN Mlm0V2FPT0WU
LCLC-103H Mo\RS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFi1XWtKSzVyPUWuO|c1PzFizszN NHnpSnZUSU6JRWK=
RVH-421 MkjxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHjVOGxKSzVyPUWuO|c2OzZizszN MljkV2FPT0WU
K-562 MoXSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4Ptc2lEPTB;NT65NFM3KM7:TR?= M{\YVHNCVkeHUh?=
CAL-33 NV;LVJNDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mk\yTWM2OD14LkOxN|U6KM7:TR?= MXzTRW5ITVJ?
MDA-MB-361 NXXiS4FRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1vtOWlEPTB;Nj6zN|Y6QSEQvF2= MYTTRW5ITVJ?
IGROV-1 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVjhU5RFUUN3ME22MlQ4OTlzIN88US=> MXzTRW5ITVJ?
NY NGXOcGhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX;HdI9{UUN3ME22MlU{PTl7IN88US=> NGnZfJFUSU6JRWK=
Ramos-2G6-4C10 MnK5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MULJR|UxRTZwNk[5N|Eh|ryP MnL5V2FPT0WU
HuO9 M2\MW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVXJR|UxRTZwN{O5OlQh|ryP NYXEcpNNW0GQR1XS
MS-1 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlzWTWM2OD15LkGxPVU{KM7:TR?= Moq0V2FPT0WU
RPMI-8226 NH\u[lZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoL1TWM2OD15LkK4Nlg4KM7:TR?= NH3LZWFUSU6JRWK=
HDLM-2 NFn1UHhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF[wfmdKSzVyPUeuOFAyPDlizszN MWrTRW5ITVJ?
D-566MG NVjYU4NPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX\JR|UxRTdwNEexOVUh|ryP MYjTRW5ITVJ?
SK-MEL-24 NX\aR5RDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnfETWM2OD15Lk[zN|kzKM7:TR?= MX3TRW5ITVJ?
COLO-679 NHXFTJJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{POc2lEPTB;Nz65PFY4OSEQvF2= MmXiV2FPT0WU
EW-13 NYPTUWx{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWS3ZW1vUUN3ME24MlMzODV2IN88US=> M33ndHNCVkeHUh?=
A388 NFq0WFFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYnJR|UxRThwM{i0PFEh|ryP M4rWOnNCVkeHUh?=
UM-UC-3 Mk\HS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3q5TmlEPTB;OD60N|k2PiEQvF2= M3jlXXNCVkeHUh?=
NUGC-3 NInoWolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3vqXWlEPTB;OD61N|U5OiEQvF2= MmXuV2FPT0WU
COLO-668 NF;iSZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoXCTWM2OD16LkW5OFkyKM7:TR?= NIDNVWVUSU6JRWK=
MOLT-4 NGezcmZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3P2UWlEPTB;OD62NlM2OyEQvF2= NGL3cWJUSU6JRWK=
D-423MG MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIDSbYhKSzVyPUiuPFM4PTZizszN M{fzZXNCVkeHUh?=
CTB-1 MkXZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmXqTWM2OD16Lki3NVI5KM7:TR?= M2X6fnNCVkeHUh?=
BCPAP NIX0fWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUTJR|UxRTlwMEK1OlIh|ryP MkPaV2FPT0WU
GCT NU[xOZF4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUPJR|UxRTlwMEm4N|Eh|ryP NVHmfJFJW0GQR1XS
ACHN M2Ho[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUTJR|UxRTlwMkO2N|Ih|ryP MnfhV2FPT0WU
KYSE-520 MkXTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2PZO2lEPTB;OT6zN|Q5OiEQvF2= MlnIV2FPT0WU
LB771-HNC NVe3dY9MT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYTJR|UxRTlwN{[0PVch|ryP MX;TRW5ITVJ?
MLMA MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkfaTWM2OD1zMD6wNVMzKM7:TR?= NFXEdY1USU6JRWK=
HEC-1 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHXP[mVKSzVyPUGwMlI5ODRizszN MnXOV2FPT0WU
HL-60 MofVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXrOdm5WUUN3ME2xNE43QDV|IN88US=> M3rlVXNCVkeHUh?=
A101D M4TTV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M13IWmlEPTB;MUCuPFkzOyEQvF2= NEfqeFdUSU6JRWK=
A2058 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2fwe2lEPTB;MUCuPVI1PSEQvF2= Ml;6V2FPT0WU
KARPAS-45 NYfvfod4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkTFTWM2OD1zMT6wOlM2KM7:TR?= NV;IcYdRW0GQR1XS
697 NV;WVW1sT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3\ifWlEPTB;MUGuNlExOSEQvF2= MmnlV2FPT0WU
NCI-N87 MkK3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXfEOHBkUUN3ME2xNU44PzNzIN88US=> M3rBXnNCVkeHUh?=
DSH1 NUfKU4xIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVHJR|UxRTFzLke5OVMh|ryP NGDxWmpUSU6JRWK=
HLE NFnrRm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYLJR|UxRTFzLki4N|kh|ryP MVHTRW5ITVJ?
NCI-H720 NULrVIFLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{XEfGlEPTB;MUKuOlgxOSEQvF2= MXPTRW5ITVJ?
EW-3 MlXlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIPOOG9KSzVyPUGyMlk{ODdizszN NHuxRXdUSU6JRWK=
AGS MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXTJR|UxRTF|LkCzOVEh|ryP M2D2cnNCVkeHUh?=
ES5 NUH3eGZIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVPJR|UxRTF|LkC1NVIh|ryP MlO0V2FPT0WU
DB M2GyRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH3uToRKSzVyPUGzMlMzPTZizszN MmnsV2FPT0WU
A4-Fuk NWThSXhUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVTJR|UxRTF|LkSxNFIh|ryP NGPocpdUSU6JRWK=
A427 NEXqe41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWjacIcyUUN3ME2xN{41QTd{IN88US=> MYPTRW5ITVJ?
MN-60 NFzGSXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFvGb5ZKSzVyPUGzMlU5PDNizszN NX3SN3lHW0GQR1XS
HCC2218 MmrXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUnJR|UxRTF|LkW4OVYh|ryP MWPTRW5ITVJ?
MV-4-11 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlvVTWM2OD1zMz64NVM4KM7:TR?= NEPKPJhUSU6JRWK=
GI-1 NVH3ZXk1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVX0PYg2UUN3ME2xOE4yOTh2IN88US=> NX3aRYVWW0GQR1XS
JVM-3 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoS2TWM2OD1zND6yOlU3KM7:TR?= MkPPV2FPT0WU
NCI-H2029 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH\T[mpKSzVyPUG0MlI4OjdizszN NXfwdpo6W0GQR1XS
TE-12 M4HEcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NInseFVKSzVyPUG0MlYxPDZizszN NH60PHdUSU6JRWK=
WM-115 NEPoRnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkewTWM2OD1zNT61Olg{KM7:TR?= NXXRVFRrW0GQR1XS
BB65-RCC NIS0O3VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2jvbGlEPTB;MU[uNFI1OSEQvF2= NUfTWmF4W0GQR1XS
NCI-H1693 M4PDR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MojsTWM2OD1zNj6zPFAzKM7:TR?= M{e0UHNCVkeHUh?=
KARPAS-299 M3HWfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmrNTWM2OD1zNj62NlA{KM7:TR?= NUPwWIN7W0GQR1XS
UACC-257 NGrV[ZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn7STWM2OD1zNz6wOVgzKM7:TR?= M1rUdXNCVkeHUh?=
RKO NFSwVJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NILPZYlKSzVyPUG3MlY1OzNizszN NWnFXpZVW0GQR1XS
HT-29 M2TlW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{LRNWlEPTB;MUeuO|g5QSEQvF2= MUXTRW5ITVJ?
ES7 M3zKWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWnZ[2RGUUN3ME2xPE4yOTJ{IN88US=> MnHKV2FPT0WU
DEL MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHLqfVFKSzVyPUG4MlMyPzJizszN NHrtOmZUSU6JRWK=
BT-549 NHW5eHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlfoTWM2OD1zOD60NFkzKM7:TR?= MUPTRW5ITVJ?
NCI-H1755 MkXLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWDJR|UxRTF6LkW3NlMh|ryP M4i4UXNCVkeHUh?=
HCE-T MoGzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXPJR|UxRTF6LkizOFEh|ryP NIr5fnpUSU6JRWK=
LU-139 MnXwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{jNR2lEPTB;MUmuNFQ2QCEQvF2= Mn;3V2FPT0WU
ECC10 M2HCZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVrJR|UxRTF7LkK0O|Uh|ryP NXK1NZlqW0GQR1XS
769-P MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2XBU2lEPTB;MUmuOlM{PSEQvF2= MnzxV2FPT0WU
BALL-1 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoXZTWM2OD1zOT62O|c2KM7:TR?= M1;5fHNCVkeHUh?=
LXF-289 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWDJR|UxRTF7Lki5O|kh|ryP MojLV2FPT0WU
TYK-nu NVrITXJMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXXGVoVjUUN3ME2xPU46OzF3IN88US=> M2PFSnNCVkeHUh?=
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NCI-SNU-5 M3vsb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYHJR|UxRTN7Lk[5NVYh|ryP NX7idIRuW0GQR1XS
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SCC-4 Mmr1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MljQTWM2OD12MT6yNVM4KM7:TR?= MVfTRW5ITVJ?
no-11 Mlj3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHPFZ5BKSzVyPUSxMlc{PTRizszN NUXNdHd{W0GQR1XS
HT-144 M1HCeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFS5N4dKSzVyPUSyMlA2PjdizszN NWPYdVhZW0GQR1XS
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ES8 NX\jTXdIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2\4WWlEPTB;NEOuN|Y6QCEQvF2= NUnLSZo6W0GQR1XS
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GAMG MmnkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2jhVWlEPTB;NEOuOFUyPyEQvF2= NWf5N29CW0GQR1XS
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TE-1 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmnlTWM2OD12NT6xOlU1KM7:TR?= MkLzV2FPT0WU
J-RT3-T3-5 MmriS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWrDc|lmUUN3ME20OU41OzF3IN88US=> MlX2V2FPT0WU
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D-392MG M13WXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVO2ZlBTUUN3ME20OU46OjV4IN88US=> MlSyV2FPT0WU
KALS-1 M3j6PGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlnUTWM2OD12Nj63NlU4KM7:TR?= MXXTRW5ITVJ?
MMAC-SF MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYHVU|hmUUN3ME20Ok46QTV{IN88US=> NEnZcnJUSU6JRWK=
HSC-3 NIfhVJVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGfzbGxKSzVyPUS3MlM3ODhizszN MlfJV2FPT0WU
KM-H2 MnXFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV3JR|UxRTR5Lk[wNFch|ryP MojNV2FPT0WU
LoVo MlfRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUXJR|UxRTR6LkGwNFIh|ryP MmKxV2FPT0WU
NCI-H510A MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1PtZ2lEPTB;NEiuNVg4OSEQvF2= Mo\pV2FPT0WU
EW-11 MmLLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYXJR|UxRTR6LkKzOFgh|ryP NYXGPFlbW0GQR1XS
HCC2998 NYTHRpVxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NU[5cGkxUUN3ME20PE43OjN4IN88US=> NVX1[o1[W0GQR1XS
J82 M4foUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3G0S2lEPTB;NEiuO|I1OiEQvF2= MmfKV2FPT0WU
ML-2 NGPJNFRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1HoXGlEPTB;NEmuOFYxPSEQvF2= M3PoRnNCVkeHUh?=
NCI-H2030 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVfJR|UxRTR7LkexNVch|ryP MUXTRW5ITVJ?
NCI-H1792 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXvvU4g4UUN3ME20PU45PTF6IN88US=> MkTxV2FPT0WU

多くの細胞株試験データを見る場合、クリックしてください

体内試験 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]

お薦めの試験操作(参考用のみ)

細胞試験: [4]
+ 展開
  • 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.
    (参考用のみ)
動物試験:[6]
+ 展開
  • 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
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 27 mg/mL (50.98 mM)
Water Insoluble
Ethanol Insoluble
体内 順序で溶剤を入れること:
4% DMSO+30% PEG 300+5% Tween 80+ddH2O
3mg/mL

* 溶解度検測はSelleck技術部門によって行いますので、文献より提供された溶解度と差異がある可能性がありますが、生産工芸と不同ロット(lot)で起きる正常な現象ですから、ご安心ください。

化学情報

分子量 529.52
化学式

C28H22F3N7O

CAS No. 641571-10-0
保管
in solvent
別名 N/A

便利ツール

モル濃度計算器

モル濃度計算器

解決のために必要とされるマス、ボリュームまたは濃度を計算してください。

マス (g) = 濃度 (mol/L) x ボリューム (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • マス
    濃度
    ボリューム
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備することを要求される希釈剤を計算してください. セレック希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 輸入 輸出 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

マス 濃度 ボリューム 分子量

臨床試験

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02973711 Not yet recruiting Leukemia, Chronic Myeloid University of Michigan Cancer Center February 2017 Phase 1|Phase 2
NCT02954978 Recruiting Parkinson Disease|Parkinsons Disease With Dementia Georgetown University January 2017 Phase 2
NCT02947893 Recruiting Alzheimers Disease Georgetown University January 2017 Phase 2
NCT02602314 Not yet recruiting Chronyc Myeloid Leukemia Gruppo Italiano Malattie EMatologiche dellAdulto December 2016 Phase 4
NCT02709083 Recruiting Chronic Myelogenous Leukemia|Chronic Myeloid Leukemia|Leukemia Emory University October 2016 Phase 2
NCT02917720 Not yet recruiting Chronic Myeloid Leukemia European LeukemiaNet|Heidelberg University|Ludwig-Maximilians - University of Munich October 2016 Phase 2

技術サポート

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Handling Instructions

他の質問がある場合は、お気軽くお問合せください。

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Bcr-Abl信号経路図

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Tags: Nilotinib (AMN-107)を買う | Nilotinib (AMN-107) ic50 | Nilotinib (AMN-107)供給者 | Nilotinib (AMN-107)を購入する | Nilotinib (AMN-107)費用 | Nilotinib (AMN-107)生産者 | オーダーNilotinib (AMN-107) | Nilotinib (AMN-107)化学構造 | Nilotinib (AMN-107)分子量 | Nilotinib (AMN-107)代理店
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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID