Ibrutinib (PCI-32765)

For research use only. Not for use in humans.

製品コードS2680

Ibrutinib (PCI-32765)化学構造

CAS No. 936563-96-1

Ibrutinib (PCI-32765) is a potent and highly selective Brutons tyrosine kinase (Btk) inhibitor with IC50 of 0.5 nM in cell-free assays, modestly potent to Bmx, CSK, FGR, BRK, HCK, less potent to EGFR, Yes, ErbB2, JAK3, etc.

サイズ 価格(税別)  
10mM (1mL in DMSO) JPY 47100
JPY 30200
JPY 163000
JPY 412000
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文献中Selleckの製品使用例(447)

製品安全説明書

Target Protein Ligand阻害剤の選択性比較

生物活性

製品説明 Ibrutinib (PCI-32765) is a potent and highly selective Brutons tyrosine kinase (Btk) inhibitor with IC50 of 0.5 nM in cell-free assays, modestly potent to Bmx, CSK, FGR, BRK, HCK, less potent to EGFR, Yes, ErbB2, JAK3, etc.
ターゲット
BTK [1]
(Cell-free assay)
BLK [1]
(Cell-free assay)
Bmx [1]
(Cell-free assay)
CSK [1]
(Cell-free assay)
FGR [1]
(Cell-free assay)
0.5 nM 0.5 nM 0.8 nM 2.3 nM 2.3 nM
体外試験

Ibrutinib shows the potent and irreversible inhibitory effect and selectivity for Btk enzymatic activity. In BCR pathway-activated DOHH2 cell line, Ibrutinib inhibits autophosphorylation of Btk, phosphorylation of Btk's physiological substrate PLCγ, and phosphorylation of further downstream kinase, ERK with IC50 of 11 nM, 29 nM and 13 nM, respectively. [1] Ibrutinib exhibits a significant dose-dependent and time-dependent induction of cytotoxicity in chronic lymphocytic leukemia (CLL) cells. In addition, Ibrutinib induces cell death depending on caspase pathway activation and antagonizes the ability of CLL cells to proliferate after TLR signaling. [2] A recent study shows that Ibrutinib inhibits BCR-activated primary B cell proliferation with IC50 of 8 nM and results in inhibition of TNFα, IL-1β and IL-6 production in primary monocytes with IC50 of 2.6 nM, 0.5 nM and 3.9 nM, respectively. [3]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human Rec1 cells MlzQSpVv[3Srb36gZZN{[Xl? MoK2Nk42KM7:TR?= MmHDOkBp NE[wV5dKdmirYnn0bY9vKG:oIFz5ckBxcG:|cHjvdplt[XSrb36gbY4hcHWvYX6gVoVkOSClZXzsd{BifCB{LkWgeW0hcW6ldXLheIVlKG[xcjC2JIhzeyCkeTDX[ZN1\XKwIHLsc5R1cW6pIH3leIhw\A>? MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJ{Mki3O{c,OjV{MkK4O|c9N2F-
human WSU-NHL cells M2Xa[GN6fG:2b4jpZ:Kh[XO|YYm= NHnVfY84OiCq NFfBSVBEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBYW1VvTljMJINmdGy|IHHzd4V{e2WmIHHzJIdzd3e2aDDpcohq[mm2aX;uJIFnfGW{IEeyJIhzeyCkeTDD[YxtXGm2ZYKtS4xwKGy3bXnu[ZNk\W62IHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuNFkh|ryP NU\kXXR[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5NVUzQTFpPkK0PVE2OjlzPD;hQi=>
human SU-DHL6 cells M2nMb2N6fG:2b4jpZ:Kh[XO|YYm= M4nxZlczKGh? Mk[yR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gV3UuTEiONjDj[YxteyCjc4Pld5Nm\CCjczDndo94fGhiaX7obYJqfGmxbjDh[pRmeiB5MjDodpMh[nliQ3XscHRqfGW{LVfsc{BtfW2rbnXzZ4VvfCClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkW4JO69VS5? NYj5N|k1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5NVUzQTFpPkK0PVE2OjlzPD;hQi=>
human DOHH2 cells M{PERWN6fG:2b4jpZ:Kh[XO|YYm= NF7oSZI4OiCq MX3DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDEU2hJOiClZXzsd{Bie3Onc4Pl[EBieyCpcn;3eIghcW6qaXLpeIlwdiCjZoTldkA4OiCqcoOgZpkhS2WubGTpeIVzNUeubzDseY1qdmW|Y3XueEBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjRzIN88UU4> NGP2NXQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEmxOVI6OSd-MkS5NVUzQTF:L3G+
Sf9 cells MnOxSpVv[3Srb36gZZN{[Xl? MYKxJIg> MnHRTY5pcWKrdHnvckBw\iCOWV6tRUBmgHC{ZYPz[YQhcW5iU3[5JINmdGy|IHHmeIVzKDZyIH3pcpMh[nliVGKtSnJGXCCDc4PhfUwhUUN3ME2wMlIh|ryPLh?= NEnZc5k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUm1PFU1Pyd-MkG5OVg2PDd:L3G+
human Ramos cells NIjweW1HfW6ldHnvckBie3OjeR?= M1LpZVEhcA>? M1G0NGlvcGmkaYTpc44hd2ZiQoTrJIlvKGi3bXHuJHJidW:|IHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhWEyFLXfhcY1iOiCyaH;zdIhwenmuYYTpc44h[XRiVInyNVIyPyCjZoTldkAyKGi{IHL5JHdme3Sncn6gZoxwfCCjbnHsfZNqeyxiSVO1NF0yPCCwTT6= M1vRdFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUG1NlkyLz5{NEmxOVI6OTxxYU6=
human Pfeiffer cells MWTGeY5kfGmxbjDhd5NigQ>? NUC1N5EzPzJiaB?= NVfiN214S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hWG[naX\m[ZIh[2WubIOgZZN{\XO|ZXSgZZMh\3Kxd4ToJIlvcGmkaYTpc44h[W[2ZYKgO|IhcHK|IHL5JGNmdGyWaYTldk1IdG9ibIXtbY5me2OnboSgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NkBvVS5? MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDlzNUK5NUc,OjR7MUWyPVE9N2F-
Sf9 cells MmLKSpVv[3Srb36gZZN{[Xl? MmqxNUBp MWDJcohq[mm2aX;uJI9nKGi3bXHuJIZ2dGxvbHXu[5RpKEKWSzDlfJBz\XO|ZXSgbY4hW2Z7IHPlcIx{KHW|aX7nJGZCVS2VcnP0bYRmKHCncITp[IUh[XNic4Xid5Rz[XSnIHHmeIVzKDZyIH3pcpMh[nliVGKtSnJGXCCDc4Phfg+9lCCLQ{WwQVAvPSCwTT6= MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTl3OEW0O{c,OjF7NUi1OFc9N2F-
Sf9 insect cells MXPGeY5kfGmxbjDhd5NigQ>? MWW2NEBucW6| MYnJR|UxKD1iMD6wNFA{KM7:TR?= NV\YN4Z3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmxOFYyOzZpPkK5NVQ3OTN4PD;hQi=>
sf9 cells M3nMbGZ2dmO2aX;uJIF{e2G7 MVrJR|UxKD1iMD6wNFA{KM7:TR?= NYD3OXFiRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke5PVQ4OzZpPkK3PVk1PzN4PD;hQi=>
Sf9 insect cells NW\RN3JWTnWwY4Tpc44h[XO|YYm= M3qyTlYxKG2rboO= MXXJR|UxKD1iMD6wNFA{PCEQvF2= M3rmflxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5OUGyNVc2Lz5{N{mxNlE4PTxxYU6=
Sf9 insect cells NYPVUHg4TnWwY4Tpc44h[XO|YYm= NIGyO5Q3OCCvaX7z MV7JR|UxKD1iMD6wNFA{PCEQvF2= MmPGQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh2M{K5OFYoRjJ6NEOyPVQ3RC:jPh?=
Sf9 insect cells NYHodHdjTnWwY4Tpc44h[XO|YYm= NVXIVZBrPjBibXnudy=> NFXVVZpKSzVyIE2gNE4xODB|NDFOwG0> NV33b2ZQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke5OVYxOzdpPkK3PVU3ODN5PD;hQi=>
Sf9 cells NULrboZZTnWwY4Tpc44h[XO|YYm= NH\4WYM3OCCvaX7z MlLZTWM2OCB;IECuNFAxPCEQvF2= NEOwbXg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MECwOlE1Oyd-M{CwNFYyPDN:L3G+
Sf9 cells M4nLUGZ2dmO2aX;uJIF{e2G7 NEfJNWI3OCCvaX7z M4HDR2lEPTBiPTCwMlAxODVizszN MmmzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF7NUi1OFcoRjJzOUW4OVQ4RC:jPh?=
Ramos cells MX;GeY5kfGmxbjDhd5NigQ>? M{\kU|EhcA>? M{LkSGlEPTBiPTCwMlAxODVizszN NEPHZoo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEK4NFI3OSd-MkiyPFAzPjF:L3G+
Sf9 cells MkX5SpVv[3Srb36gZZN{[Xl? M1jwOlYxKG2rboO= MV7JR|UxKD1iMD6wNFEh|ryP MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODB5N{[wPEc,OzByN{e2NFg9N2F-
Pfeiffer cells NIq2[ZpEgXSxdH;4bYNqfHliYYPzZZk> M3zT[|czKGh? MWLHTVUxKD1iMD6wNFIh|ryP NEfDcpo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEmxOVI6OSd-MkS5NVUzQTF:L3G+
B cells NGjvWJRHfW6ldHnvckBie3OjeR?= M4fPWFEhcA>? M3LMdmlEPTBiPTCwMlAxPDZizszN NIG4SJk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEK5NFk5QCd-M{CyPVA6QDh:L3G+
Sf9 insect cells NVPwNplPTnWwY4Tpc44h[XO|YYm= M{LpPFIhfG9iNkCgcYlvew>? M3LEZWtqKD1iMD6wNFQ5KM7:TR?= M3PGbVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6M{G1OVk4Lz5{OEOxOVU6PzxxYU6=
Ramos cells NV;oN2N1TnWwY4Tpc44h[XO|YYm= MWSxJIg> M2i4PGlEPTBiPTCwMlAxPzVizszN NWL0XG5{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5NVUzQTFpPkK0PVE2OjlzPD;hQi=>
Sf9 insect cells MUHGeY5kfGmxbjDhd5NigQ>? NGPuRok3OCCvaX7z MU\JR|UxKD1iMD6wNFgh|ryP NWP0[3lWRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkizNVU2QTdpPkK4N|E2PTl5PD;hQi=>
TMD8 cells M1zYO2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 M1X5NlczKGh? Mn23TWM2OCB;IECuNFEh|ryP M3f3ZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7N{G1NFI{Lz5{OUexOVAzOzxxYU6=
CD19+ B cells NYXvZYR5TnWwY4Tpc44h[XO|YYm= MVyxJIg> NUX3TYREUUN3MDC9JFAvODF{IN88US=> MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR3N{m4Nkc,Ojl2NUe5PFI9N2F-
Sf9 insect cells MlrXSpVv[3Srb36gZZN{[Xl? NH74NmQ3OCCvaX7z NEC1[G5KSzVyIE2gNE4xOTJizszN NGjSR|g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEOxOVU6Pyd-MkizNVU2QTd:L3G+
Ramos cells MYfGeY5kfGmxbjDhd5NigQ>? NHjyV3MyKGh? NWDzW4xMUUN3MDC9JFAvODF2IN88US=> MnLKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7MUWyPVEoRjJ2OUG1NlkyRC:jPh?=
Sf9 insect cells MoX6SpVv[3Srb36gZZN{[Xl? MojlNUBp MXPJR|UxKD1iMD6wNVQ1KM7:TR?= NUjy[JVxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm3NVUxOjNpPkK5O|E2ODJ|PD;hQi=>
Sf9 insect cells NHiwdGlHfW6ldHnvckBie3OjeR?= M{nEfVYxKG2rboO= NHfafmpKSzVyIE2gNE4xOTZzIN88US=> MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTF2NkGzOkc,OjlzNE[xN|Y9N2F-
HCC827 cells MoXlRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZZN{[Xl? NF32VGk4OiCq NVyxXY85UUN3MDC9JFAvODN7IN88US=> M3;ZblxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6N{O0OVgyLz5{OEezOFU5OTxxYU6=
PC9 cells M33NS2Z2dmO2aX;uJIF{e2G7 Mke3O|IhcA>? MYTHTVUxKD1iMD6wOUDPxE1? Mln0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh{OEKxNlIoRjJ6MkiyNVIzRC:jPh?=
Sf9 cells NVzzSYNSTnWwY4Tpc44h[XO|YYm= MVi2NEBucW6| MmPNTWM2OCB;IECuNUDPxE1? NGG5cos9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MECwOlE1Oyd-M{CwNFYyPDN:L3G+
H3255 cells M4i4XGZ2dmO2aX;uJIF{e2G7 NF2wVGg4OiCq MUPHTVUxKD1iMD6xNUDPxE1? NXHFbmZSRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkiyPFIyOjJpPkK4NlgzOTJ{PD;hQi=>
BaF3 cells M3jBfWZ2dmO2aX;uJIF{e2G7 M{HsPFczKGh? NH3EbodIUTVyIE2gNE4yOiEQvF2= Mkf6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ4M{C1OVMoRjJ4NkOwOVU{RC:jPh?=
BAF3 cells MXrBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? NVnMNW9nPzJiaB?= MVXHTVUxKD1iMD6xNkDPxE1? M2rUXFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6OUW2PVI{Lz5{OEm1OlkzOzxxYU6=
Sf9 insect cells MUnGeY5kfGmxbjDhd5NigQ>? MVK2NEBucW6| NWHnPHBMUUN3MDC9JFAvOTJ|IN88US=> M4rkUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6M{G1OVk4Lz5{OEOxOVU6PzxxYU6=
Sf9 insect cells MoTPSpVv[3Srb36gZZN{[Xl? MVW2NEBucW6| NXjxXWRSUUN3MDC9JFAvOTR4IN88US=> MnjxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh|MUW1PVcoRjJ6M{G1OVk4RC:jPh?=
BAF3 cells MXXGeY5kfGmxbjDhd5NigQ>? NXuzWY9sPzJiaB?= NX\qTZhqT0l3MDC9JFAvOTZizszN NWC3Z5B{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkiyPFIyOjJpPkK4NlgzOTJ{PD;hQi=>
Sf9 cells NWHmW5I2TnWwY4Tpc44h[XO|YYm= NF:4ZVU3OCCvaX7z NF\FZWhKSzVyIE2gNE4zKM7:TR?= MnHlQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF7NUi1OFcoRjJzOUW4OVQ4RC:jPh?=
MV411 cells M4\QS2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Ml[xS2k2OCB;IECuNlUh|ryP M1PGbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6M{G1OVk4Lz5{OEOxOVU6PzxxYU6=
MV4-11 cells MYHBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? MlzGO|IhcA>? NYfqVWFuT0l3MDC9JFAvOzNizszN NXT5SnZRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[2N|A2PTNpPkK2OlMxPTV|PD;hQi=>
MV4-11 cells M1;PO2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 NGD3S5I4OiCq M3W5VmdKPTBiPTCwMlM{KM7:TR?= MmnUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh7NU[5NlMoRjJ6OUW2PVI{RC:jPh?=
DOHH2 cells NFnzTZdEgXSxdH;4bYNqfHliYYPzZZk> NYjodm17PzJiaB?= M3PwVWdKPTBiPTCwMlQyKM7:TR?= MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDlzNUK5NUc,OjR7MUWyPVE9N2F-
HCC827 cells MVrBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? NVvJToNEQTZiaB?= M{jaRWVEPTBiPTCwMlQ2KM7:TR?= MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDh3M{W3OUc,Ojh6NUO1O|U9N2F-
SU-DHL6 cells MX3DfZRwfG:6aXPpeJkh[XO|YYm= M3HF[FczKGh? NVOzVXdzT0l3MDC9JFAvPThizszN NV3XfFR[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5NVUzQTFpPkK0PVE2OjlzPD;hQi=>
M07e cells NX\scHFST3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Ml3zS2k2OCB;IECuOVkh|ryP MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDNzNUW5O{c,Ojh|MUW1PVc9N2F-
NCI-H1975 cells NXfz[ZhQSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[XO|YYm= MVO5OkBp NHPh[lRGSzVyIE2gNE43PCEQvF2= NYLabotQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki4OVM2PzVpPkK4PFU{PTd3PD;hQi=>
SU-DHL-2 cells MnPlS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NI[zeFRIUTVyIE2gNE43PCEQvF2= MmTUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh|MUW1PVcoRjJ6M{G1OVk4RC:jPh?=
HEK293T cells MmjwSpVv[3Srb36gZZN{[Xl? MW[xJIg> NGXlXINKSzVyIE2gNE46KM7:TR?= M{Ppb|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MkiwNlYyLz5{OEK4NFI3OTxxYU6=
Ramos cells MY\BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? M2faOlczKGh? M3XINGlEPTBiPTCwMlkzKM7:TR?= NGC5OXI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUexOVAzOyd-Mkm3NVUxOjN:L3G+
BA/F3 cells NVvvT2tESW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[XO|YYm= M4LFRVczKGh? M13SbGlEPTBiPTCxJO69VQ>? M1m5PFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MkW4OVIyLz5{NkK1PFUzOTxxYU6=
WSU-NHL cells M4Loc2N6fG:2b4jpZ4l1gSCjc4PhfS=> M2LY[|czKGh? MWPHTVUxKD1iMT6wPUDPxE1? NU\NZXlFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5NVUzQTFpPkK0PVE2OjlzPD;hQi=>
NCI-H1975 cells NH:5folHfW6ldHnvckBie3OjeR?= M2TDNFczKGh? NXjZeohxT0l3MDC9JFEvOiEQvF2= MoPOQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh{OEKxNlIoRjJ6MkiyNVIzRC:jPh?=
NCI-H1975 cells NYHucGZjSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[XO|YYm= M4HqNlczKGh? NUDOVFU2UUN3MDC9JFEvOjdizszN NYHj[HNoRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki3N|Q2QDFpPkK4O|M1PThzPD;hQi=>
Raji cells MkXiRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZZN{[Xl? M4HxUFQ5KGh? NXHRT3BnUUN3MDC9JFEvPDlizszN NYrFNWNZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm1OlczQTVpPkK5OVY4Ojl3PD;hQi=>
Pfeiffer cells MkLMS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M{j2dWdKPTBiPTCxMlYh|ryP NHrUdXE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEOxOVU6Pyd-MkizNVU2QTd:L3G+
A431 cells MlfzRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZZN{[Xl? NIH3XVU6PiCq MmTLSWM2OCB;IEKuN|gh|ryP NEKxXJA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEi1N|U4PSd-Mki4OVM2PzV:L3G+
BAF3 cells NYHtc3VJSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[XO|YYm= MnrUO|IhcA>? MoHnS2k2OCB;IEKuOUDPxE1? NYLWZ4hHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki5OVY6OjNpPkK4PVU3QTJ|PD;hQi=>
U937 cells MoHXS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NHm0e41IUTVyIE2gNk46KM7:TR?= NHvndFE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEOxOVU6Pyd-MkizNVU2QTd:L3G+
NB4 cells MmX0S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NVzVenp1T0l3MDC9JFMh|ryP MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDNzNUW5O{c,Ojh|MUW1PVc9N2F-
Ramos cells MoX4S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NYewcZhvT0l3MDC9JFMvPCEQvF2= M{HQclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6M{G1OVk4Lz5{OEOxOVU6PzxxYU6=
SKM1 cells MVLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M4X2RWdKPTBiPTCzMlYh|ryP MlHoQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh|MUW1PVcoRjJ6M{G1OVk4RC:jPh?=
U2932 cells MkjlS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MU\HTVUxKD1iND60JO69VQ>? NHXNenk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEOxOVU6Pyd-MkizNVU2QTd:L3G+
Ramos cells M{i0b2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 M4XYd|czKGh? NVvRcYlmUUN3MDC9JFUvOTRizszN M3PNW|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMEC2NVQ{Lz5|MECwOlE1OzxxYU6=
Ramos cells MWrBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? Mle2OFghcA>? M4PZR2lEPTBiPTC1MlE1KM7:TR?= M1;kTFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5OUW2NFM4Lz5{N{m1OlA{PzxxYU6=
Ramos cells NHnsVHlCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= M1PR[lQ5KGh? NIizRZdKSzVyIE2gOU45QCEQvF2= MmnQQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh2M{K5OFYoRjJ6NEOyPVQ3RC:jPh?=
Ramos cells M4ex[GFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 M2fWdVczKGh? NXjQN2VjUUN3MDC9JFYvPjJizszN NF32cHo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUG0OlE{Pid-MkmxOFYyOzZ:L3G+
K562 cells MlOwRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZZN{[Xl? NF63fmQ1QCCq NVzh[GFbUUN3MDC9JFcvPSEQvF2= NGTjdGc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEC3O|YxQCd-M{CwO|c3ODh:L3G+
HL60 cells M2Lrd2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 NVnnWG9HPDhiaB?= NGTaWo9KSzVyIE2gPEDPxE1? M1PxeFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMEe3OlA5Lz5|MEC3O|YxQDxxYU6=
Ramos cells Ml6yRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZZN{[Xl? MlLMOFghcA>? NFnJT5JKSzVyIE2gPE4yOSEQvF2= MmLqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd7OUS3N|YoRjJ5OUm0O|M3RC:jPh?=
Ramos cells MVTBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? NHe5S4k1QCCq MYfJR|UxKD1iOD6yOkDPxE1? MmrwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl3NkeyPVUoRjJ7NU[3Nlk2RC:jPh?=
OCI-AML3 cells NITNb41Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= MlfsS2k2OCB;IEmuNkDPxE1? NVzaWYVJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkizNVU2QTdpPkK4N|E2PTl5PD;hQi=>
BAF3 cells NHf6TmlEgXSxdH;4bYNqfHliYYPzZZk> M1n1OlczKGh? MlTCS2k2OCB;IEGwJO69VQ>? M3PwelxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NkOwOVU{Lz5{Nk[zNFU2OzxxYU6=
BAF3 cells Mk[1RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZZN{[Xl? NYjXXlQ6PzJiaB?= NHLJT2JIUTVyIE2gNVAh|ryP NIrvNpg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEm1OlkzOyd-Mki5OVY6OjN:L3G+
BAF3 cells MoXsS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MoXLO|IhcA>? NFLscXNIUTVyIE2gNVAh|ryP NFfWU5M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEK4NlEzOid-MkiyPFIyOjJ:L3G+
NAMALWA cells NILibVNCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= M2TQZ|czKGh? NUDLVmxQUUN3MDC9JFExNjR3IN88US=> M3zPRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7MUS2NVM3Lz5{OUG0OlE{PjxxYU6=
Ramos cells MWLBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? NI\SeHA1QCCq MWfJR|UxKD1iMUKuOkDPxE1? M{DZcFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5OUGyNVc2Lz5{N{mxNlE4PTxxYU6=
Raji cells MmHaRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZZN{[Xl? NWfBNWxyPDhiaB?= MWXJR|UxKD1iMUSuNkDPxE1? NFS0TII9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEC3O|YxQCd-M{CwO|c3ODh:L3G+
Raji cells MX\BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? NVTtdoprPDhiaB?= NWXONnhoUUN3MDC9JFE2NjJizszN MkHmQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd7OUS3N|YoRjJ5OUm0O|M3RC:jPh?=
MIAPaCa2 cells MlTQR5l1d3SxeHnjbZR6KGG|c3H5 NYDqWopuOyCmYYnz MnGyTWM2OCB;IEG2MlYh|ryP MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzB5N{KyPEc,OjdyN{eyNlg9N2F-
HeLa cells MULDfZRwfG:6aXPpeJkh[XO|YYm= M32zblMh\GG7cx?= M4\4RWlEPTBiPTCxOk45KM7:TR?= M3PU[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MEe3NlI5Lz5{N{C3O|IzQDxxYU6=
Raji cells MUDBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? NXL4XGNbPDhiaB?= M2XPeWlEPTBiPTCxPU4{KM7:TR?= MlGyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd7MUKxO|UoRjJ5OUGyNVc2RC:jPh?=
Raji cells M37sVmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 M3j0bFQ5KGh? Mof5TWM2OCB;IEG5MlMh|ryP NHLzVXI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OESzNlk1Pid-Mki0N|I6PDZ:L3G+
Raji cells MUDBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? Mk\IO|IhcA>? NW\WTWc1UUN3MDC9JFE6NjVizszN M3fuSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMEC2NVQ{Lz5|MECwOlE1OzxxYU6=
Raji cells M2nHOmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 M3Tm[lQ5KGh? NIr3dldKSzVyIE2gNVkvPSEQvF2= NULGUlQxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke5OVYxOzdpPkK3PVU3ODN5PD;hQi=>
NAMALWA cells MWjBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? MYO3NkBp MV3JR|UxKD1iMUmuOkDPxE1? NWe3dXA6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CwNFYyPDNpPkOwNFA3OTR|PD;hQi=>
A2780 cells NUDqe3FQS3m2b4TvfIlkcXS7IHHzd4F6 MluzN{Bl[Xm| MmWwSWM2OCB;IEKwMlEh|ryP M4C3XFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MEe3NlI5Lz5{N{C3O|IzQDxxYU6=
Raji cells M1j6eGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 NXTU[ZBoPzJiaB?= NWTWbo1yUUN3MDC9JFIxNjh6IN88US=> M2L6OVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7MUS2NVM3Lz5{OUG0OlE{PjxxYU6=
A549 cells NICzTmhCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= M3XiW|czKGh? MU\JR|UxKD1iMkGuO|kh|ryP NYXWNm9ORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki3N|Q2QDFpPkK4O|M1PThzPD;hQi=>
SW480 cells M2nQbmN6fG:2b4jpZ4l1gSCjc4PhfS=> NYrMUodOOyCmYYnz NEP5b|ZKSzVyIE2gNlUvPiEQvF2= MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzB5N{KyPEc,OjdyN{eyNlg9N2F-
Ramos cells MmL5R5l1d3SxeHnjbZR6KGG|c3H5 NIDWdnEzPCCq MoLtTWM2OCB;IEK4Mlch|ryP NGO2O5o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEK3OFY4PSd-MkiyO|Q3PzV:L3G+

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アッセイ
Methods Test Index PMID
Western blot
pEGFR(Tyr1068) / EGFR; 

PubMed: 28061447     


Ibrutinib inhibitory effects on EGFRY1068 auto-phosphorylation in the HCC827 cell line at different time points by removal of drug after 4 h pretreatment.

pBTK / pPLCγ2 / pAKT / pERK / pJNK; 

PubMed: 23940282     


Mino (left panel) or Jeko1 (right panel) cells pretreated with vehicle or ibrutinib 10, 100, or 1000 nM were either stimulated with anti-IgM, CXCL12, or CXCL13 or treated with medium (Med) for 15 minutes and then immunoblotted for pBTK, pPLCγ2, pAKT, pERK, and pJNK.

28061447 23940282
Immunofluorescence
CD11b; 

PubMed: 30231870     


BV2 microglial cells were pretreated with ibrutinib (1 μM) or vehicle (1% DMSO) for 30 min, followed by treatment with LPS (1 μg/ml) or PBS for 5.5 h and immunostaining with an anti-CD11b antibody. Scale bar = 20 μm.

COX-2; 

PubMed: 30231870     


BV2 microglial cells were treated with vehicle (1% DMSO) or ibrutinib (1 μM) for 30 min, followed by PBS or LPS (1 μg/ml) for 5.5 h, and immunocytochemistry was conducted with anti-CD11b and anti-COX-2 antibodies. 

30231870
ELISA
hTNFα; 

PubMed: 26627823     


PBMs were isolated and pretreated with 1, 5, or 10 μm ibrutinib (IB) or left untreated (UT, −). Pretreated PBMs were incubated for 24 h in 96-well plates precoated without (PBS) or with 10 μg/ml whole human IgG. Cleared supernatants were collected and analyzed by ELISA for TNFα (n = 3).

IL-10; 

PubMed: 27792904     


LMP2A-negative (vector.1/.2) and -positive (express LMP2A) B cell lines were incubated in the absence or presence of increasing concentrations of Ibrutinib for 24 hours and supernatants were isolated for analysis using an IL-10 ELISA.

26627823 27792904
体内試験

In a collagen-induced arthritis model, Ibrutinib significantly reduces clinical arthritis scores reflecting paw swelling and joint inflammation by inhibiting B-cell activation. In a MRL-Fas(lpr) lupus model, Ibrutinib reduces renal disease and autoantibody production. [1] In an adoptive transfer TCL1 mouse model of CLL, Ibrutinib (25 mg/kg/day) causes a transient early lymphocytosis, and delays CLL disease progression. [4]

お薦めの試験操作(参考用のみ)

キナーゼ試験:

[1]

- 合併

Kinase Assays :

In vitro kinase IC50 values are measured using 33P filtration binding assay after 1 hour incubation of kinase, 33P-ATP, Ibrutinib, and substrate [0.2 mg/mL poly(EY)(4:1]. Assays are performed at Reaction Biology.
細胞試験:

[2]

- 合併
  • 細胞株: Chronic lymphocytic leukemia (CLL) cells
  • 濃度: 0.01-100 μM
  • 反応時間: 48 hours
  • 実験の流れ:

    MTT (3'[4,5-dimethylthiazol-2-yl]-2,5-diphenyl-tetrazolium bromide) assays are performed to determine cytotoxicity. Briefly, cells (CLL B cells or healthy volunteer T cells or NK cells) are incubated for 48 hours with different concentrations of Ibrutinib, or vehicle control. MTT reagent is then added, and plates are incubated for an additional 20 hours before washing with protamine sulfate in phosphate-buffered saline. Dimethyl sulfoxide is added, and absorbance is measured by spectrophotometry at 540 nm in a Labsystems plate reader. Cell viability is also measured at various time points with the use of annexin/PI flow cytometry. Data are analyzed with Expo-ADC32 software package. Results are expressed as the percentage of total positive cells over untreated control. Experiments examining caspase-dependent apoptosis includes the addition of 100μM Z-VAD.


    (参考用のみ)
動物試験:

[1]

- 合併
  • 動物モデル: MRL-Fas(lpr) lupus model and collagen-induced arthritis model.
  • 投薬量: ≤50 mg/kg
  • 投与方法: Administered via p.o.
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 88 mg/mL (199.77 mM)
Ethanol 45 mg/mL (102.15 mM)
Water Insoluble
体内 左から(NMPから)右の順に溶剤を製品に加えます(文献ではなく、Selleckの実験によるデータ):
5% DMSO+30% PEG 300+5% Tween 80+ddH2O
混合させたのち直ちに使用することを推奨します。
10mg/mL

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程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 440.5
化学式

C25H24N6O2

CAS No. 936563-96-1
Storage powder
in solvent
別名 N/A
Smiles C=CC(=O)N1CCCC(C1)N2C3=NC=NC(=C3C(=N2)C4=CC=C(C=C4)OC5=CC=CC=C5)N

投与溶媒組成計算器(クリア溶液)

ステップ1:実験データを入力してください。(実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します)
投与量 mg/kg 動物平均体重 g 投与体積(動物毎) ul 動物数
ステップ2:投与溶媒の組成を入力してください。(ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください)
% DMSO % % Tween 80 % ddH2O
計算リセット

便利ツール

モル濃度計算器

モル濃度計算器

求めたい質量、体積または濃度を計算してください。

質量 (mg) = 濃度 (mM) x 体積 (mL) x 分子量 (g/mol)

モル濃度計算器方程式

  • 質量
    濃度
    体積
    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SDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備するために必要な希釈率を計算してください。Selleck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 ( 入力 出力 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとSDS/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

質量 濃度 体積 分子量

臨床試験

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04876092 Recruiting Drug: JNJ-67856633|Drug: Ibrutinib Leukemia Lymphocytic Chronic B-Cell|Lymphoma Non-Hodgkin Janssen Research & Development LLC July 28 2021 Phase 1
NCT04665115 Not yet recruiting Drug: Ibrutinib|Other: Quality-of-Life Assessment Asymptomatic COVID-19 Infection Laboratory-Confirmed|B-Cell Neoplasm|Chronic Lymphocytic Leukemia|Chronic Lymphocytic Leukemia/Small Lymphocytic Lymphoma|Mantle Cell Lymphoma|Marginal Zone Lymphoma|Small Lymphocytic Lymphoma|Symptomatic COVID-19 Infection Laboratory-Confirmed|Waldenstrom Macroglobulinemia Academic and Community Cancer Research United|National Cancer Institute (NCI) June 30 2021 Phase 2
NCT04294641 Recruiting Drug: Ibrutinib Chronic GVHD National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) May 10 2021 Phase 2
NCT04514393 Not yet recruiting Drug: Methotrexate|Drug: Ibrutinib|Drug: Temozolomide Primary Central Nervous System Lymphoma|PCNSL|Non Hodgkin Lymphoma Huiqiang Huang|Guangdong 999 Brain Hospital|Nanfang Hospital of Southern Medical University|Xian-Janssen Pharmaceutical Ltd.|Sun Yat-sen University December 1 2020 Phase 2
NCT03679624 Recruiting Drug: Ibrutinib|Drug: Daratumumab Waldenstrom Macroglobulinemia|Waldenstrom''s Disease|Waldenström; Hypergammaglobulinemia|Waldenstrom''s Macroglobulinemia Recurrent|Waldenstrom''s Macroglobulinemia of Lymph Nodes|Waldenstrom''s Macroglobulinaemia Without Mention of Remission|Waldenstrom''s Macroglobulinemia Refractory Weill Medical College of Cornell University|Janssen Scientific Affairs LLC|Mayo Clinic July 30 2020 Phase 2

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

  • * 必須

よくある質問(FAQ)

  • 質問1:

    How to reconstitute the compound S2680 for in vivo studies?

  • 回答:

    For in vivo study, we suggest to use 5% DMSO+30% PEG 300+5% Tween 80+ddH2O up to 10mg/ml.

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