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(423)

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 M1LaSmZ2dmO2aX;uJIF{e2G7 MUKyMlUh|ryP MnPROkBp MX\Jcohq[mm2aX;uJI9nKEy7bjDwbI9{eGixconsZZRqd25iaX6gbJVu[W5iUnXjNUBk\WyuczDheEAzNjVidV2gbY5kfWKjdHXkJIZweiB4IHjyd{BjgSCZZYP0[ZJvKGKub4T0bY5oKG2ndHjv[C=> MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJ{Mki3O{c,OjV{MkK4O|c9N2F-
human WSU-NHL cells MYPDfZRwfG:6aXRCpIF{e2G7 NXvaUZVlPzJiaB?= M1TrOmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHdUXS2QSFygZ4VtdHNiYYPz[ZN{\WRiYYOg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiN{KgbJJ{KGK7IFPlcIxVcXSncj3HcI8hdHWvaX7ld4NmdnRiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT6wPUDPxE1? NF7U[2k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEmxOVI6OSd-MkS5NVUzQTF:L3G+
human SU-DHL6 cells NYPCXFNoS3m2b4TvfIlkyqCjc4PhfS=> MY[3NkBp MVrDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTWU1FUEx4IHPlcIx{KGG|c3Xzd4VlKGG|IHfyc5d1cCCrbnjpZol1cW:wIHHmeIVzKDd{IHjyd{BjgSCFZXzsWIl1\XJvR3zvJIx2dWmwZYPj[Y51KGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwNUig{txONg>? NXjZeFlYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5NVUzQTFpPkK0PVE2OjlzPD;hQi=>
human DOHH2 cells Mk\6R5l1d3SxeHnjxsBie3OjeR?= NVXTUHJYPzJiaB?= MYfDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDEU2hJOiClZXzsd{Bie3Onc4Pl[EBieyCpcn;3eIghcW6qaXLpeIlwdiCjZoTldkA4OiCqcoOgZpkhS2WubGTpeIVzNUeubzDseY1qdmW|Y3XueEBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjRzIN88UU4> M1L6dlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUG1NlkyLz5{NEmxOVI6OTxxYU6=
Sf9 cells M1;Qe2Z2dmO2aX;uJIF{e2G7 Mk\uNUBp MWfJcohq[mm2aX;uJI9nKEy\Tj3BJIV5eHKnc4Pl[EBqdiCVZkmgZ4VtdHNiYX\0[ZIhPjBibXnud{BjgSCWUj3GVmVVKEG|c3H5MEBKSzVyPUCuNkDPxE1w NWPFUlhWRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG5OVg2PDdpPkKxPVU5PTR5PD;hQi=>
human Ramos cells MmC4SpVv[3Srb36gZZN{[Xl? NWXpWlJGOSCq Mo\ITY5pcWKrdHnvckBw\iCEdHugbY4hcHWvYX6gVoFud3NiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBRVENvZ3HtcYEzKHCqb4PwbI9zgWyjdHnvckBifCCWeYKxNlE4KGGodHXyJFEhcHJiYomgW4V{fGW{bjDicI91KGGwYXz5d4l{NCCLQ{WwQVE1KG6PLh?= M2LRRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUG1NlkyLz5{NEmxOVI6OTxxYU6=
human Pfeiffer cells NVjvRpZOTnWwY4Tpc44h[XO|YYm= M4D3d|czKGh? MWDDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDQ[oVq\m[ncjDj[YxteyCjc4Pld5Nm\CCjczDndo94fGhiaX7obYJqfGmxbjDh[pRmeiB5MjDodpMh[nliQ3XscHRqfGW{LVfsc{BtfW2rbnXzZ4VvfCClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1{IH7NMi=> NInVUWc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEmxOVI6OSd-MkS5NVUzQTF:L3G+
Sf9 cells Mn3NSpVv[3Srb36gZZN{[Xl? NXrENJdbOSCq NYjONlJnUW6qaXLpeIlwdiCxZjDoeY1idiCodXzsMYxmdme2aDDCWGsh\XiycnXzd4VlKGmwIGPmPUBk\WyuczD1d4lv\yCIQV2tV5JkfGmmZTDw[ZB1cWSnIHHzJJN2[nO2cnH0[UBi\nSncjC2NEBucW6|IHL5JHRTNU[URWSgRZN{[XoxvJygTWM2OD1yLkWgcm0v M4DLcVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzOUW4OVQ4Lz5{MUm1PFU1PzxxYU6=
Sf9 insect cells MWXGeY5kfGmxbjDhd5NigQ>? MoLXOlAhdWmwcx?= NWHlNZBmUUN3MDC9JFAvODByMzFOwG0> NF7KSIM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUG0OlE{Pid-MkmxOFYyOzZ:L3G+
sf9 cells MV3GeY5kfGmxbjDhd5NigQ>? MY\JR|UxKD1iMD6wNFA{KM7:TR?= NV7hXld2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke5PVQ4OzZpPkK3PVk1PzN4PD;hQi=>
Sf9 insect cells NHjuUVlHfW6ldHnvckBie3OjeR?= MlP0OlAhdWmwcx?= M33oW2lEPTBiPTCwMlAxODN2IN88US=> NFPScJQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{mxNlE4PSd-Mke5NVIyPzV:L3G+
Sf9 insect cells MVHGeY5kfGmxbjDhd5NigQ>? M1zCUVYxKG2rboO= MYLJR|UxKD1iMD6wNFA{PCEQvF2= MoKwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh2M{K5OFYoRjJ6NEOyPVQ3RC:jPh?=
Sf9 insect cells NULoRVIzTnWwY4Tpc44h[XO|YYm= NUP4PGU4PjBibXnudy=> NVHtZ2d4UUN3MDC9JFAvODByM{Sg{txO NXzJNlk6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke5OVYxOzdpPkK3PVU3ODN5PD;hQi=>
Sf9 cells NG[1UHFHfW6ldHnvckBie3OjeR?= M1\ZS|YxKG2rboO= M3jXXGlEPTBiPTCwMlAxODRizszN NEXBOI09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MECwOlE1Oyd-M{CwNFYyPDN:L3G+
Sf9 cells M3PKTmZ2dmO2aX;uJIF{e2G7 NWjERVdiPjBibXnudy=> M4\0XWlEPTBiPTCwMlAxODVizszN NF24cZc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUm1PFU1Pyd-MkG5OVg2PDd:L3G+
Ramos cells Ml7FSpVv[3Srb36gZZN{[Xl? MYWxJIg> NGrIV4pKSzVyIE2gNE4xODB3IN88US=> NYi0Zox5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkiyPFAzPjFpPkK4NlgxOjZzPD;hQi=>
Sf9 cells MU\GeY5kfGmxbjDhd5NigQ>? NEO3[pM3OCCvaX7z MU\JR|UxKD1iMD6wNFEh|ryP M4eyRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMEe3OlA5Lz5|MEC3O|YxQDxxYU6=
Pfeiffer cells NFrIdHZEgXSxdH;4bYNqfHliYYPzZZk> Mm\LO|IhcA>? MV3HTVUxKD1iMD6wNFIh|ryP MoC3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7MUWyPVEoRjJ2OUG1NlkyRC:jPh?=
B cells NXHTPXhXTnWwY4Tpc44h[XO|YYm= MWWxJIg> M1zteGlEPTBiPTCwMlAxPDZizszN NYDSb|RjRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CyPVA6QDhpPkOwNlkxQTh6PD;hQi=>
Sf9 insect cells M3TxdGZ2dmO2aX;uJIF{e2G7 MlK1NkB1dyB4MDDtbY5{ MWDLbUA:KDBwMEC0PEDPxE1? M1jNPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6M{G1OVk4Lz5{OEOxOVU6PzxxYU6=
Ramos cells MnrESpVv[3Srb36gZZN{[Xl? M2G2WFEhcA>? NGjubVlKSzVyIE2gNE4xODd3IN88US=> NVrFZYNNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5NVUzQTFpPkK0PVE2OjlzPD;hQi=>
Sf9 insect cells MXfGeY5kfGmxbjDhd5NigQ>? NF7HSFI3OCCvaX7z M33OPGlEPTBiPTCwMlAxQCEQvF2= NIrFeWw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEOxOVU6Pyd-MkizNVU2QTd:L3G+
TMD8 cells M1j0W2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 M2jl[lczKGh? Moj4TWM2OCB;IECuNFEh|ryP M{j2VVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7N{G1NFI{Lz5{OUexOVAzOzxxYU6=
CD19+ B cells M174OGZ2dmO2aX;uJIF{e2G7 NEHPOFkyKGh? MkjETWM2OCB;IECuNFEzKM7:TR?= NGHsdXE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUS1O|k5Oid-Mkm0OVc6QDJ:L3G+
Sf9 insect cells MXTGeY5kfGmxbjDhd5NigQ>? MWC2NEBucW6| MVzJR|UxKD1iMD6wNVIh|ryP Mn;PQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh|MUW1PVcoRjJ6M{G1OVk4RC:jPh?=
Ramos cells NY\VTWtxTnWwY4Tpc44h[XO|YYm= NUXVSWQ2OSCq NH;OOlZKSzVyIE2gNE4xOTRizszN M3PH[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUG1NlkyLz5{NEmxOVI6OTxxYU6=
Sf9 insect cells M{jMNWZ2dmO2aX;uJIF{e2G7 Mn;wNUBp MVTJR|UxKD1iMD6wNVQ1KM7:TR?= MlezQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl5MUWwNlMoRjJ7N{G1NFI{RC:jPh?=
Sf9 insect cells Mnu1SpVv[3Srb36gZZN{[Xl? NIXXbnY3OCCvaX7z NXfPVWp{UUN3MDC9JFAvODF4MTFOwG0> MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTF2NkGzOkc,OjlzNE[xN|Y9N2F-
HCC827 cells M3TxeWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 MY[3NkBp MUPJR|UxKD1iMD6wN|kh|ryP MknWQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh5M{S1PFEoRjJ6N{O0OVgyRC:jPh?=
PC9 cells NHvHOZpHfW6ldHnvckBie3OjeR?= M2jJdFczKGh? M3LabmdKPTBiPTCwMlA2KM7:TR?= MkHxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh{OEKxNlIoRjJ6MkiyNVIzRC:jPh?=
Sf9 cells M13SUWZ2dmO2aX;uJIF{e2G7 NYq5Z5Z{PjBibXnudy=> M2fNZ2lEPTBiPTCwMlEh|ryP MkXmQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzByME[xOFMoRjNyMEC2NVQ{RC:jPh?=
H3255 cells MnfBSpVv[3Srb36gZZN{[Xl? MoLlO|IhcA>? Mlz2S2k2OCB;IECuNVEh|ryP NE\zNlQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEK4NlEzOid-MkiyPFIyOjJ:L3G+
BaF3 cells MoruSpVv[3Srb36gZZN{[Xl? MmnzO|IhcA>? M3L0bmdKPTBiPTCwMlEzKM7:TR?= NITGdnY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nk[zNFU2Oyd-Mk[2N|A2PTN:L3G+
BAF3 cells Mke0RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZZN{[Xl? NG\2SmU4OiCq M2fMT2dKPTBiPTCwMlEzKM7:TR?= Ml7PQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh7NU[5NlMoRjJ6OUW2PVI{RC:jPh?=
Sf9 insect cells M4TiXWZ2dmO2aX;uJIF{e2G7 MXy2NEBucW6| M1LldmlEPTBiPTCwMlEzOyEQvF2= MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDNzNUW5O{c,Ojh|MUW1PVc9N2F-
Sf9 insect cells NXnX[GpDTnWwY4Tpc44h[XO|YYm= M4qyS|YxKG2rboO= M4HFeGlEPTBiPTCwMlE1PiEQvF2= M1vQUFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6M{G1OVk4Lz5{OEOxOVU6PzxxYU6=
BAF3 cells MWXGeY5kfGmxbjDhd5NigQ>? MlP6O|IhcA>? MkThS2k2OCB;IECuNVYh|ryP M2DyUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MkiyNVIzLz5{OEK4NlEzOjxxYU6=
Sf9 cells NYLiSFdsTnWwY4Tpc44h[XO|YYm= MVi2NEBucW6| MYfJR|UxKD1iMD6yJO69VQ>? NXnuRmR5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG5OVg2PDdpPkKxPVU5PTR5PD;hQi=>
MV411 cells NVnLU3p1T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Mn23S2k2OCB;IECuNlUh|ryP M1XRbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6M{G1OVk4Lz5{OEOxOVU6PzxxYU6=
MV4-11 cells NIrJSm9CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= MlzOO|IhcA>? NX;RTHhkT0l3MDC9JFAvOzNizszN MnHyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ4M{C1OVMoRjJ4NkOwOVU{RC:jPh?=
MV4-11 cells MXzBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? M2r4R|czKGh? NVjJbYJ1T0l3MDC9JFAvOzNizszN Mn3UQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh7NU[5NlMoRjJ6OUW2PVI{RC:jPh?=
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HCC827 cells NELIWnNCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= MmPzPVYhcA>? MYnFR|UxKD1iMD60OUDPxE1? MojhQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh6NUO1O|UoRjJ6OEWzOVc2RC:jPh?=
SU-DHL6 cells NYG0UpY4S3m2b4TvfIlkcXS7IHHzd4F6 NHz6XXY4OiCq NI\4[XpIUTVyIE2gNE42QCEQvF2= M3\Ec|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUG1NlkyLz5{NEmxOVI6OTxxYU6=
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NCI-H1975 cells MXvBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? M4O1d|k3KGh? NFrTcGNGSzVyIE2gNE43PCEQvF2= NYT2fYVURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki4OVM2PzVpPkK4PFU{PTd3PD;hQi=>
SU-DHL-2 cells M3raWGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MnW4S2k2OCB;IECuOlQh|ryP MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDNzNUW5O{c,Ojh|MUW1PVc9N2F-
HEK293T cells MojhSpVv[3Srb36gZZN{[Xl? MYCxJIg> MoH1TWM2OCB;IECuPUDPxE1? NILpXHk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEK4NFI3OSd-MkiyPFAzPjF:L3G+
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NCI-H1975 cells M3W3ZWZ2dmO2aX;uJIF{e2G7 M2TOSVczKGh? NV2xOWt2T0l3MDC9JFEvOiEQvF2= NFzYXGE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEK4NlEzOid-MkiyPFIyOjJ:L3G+
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Raji cells M{S0PGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 MWe0PEBp NGi3UopKSzVyIE2gNU41QSEQvF2= M3zvTlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NU[3Nlk2Lz5{OUW2O|I6PTxxYU6=
Pfeiffer cells NGi3WmNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NHvJeWZIUTVyIE2gNU43KM7:TR?= M3fmXVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6M{G1OVk4Lz5{OEOxOVU6PzxxYU6=
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BAF3 cells NVHrbYhmSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[XO|YYm= M17yTFczKGh? M3HJXmdKPTBiPTCyMlUh|ryP M2H3OFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6OUW2PVI{Lz5{OEm1OlkzOzxxYU6=
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NB4 cells M{fXR2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MkTMS2k2OCB;IEOg{txO NWHTV3ViRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkizNVU2QTdpPkK4N|E2PTl5PD;hQi=>
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U2932 cells M2q2[Gdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NGfNZXhIUTVyIE2gOE41KM7:TR?= M3WweFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6M{G1OVk4Lz5{OEOxOVU6PzxxYU6=
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Ramos cells M1r0[mFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 MXq0PEBp Ml35TWM2OCB;IEWuNVQh|ryP NGWy[Zg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{m1OlA{Pyd-Mke5OVYxOzd:L3G+
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NAMALWA cells NIrjbI5CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= MXK3NkBp NWrIbnU5UUN3MDC9JFExNjR3IN88US=> MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTF2NkGzOkc,OjlzNE[xN|Y9N2F-
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Raji cells M4XQ[WFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 M3LiUlQ5KGh? M2PBemlEPTBiPTCxOE4zKM7:TR?= NHvRbGs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEC3O|YxQCd-M{CwO|c3ODh:L3G+
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MIAPaCa2 cells NILBb4pEgXSxdH;4bYNqfHliYYPzZZk> MW[zJIRigXN? MVfJR|UxKD1iMU[uOkDPxE1? MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzB5N{KyPEc,OjdyN{eyNlg9N2F-
HeLa cells NVPQTGtuS3m2b4TvfIlkcXS7IHHzd4F6 MV6zJIRigXN? M4\HUWlEPTBiPTCxOk45KM7:TR?= MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzB5N{KyPEc,OjdyN{eyNlg9N2F-
Raji cells MXTBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? MYW0PEBp M2nSRWlEPTBiPTCxPU4{KM7:TR?= M1fRVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5OUGyNVc2Lz5{N{mxNlE4PTxxYU6=
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Raji cells MV\BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? M37mXVczKGh? M1TpfGlEPTBiPTCxPU42KM7:TR?= Mle3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzByME[xOFMoRjNyMEC2NVQ{RC:jPh?=
Raji cells M1\mb2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 MWC0PEBp M3nub2lEPTBiPTCxPU42KM7:TR?= NX3YZm1bRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke5OVYxOzdpPkK3PVU3ODN5PD;hQi=>
NAMALWA cells M4TxSmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 NH7WU5M4OiCq MWnJR|UxKD1iMUmuOkDPxE1? MoLoQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzByME[xOFMoRjNyMEC2NVQ{RC:jPh?=
A2780 cells MmDzR5l1d3SxeHnjbZR6KGG|c3H5 MlO0N{Bl[Xm| MUHFR|UxKD1iMkCuNUDPxE1? NWD1bFBIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkewO|czOjhpPkK3NFc4OjJ6PD;hQi=>
Raji cells NIXoWIlCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= NF24e2s4OiCq M{XOeWlEPTBiPTCyNE45QCEQvF2= M4XKV|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7MUS2NVM3Lz5{OUG0OlE{PjxxYU6=
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SW480 cells NWPyO2RRS3m2b4TvfIlkcXS7IHHzd4F6 MXKzJIRigXN? MkDBTWM2OCB;IEK1MlYh|ryP M3vKbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MEe3NlI5Lz5{N{C3O|IzQDxxYU6=
Ramos cells MWfDfZRwfG:6aXPpeJkh[XO|YYm= M2\HT|I1KGh? NUP4W3JRUUN3MDC9JFI5NjdizszN M2TrZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6Mke0Olc2Lz5{OEK3OFY4PTxxYU6=

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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

質量 濃度 体積 分子量

臨床試験

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04294641 Recruiting Drug: Ibrutinib Chronic GVHD National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) January 5 2021 Phase 2
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) December 31 2020 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

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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