Ibrutinib (PCI-32765)

For research use only.

Catalog No.S2680

447 publications

Ibrutinib (PCI-32765) Chemical Structure

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. Ibrutinib is applicable as a Btk ligand in the synthesis of a series of PROTACs including P13I.

Selleck's Ibrutinib (PCI-32765) has been cited by 447 publications

Purity & Quality Control

Choose Selective Target Protein Ligand Inhibitors

Biological Activity

Description 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. Ibrutinib is applicable as a Btk ligand in the synthesis of a series of PROTACs including P13I.
Targets
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
In vitro

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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human Rec1 cells MUjGeY5kfGmxbjDhd5NigQ>? M3OxUlIvPSEQvF2= Mlu2OkBp MWnJcohq[mm2aX;uJI9nKEy7bjDwbI9{eGixconsZZRqd25iaX6gbJVu[W5iUnXjNUBk\WyuczDheEAzNjVidV2gbY5kfWKjdHXkJIZweiB4IHjyd{BjgSCZZYP0[ZJvKGKub4T0bY5oKG2ndHjv[C=> NHTHUXE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUKyNlg4Pyd-MkWyNlI5Pzd:L3G+
human WSU-NHL cells Mlz0R5l1d3SxeHnjxsBie3OjeR?= M3faWFczKGh? NHvQdZFEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBYW1VvTljMJINmdGy|IHHzd4V{e2WmIHHzJIdzd3e2aDDpcohq[mm2aX;uJIFnfGW{IEeyJIhzeyCkeTDD[YxtXGm2ZYKtS4xwKGy3bXnu[ZNk\W62IHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuNFkh|ryP MkXzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7MUWyPVEoRjJ2OUG1NlkyRC:jPh?=
human SU-DHL6 cells M17JO2N6fG:2b4jpZ:Kh[XO|YYm= M3T5Z|czKGh? M4[wWWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHNWNUSKTE[gZ4VtdHNiYYPz[ZN{\WRiYYOg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiN{KgbJJ{KGK7IFPlcIxVcXSncj3HcI8hdHWvaX7ld4NmdnRiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD61PEDPxE1w NWrpeFUzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5NVUzQTFpPkK0PVE2OjlzPD;hQi=>
human DOHH2 cells NWrkOHNjS3m2b4TvfIlkyqCjc4PhfS=> MlHHO|IhcA>? NV7Bd5o5S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hTE:KSEKgZ4VtdHNiYYPz[ZN{\WRiYYOg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiN{KgbJJ{KGK7IFPlcIxVcXSncj3HcI8hdHWvaX7ld4NmdnRiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD60NUDPxE1w NXrtcohtRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5NVUzQTFpPkK0PVE2OjlzPD;hQi=>
Sf9 cells NVXMbo5YTnWwY4Tpc44h[XO|YYm= NF;5cXQyKGh? M1zhR2lvcGmkaYTpc44hd2ZiTGnOMWEh\XiycnXzd4VlKGmwIGPmPUBk\WyuczDh[pRmeiB4MDDtbY5{KGK7IGTSMWZTTVRiQYPzZZktKEmFNUC9NE4zKM7:TT6= MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTl3OEW0O{c,OjF7NUi1OFc9N2F-
human Ramos cells Mn:1SpVv[3Srb36gZZN{[Xl? NXOzfHpVOSCq MkD6TY5pcWKrdHnvckBw\iCEdHugbY4hcHWvYX6gVoFud3NiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBRVENvZ3HtcYEzKHCqb4PwbI9zgWyjdHnvckBifCCWeYKxNlE4KGGodHXyJFEhcHJiYomgW4V{fGW{bjDicI91KGGwYXz5d4l{NCCLQ{WwQVE1KG6PLh?= MlvIQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7MUWyPVEoRjJ2OUG1NlkyRC:jPh?=
human Pfeiffer cells M3n6T2Z2dmO2aX;uJIF{e2G7 NX7xN2czPzJiaB?= MVzDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDQ[oVq\m[ncjDj[YxteyCjc4Pld5Nm\CCjczDndo94fGhiaX7obYJqfGmxbjDh[pRmeiB5MjDodpMh[nliQ3XscHRqfGW{LVfsc{BtfW2rbnXzZ4VvfCClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1{IH7NMi=> M1zZdVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUG1NlkyLz5{NEmxOVI6OTxxYU6=
Sf9 cells NUfKfWtiTnWwY4Tpc44h[XO|YYm= NGDRVmEyKGh? MkD3TY5pcWKrdHnvckBw\iCqdX3hckBnfWyuLXzlcod1cCCEVFug[ZhxemW|c3XkJIlvKFOoOTDj[YxteyC3c3nu[{BHSU1vU4LjeIll\SCyZYD0bYRmKGG|IIP1ZpN1emG2ZTDh[pRmeiB4MDDtbY5{KGK7IGTSMWZTTVRiQYPzZZnwxIxiSVO1NF0xNjVibl2u MmrIQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF7NUi1OFcoRjJzOUW4OVQ4RC:jPh?=
Sf9 insect cells NHfTR2dHfW6ldHnvckBie3OjeR?= MmnXOlAhdWmwcx?= Ml;xTWM2OCB;IECuNFAxOyEQvF2= NIXMW4k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUG0OlE{Pid-MkmxOFYyOzZ:L3G+
sf9 cells NFvHcJFHfW6ldHnvckBie3OjeR?= M2G3SGlEPTBiPTCwMlAxODNizszN M3XwTlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5OUm0O|M3Lz5{N{m5OFc{PjxxYU6=
Sf9 insect cells M{WwV2Z2dmO2aX;uJIF{e2G7 M3[wUVYxKG2rboO= M4LGO2lEPTBiPTCwMlAxODN2IN88US=> MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzlzMkG3OUc,Ojd7MUKxO|U9N2F-
Sf9 insect cells NHTifHVHfW6ldHnvckBie3OjeR?= MoXjOlAhdWmwcx?= M4DUVGlEPTBiPTCwMlAxODN2IN88US=> NUHze2NGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki0N|I6PDZpPkK4OFMzQTR4PD;hQi=>
Sf9 insect cells MX\GeY5kfGmxbjDhd5NigQ>? NVHpWY1oPjBibXnudy=> M3ziWGlEPTBiPTCwMlAxODN2IN88US=> M3Xie|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5OUW2NFM4Lz5{N{m1OlA{PzxxYU6=
Sf9 cells MVXGeY5kfGmxbjDhd5NigQ>? NH3jbIw3OCCvaX7z NILoNZNKSzVyIE2gNE4xODB2IN88US=> NW\6eGRiRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CwNFYyPDNpPkOwNFA3OTR|PD;hQi=>
Sf9 cells M1\2WWZ2dmO2aX;uJIF{e2G7 MYO2NEBucW6| MUnJR|UxKD1iMD6wNFA2KM7:TR?= MljUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF7NUi1OFcoRjJzOUW4OVQ4RC:jPh?=
Ramos cells MY\GeY5kfGmxbjDhd5NigQ>? MYKxJIg> MoH5TWM2OCB;IECuNFAxPSEQvF2= MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDJ6MEK2NUc,Ojh{OECyOlE9N2F-
Sf9 cells M4nOOWZ2dmO2aX;uJIF{e2G7 NYj2WXB[PjBibXnudy=> M4nPXmlEPTBiPTCwMlAxOSEQvF2= NX\1enVPRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CwO|c3ODhpPkOwNFc4PjB6PD;hQi=>
Pfeiffer cells Mn;uR5l1d3SxeHnjbZR6KGG|c3H5 MlKwO|IhcA>? MWDHTVUxKD1iMD6wNFIh|ryP MorZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7MUWyPVEoRjJ2OUG1NlkyRC:jPh?=
B cells Ml3XSpVv[3Srb36gZZN{[Xl? MUKxJIg> M{TEc2lEPTBiPTCwMlAxPDZizszN NHzhbYY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEK5NFk5QCd-M{CyPVA6QDh:L3G+
Sf9 insect cells M{O2UmZ2dmO2aX;uJIF{e2G7 NYjvWmd{OiC2bzC2NEBucW6| MYfLbUA:KDBwMEC0PEDPxE1? M4npUFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6M{G1OVk4Lz5{OEOxOVU6PzxxYU6=
Ramos cells MYfGeY5kfGmxbjDhd5NigQ>? NUXiTFRiOSCq NGTKNotKSzVyIE2gNE4xODd3IN88US=> NY\mbohxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5NVUzQTFpPkK0PVE2OjlzPD;hQi=>
Sf9 insect cells NUjsdmY1TnWwY4Tpc44h[XO|YYm= NGPie2M3OCCvaX7z M1vOOmlEPTBiPTCwMlAxQCEQvF2= M1;Qe|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6M{G1OVk4Lz5{OEOxOVU6PzxxYU6=
TMD8 cells NIjpVVlCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= NIDyPFQ4OiCq NX7KT2pVUUN3MDC9JFAvODFizszN NW\0cpJYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm3NVUxOjNpPkK5O|E2ODJ|PD;hQi=>
CD19+ B cells NGLSeXpHfW6ldHnvckBie3OjeR?= NI\wOlMyKGh? MoHoTWM2OCB;IECuNFEzKM7:TR?= M3TI[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEW3PVgzLz5{OUS1O|k5OjxxYU6=
Sf9 insect cells M1nhWWZ2dmO2aX;uJIF{e2G7 NIfYSXI3OCCvaX7z MlvaTWM2OCB;IECuNFEzKM7:TR?= M1LEOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6M{G1OVk4Lz5{OEOxOVU6PzxxYU6=
Ramos cells M4nkRWZ2dmO2aX;uJIF{e2G7 NVPxUmczOSCq NUTJUXlpUUN3MDC9JFAvODF2IN88US=> M2Tae|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUG1NlkyLz5{NEmxOVI6OTxxYU6=
Sf9 insect cells MWfGeY5kfGmxbjDhd5NigQ>? NVK1O5FZOSCq Ml;6TWM2OCB;IECuNFE1PCEQvF2= MkH2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl5MUWwNlMoRjJ7N{G1NFI{RC:jPh?=
Sf9 insect cells NHm4XpRHfW6ldHnvckBie3OjeR?= Ml;vOlAhdWmwcx?= MUjJR|UxKD1iMD6wNVYyKM7:TR?= NH[yflQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUG0OlE{Pid-MkmxOFYyOzZ:L3G+
HCC827 cells MmLHRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZZN{[Xl? NY\xRnl7PzJiaB?= MYXJR|UxKD1iMD6wN|kh|ryP MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDd|NEW4NUc,Ojh5M{S1PFE9N2F-
PC9 cells NFu2T3NHfW6ldHnvckBie3OjeR?= MmjtO|IhcA>? M2fqbGdKPTBiPTCwMlA2KM7:TR?= NH3EN3A9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEK4NlEzOid-MkiyPFIyOjJ:L3G+
Sf9 cells NILWVFlHfW6ldHnvckBie3OjeR?= NHLBb4c3OCCvaX7z NF74OpNKSzVyIE2gNE4yKM7:TR?= M{fwbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMEC2NVQ{Lz5|MECwOlE1OzxxYU6=
H3255 cells MlfYSpVv[3Srb36gZZN{[Xl? M3TqUVczKGh? NHWzZZhIUTVyIE2gNE4yOSEQvF2= NYW3XHo4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkiyPFIyOjJpPkK4NlgzOTJ{PD;hQi=>
BaF3 cells M{f2ZmZ2dmO2aX;uJIF{e2G7 NFz6PXE4OiCq MXrHTVUxKD1iMD6xNkDPxE1? MmX3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ4M{C1OVMoRjJ4NkOwOVU{RC:jPh?=
BAF3 cells MoW2RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZZN{[Xl? NFzkcWo4OiCq NGL0WphIUTVyIE2gNE4yOiEQvF2= NGXqVXI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEm1OlkzOyd-Mki5OVY6OjN:L3G+
Sf9 insect cells NXfqZ2pYTnWwY4Tpc44h[XO|YYm= NHPldJI3OCCvaX7z NFPCS|lKSzVyIE2gNE4yOjNizszN MluxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh|MUW1PVcoRjJ6M{G1OVk4RC:jPh?=
Sf9 insect cells NW\m[3pMTnWwY4Tpc44h[XO|YYm= MXu2NEBucW6| NFnCdo9KSzVyIE2gNE4yPDZizszN NH[yfm89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEOxOVU6Pyd-MkizNVU2QTd:L3G+
BAF3 cells NH\DNVdHfW6ldHnvckBie3OjeR?= M{LBe|czKGh? NELSNXpIUTVyIE2gNE4yPiEQvF2= NWGzTW1wRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkiyPFIyOjJpPkK4NlgzOTJ{PD;hQi=>
Sf9 cells MX3GeY5kfGmxbjDhd5NigQ>? MnKzOlAhdWmwcx?= NEPMNmRKSzVyIE2gNE4zKM7:TR?= M1i4dlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzOUW4OVQ4Lz5{MUm1PFU1PzxxYU6=
MV411 cells MWPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MoHmS2k2OCB;IECuNlUh|ryP M2naXFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6M{G1OVk4Lz5{OEOxOVU6PzxxYU6=
MV4-11 cells MUPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? M1HwUVczKGh? MWLHTVUxKD1iMD6zN{DPxE1? NH\tbVk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nk[zNFU2Oyd-Mk[2N|A2PTN:L3G+
MV4-11 cells NVzlXI9sSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[XO|YYm= NHLnO4U4OiCq NGjte|BIUTVyIE2gNE4{OyEQvF2= MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDl3NkmyN{c,Ojh7NU[5NlM9N2F-
DOHH2 cells M2PJR2N6fG:2b4jpZ4l1gSCjc4PhfS=> M1fJNFczKGh? M{XTbWdKPTBiPTCwMlQyKM7:TR?= NU[3O3VtRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5NVUzQTFpPkK0PVE2OjlzPD;hQi=>
HCC827 cells NIPDdHJCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= MV25OkBp NVPTbXBbTUN3MDC9JFAvPDVizszN M4XZ[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6OEWzOVc2Lz5{OEi1N|U4PTxxYU6=
SU-DHL6 cells NV24epk{S3m2b4TvfIlkcXS7IHHzd4F6 NEP0NJQ4OiCq M1[yNGdKPTBiPTCwMlU5KM7:TR?= NGDGcnc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEmxOVI6OSd-MkS5NVUzQTF:L3G+
M07e cells M4rqbmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MWHHTVUxKD1iMD61PUDPxE1? MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDNzNUW5O{c,Ojh|MUW1PVc9N2F-
NCI-H1975 cells NW\MbZFCSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[XO|YYm= M3L3eFk3KGh? MoThSWM2OCB;IECuOlQh|ryP NFvxe249[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEi1N|U4PSd-Mki4OVM2PzV:L3G+
SU-DHL-2 cells M13sNWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NXPlRmQ4T0l3MDC9JFAvPjRizszN MnHmQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh|MUW1PVcoRjJ6M{G1OVk4RC:jPh?=
HEK293T cells NYHMSWxsTnWwY4Tpc44h[XO|YYm= MUWxJIg> M1jjTWlEPTBiPTCwMlkh|ryP M175RVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MkiwNlYyLz5{OEK4NFI3OTxxYU6=
Ramos cells NIi5d|dCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= MU[3NkBp NULMeJdmUUN3MDC9JFAvQTJizszN NXe2V5BXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm3NVUxOjNpPkK5O|E2ODJ|PD;hQi=>
BA/F3 cells NIDMTXFCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= MV63NkBp MYLJR|UxKD1iMTFOwG0> M4e0ZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MkW4OVIyLz5{NkK1PFUzOTxxYU6=
WSU-NHL cells NFXDO4pEgXSxdH;4bYNqfHliYYPzZZk> MYG3NkBp MlnFS2k2OCB;IEGuNFkh|ryP NFq5WZg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEmxOVI6OSd-MkS5NVUzQTF:L3G+
NCI-H1975 cells NF;vN|JHfW6ldHnvckBie3OjeR?= NF\ZdXA4OiCq NYT5Z2FtT0l3MDC9JFEvOiEQvF2= Mk\UQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh{OEKxNlIoRjJ6MkiyNVIzRC:jPh?=
NCI-H1975 cells M4jXeWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 NVPO[4lrPzJiaB?= NH;SRYJKSzVyIE2gNU4zPyEQvF2= NXuxU4FTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki3N|Q2QDFpPkK4O|M1PThzPD;hQi=>
Raji cells MV;BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? MYC0PEBp M4jJZmlEPTBiPTCxMlQ6KM7:TR?= MoPmQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl3NkeyPVUoRjJ7NU[3Nlk2RC:jPh?=
Pfeiffer cells MULHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MmftS2k2OCB;IEGuOkDPxE1? MknsQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh|MUW1PVcoRjJ6M{G1OVk4RC:jPh?=
A431 cells M1zlWmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 M{n2Slk3KGh? NYDXeIFoTUN3MDC9JFIvOzhizszN MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDh3M{W3OUc,Ojh6NUO1O|U9N2F-
BAF3 cells MXzBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? MXu3NkBp M1rvRmdKPTBiPTCyMlUh|ryP NE\wTGo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEm1OlkzOyd-Mki5OVY6OjN:L3G+
U937 cells MWrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NUf5VIJnT0l3MDC9JFIvQSEQvF2= M17PWVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6M{G1OVk4Lz5{OEOxOVU6PzxxYU6=
NB4 cells NEniRWpIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NHrJVGhIUTVyIE2gN{DPxE1? MljNQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh|MUW1PVcoRjJ6M{G1OVk4RC:jPh?=
Ramos cells NX;kV4NNT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NV25T4xRT0l3MDC9JFMvPCEQvF2= NX;CO5IxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkizNVU2QTdpPkK4N|E2PTl5PD;hQi=>
SKM1 cells NGjEOnBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NGLa[|JIUTVyIE2gN{43KM7:TR?= M1\I[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6M{G1OVk4Lz5{OEOxOVU6PzxxYU6=
U2932 cells M3TZZ2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NHXlSYJIUTVyIE2gOE41KM7:TR?= MkPyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh|MUW1PVcoRjJ6M{G1OVk4RC:jPh?=
Ramos cells MnPDRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZZN{[Xl? MoPaO|IhcA>? NFjoU3VKSzVyIE2gOU4yPCEQvF2= NFqxSYg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MECwOlE1Oyd-M{CwNFYyPDN:L3G+
Ramos cells MnPhRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZZN{[Xl? Mof6OFghcA>? MX;JR|UxKD1iNT6xOEDPxE1? MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzl3NkCzO{c,Ojd7NU[wN|c9N2F-
Ramos cells MVnBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? MUK0PEBp NEG1Z2VKSzVyIE2gOU45QCEQvF2= NG\tVWg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OESzNlk1Pid-Mki0N|I6PDZ:L3G+
Ramos cells NHfVXFVCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= MmPUO|IhcA>? Mlr3TWM2OCB;IE[uOlIh|ryP MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTF2NkGzOkc,OjlzNE[xN|Y9N2F-
K562 cells NFvEXIZCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= MkjLOFghcA>? MX;JR|UxKD1iNz61JO69VQ>? M4KxPVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMEe3OlA5Lz5|MEC3O|YxQDxxYU6=
HL60 cells MWfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? Mlv2OFghcA>? NH3pb21KSzVyIE2gPEDPxE1? NGjhbVc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEC3O|YxQCd-M{CwO|c3ODh:L3G+
Ramos cells Mn\jRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZZN{[Xl? Ml2yOFghcA>? MWrJR|UxKD1iOD6xNUDPxE1? NVHSfmF5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke5PVQ4OzZpPkK3PVk1PzN4PD;hQi=>
Ramos cells MUDBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? NIPH[Y41QCCq MWLJR|UxKD1iOD6yOkDPxE1? MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTV4N{K5OUc,Ojl3NkeyPVU9N2F-
OCI-AML3 cells NGnmUGdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3XLVWdKPTBiPTC5MlIh|ryP M2D5cVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6M{G1OVk4Lz5{OEOxOVU6PzxxYU6=
BAF3 cells NUXEZYlSS3m2b4TvfIlkcXS7IHHzd4F6 MYW3NkBp NUfzWnlDT0l3MDC9JFExKM7:TR?= M1u5flxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NkOwOVU{Lz5{Nk[zNFU2OzxxYU6=
BAF3 cells M4P0PWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 NES2cVM4OiCq MnSwS2k2OCB;IEGwJO69VQ>? NVP2VVZERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki5OVY6OjNpPkK4PVU3QTJ|PD;hQi=>
BAF3 cells MVTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MWq3NkBp Mnu5S2k2OCB;IEGwJO69VQ>? NF7VVZY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEK4NlEzOid-MkiyPFIyOjJ:L3G+
NAMALWA cells MVjBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? NU\QcI11PzJiaB?= NVvvXXduUUN3MDC9JFExNjR3IN88US=> M3myZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7MUS2NVM3Lz5{OUG0OlE{PjxxYU6=
Ramos cells NUTp[W92SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[XO|YYm= NF;l[Ws1QCCq Mo\ZTWM2OCB;IEGyMlYh|ryP M1jTZ|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5OUGyNVc2Lz5{N{mxNlE4PTxxYU6=
Raji cells NYO2VIRXSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[XO|YYm= NUPyVW5nPDhiaB?= MY\JR|UxKD1iMUSuNkDPxE1? M1G4XVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMEe3OlA5Lz5|MEC3O|YxQDxxYU6=
Raji cells M{C1WWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 NG\3TFA1QCCq Mlr5TWM2OCB;IEG1MlIh|ryP MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzl7NEezOkc,Ojd7OUS3N|Y9N2F-
MIAPaCa2 cells NYntPYZwS3m2b4TvfIlkcXS7IHHzd4F6 Mkf5N{Bl[Xm| MmjRTWM2OCB;IEG2MlYh|ryP M3z1VFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MEe3NlI5Lz5{N{C3O|IzQDxxYU6=
HeLa cells MlfwR5l1d3SxeHnjbZR6KGG|c3H5 MlHUN{Bl[Xm| MWfJR|UxKD1iMU[uPEDPxE1? M3HmbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MEe3NlI5Lz5{N{C3O|IzQDxxYU6=
Raji cells M4\ZV2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 MV:0PEBp M4nxd2lEPTBiPTCxPU4{KM7:TR?= MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzlzMkG3OUc,Ojd7MUKxO|U9N2F-
Raji cells MVrBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? NYrZXYJJPDhiaB?= MWDJR|UxKD1iMUmuN{DPxE1? NF;5XJA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OESzNlk1Pid-Mki0N|I6PDZ:L3G+
Raji cells NGna[IZCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= MV:3NkBp MkD2TWM2OCB;IEG5MlUh|ryP MmjrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzByME[xOFMoRjNyMEC2NVQ{RC:jPh?=
Raji cells NEDuXXlCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= NFvnOpU1QCCq NUXmXWptUUN3MDC9JFE6NjVizszN MnLDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd7NU[wN|coRjJ5OUW2NFM4RC:jPh?=
NAMALWA cells MX;BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? NEm0RmY4OiCq NYH2[Ws1UUN3MDC9JFE6NjZizszN NUPwT3kxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CwNFYyPDNpPkOwNFA3OTR|PD;hQi=>
A2780 cells Ml\3R5l1d3SxeHnjbZR6KGG|c3H5 NV\pd21GOyCmYYnz NGXjS3pGSzVyIE2gNlAvOSEQvF2= MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzB5N{KyPEc,OjdyN{eyNlg9N2F-
Raji cells MYPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? MoXNO|IhcA>? M2X1dWlEPTBiPTCyNE45QCEQvF2= MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTF2NkGzOkc,OjlzNE[xN|Y9N2F-
A549 cells NFXXOGZCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= M{HtdVczKGh? NXW0PIMzUUN3MDC9JFIyNjd7IN88US=> MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDd|NEW4NUc,Ojh5M{S1PFE9N2F-
SW480 cells M1L3SmN6fG:2b4jpZ4l1gSCjc4PhfS=> MlnWN{Bl[Xm| MVHJR|UxKD1iMkWuOkDPxE1? MlXVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdyN{eyNlgoRjJ5MEe3NlI5RC:jPh?=
Ramos cells MUTDfZRwfG:6aXPpeJkh[XO|YYm= NETDXYQzPCCq MVLJR|UxKD1iMkiuO{DPxE1? M4fxblxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6Mke0Olc2Lz5{OEK3OFY4PTxxYU6=

... Click to View More Cell Line Experimental Data

Assay
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
In vivo

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]

Protocol

Kinase Assay:

[1]

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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.
Cell Research:

[2]

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  • Cell lines: Chronic lymphocytic leukemia (CLL) cells
  • Concentrations: 0.01-100 μM
  • Incubation Time: 48 hours
  • Method:

    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.


    (Only for Reference)
Animal Research:

[1]

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  • Animal Models: MRL-Fas(lpr) lupus model and collagen-induced arthritis model.
  • Dosages: ≤50 mg/kg
  • Administration: Administered via p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 88 mg/mL (199.77 mM)
Ethanol 45 mg/mL (102.15 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+30% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.
10mg/mL

* 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.

Chemical Information

Molecular Weight 440.5
Formula

C25H24N6O2

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

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
CalculateReset

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and SDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • 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):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

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

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

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Frequently Asked Questions

  • Question 1:

    How to reconstitute the compound S2680 for in vivo studies?

  • Answer:

    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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID