Ibrutinib (PCI-32765)

For research use only.

Catalog No.S2680

411 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.

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Selleck's Ibrutinib (PCI-32765) has been cited by 411 publications

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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 MmHQSpVv[3Srb36gZZN{[Xl? Mo[wNk42KM7:TR?= M3zaeVYhcA>? M2HYZWlvcGmkaYTpc44hd2ZiTInuJJBpd3OyaH;yfYxifGmxbjDpckBpfW2jbjDS[YMyKGOnbHzzJIF1KDJwNTD1UUBqdmO3YnH0[YQh\m:{IE[gbJJ{KGK7IGfld5Rmem5iYnzveJRqdmdibXX0bI9l M{H0b|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MkKyPFc4Lz5{NUKyNlg4PzxxYU6=
human WSU-NHL cells M{T1dGN6fG:2b4jpZ:Kh[XO|YYm= M1\He|czKGh? MYDDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDXV3UuVkiOIHPlcIx{KGG|c3Xzd4VlKGG|IHfyc5d1cCCrbnjpZol1cW:wIHHmeIVzKDd{IHjyd{BjgSCFZXzsWIl1\XJvR3zvJIx2dWmwZYPj[Y51KGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTFwMEmg{txO M2CwZ|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUG1NlkyLz5{NEmxOVI6OTxxYU6=
human SU-DHL6 cells NWrmTXQ6S3m2b4TvfIlkyqCjc4PhfS=> NXG0UpJNPzJiaB?= MlPZR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gV3UuTEiONjDj[YxteyCjc4Pld5Nm\CCjczDndo94fGhiaX7obYJqfGmxbjDh[pRmeiB5MjDodpMh[nliQ3XscHRqfGW{LVfsc{BtfW2rbnXzZ4VvfCClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkW4JO69VS5? MkDNQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7MUWyPVEoRjJ2OUG1NlkyRC:jPh?=
human DOHH2 cells NWnJe5FwS3m2b4TvfIlkyqCjc4PhfS=> M3rjeVczKGh? NWHRc4dMS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hTE:KSEKgZ4VtdHNiYYPz[ZN{\WRiYYOg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiN{KgbJJ{KGK7IFPlcIxVcXSncj3HcI8hdHWvaX7ld4NmdnRiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD60NUDPxE1w MoDjQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7MUWyPVEoRjJ2OUG1NlkyRC:jPh?=
Sf9 cells M4fVU2Z2dmO2aX;uJIF{e2G7 NGToZmMyKGh? NFSyfJRKdmirYnn0bY9vKG:oIFzZUk1CKGW6cILld5Nm\CCrbjDT[lkh[2WubIOgZYZ1\XJiNkCgcYlveyCkeTDUVk1HWkWWIFHzd4F6NCCLQ{WwQVAvOiEQvF2u Ml\WQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF7NUi1OFcoRjJzOUW4OVQ4RC:jPh?=
human Ramos cells NVPkR3J7TnWwY4Tpc44h[XO|YYm= NGTPR4YyKGh? M4DOe2lvcGmkaYTpc44hd2ZiQoTrJIlvKGi3bXHuJHJidW:|IHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhWEyFLXfhcY1iOiCyaH;zdIhwenmuYYTpc44h[XRiVInyNVIyPyCjZoTldkAyKGi{IHL5JHdme3Sncn6gZoxwfCCjbnHsfZNqeyxiSVO1NF0yPCCwTT6= Ml\DQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7MUWyPVEoRjJ2OUG1NlkyRC:jPh?=
human Pfeiffer cells M4\Fc2Z2dmO2aX;uJIF{e2G7 Mn7XO|IhcA>? MUXDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDQ[oVq\m[ncjDj[YxteyCjc4Pld5Nm\CCjczDndo94fGhiaX7obYJqfGmxbjDh[pRmeiB5MjDodpMh[nliQ3XscHRqfGW{LVfsc{BtfW2rbnXzZ4VvfCClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1{IH7NMi=> MkTRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7MUWyPVEoRjJ2OUG1NlkyRC:jPh?=
Sf9 cells MkeySpVv[3Srb36gZZN{[Xl? NYjJPZE3OSCq NXX6Sm5DUW6qaXLpeIlwdiCxZjDoeY1idiCodXzsMYxmdme2aDDCWGsh\XiycnXzd4VlKGmwIGPmPUBk\WyuczD1d4lv\yCIQV2tV5JkfGmmZTDw[ZB1cWSnIHHzJJN2[nO2cnH0[UBi\nSncjC2NEBucW6|IHL5JHRTNU[URWSgRZN{[XoxvJygTWM2OD1yLkWgcm0v NWTuZWRERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG5OVg2PDdpPkKxPVU5PTR5PD;hQi=>
Sf9 insect cells NGHQZYxHfW6ldHnvckBie3OjeR?= NEK1Vm43OCCvaX7z M17SdmlEPTBiPTCwMlAxODNizszN MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTF2NkGzOkc,OjlzNE[xN|Y9N2F-
sf9 cells NF3EVolHfW6ldHnvckBie3OjeR?= NVj5ZlNmUUN3MDC9JFAvODByMzFOwG0> NVXoXGNpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke5PVQ4OzZpPkK3PVk1PzN4PD;hQi=>
Sf9 insect cells NWDUN3JETnWwY4Tpc44h[XO|YYm= NHrucZM3OCCvaX7z Mkn1TWM2OCB;IECuNFAxOzRizszN M4LBZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5OUGyNVc2Lz5{N{mxNlE4PTxxYU6=
Sf9 insect cells MnGwSpVv[3Srb36gZZN{[Xl? MWS2NEBucW6| NGfKcGRKSzVyIE2gNE4xODB|NDFOwG0> MmiyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh2M{K5OFYoRjJ6NEOyPVQ3RC:jPh?=
Sf9 insect cells NVnZNJc4TnWwY4Tpc44h[XO|YYm= NGWyVng3OCCvaX7z NUe4NY5JUUN3MDC9JFAvODByM{Sg{txO MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzl3NkCzO{c,Ojd7NU[wN|c9N2F-
Sf9 cells MWnGeY5kfGmxbjDhd5NigQ>? M2PBPFYxKG2rboO= NFH4d|ZKSzVyIE2gNE4xODB2IN88US=> MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODByNkG0N{c,OzByME[xOFM9N2F-
Sf9 cells NYXNSVV7TnWwY4Tpc44h[XO|YYm= MnT4OlAhdWmwcx?= NE\HS3pKSzVyIE2gNE4xODB3IN88US=> M2nQSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzOUW4OVQ4Lz5{MUm1PFU1PzxxYU6=
Ramos cells M2[wb2Z2dmO2aX;uJIF{e2G7 MnXENUBp MVvJR|UxKD1iMD6wNFA2KM7:TR?= MnvOQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh{OECyOlEoRjJ6MkiwNlYyRC:jPh?=
Sf9 cells MUjGeY5kfGmxbjDhd5NigQ>? MkLUOlAhdWmwcx?= MYnJR|UxKD1iMD6wNFEh|ryP MnHBQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzByN{e2NFgoRjNyMEe3OlA5RC:jPh?=
Pfeiffer cells M1T5UGN6fG:2b4jpZ4l1gSCjc4PhfS=> M{G1e|czKGh? M4TUOGdKPTBiPTCwMlAxOiEQvF2= NEGyfFg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEmxOVI6OSd-MkS5NVUzQTF:L3G+
B cells MnX1SpVv[3Srb36gZZN{[Xl? MVOxJIg> NWThWY9tUUN3MDC9JFAvODB2NjFOwG0> M1\WOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMkmwPVg5Lz5|MEK5NFk5QDxxYU6=
Sf9 insect cells M2GzemZ2dmO2aX;uJIF{e2G7 NWLWN3pVOiC2bzC2NEBucW6| NEPMbIZMcSB;IECuNFA1QCEQvF2= MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDNzNUW5O{c,Ojh|MUW1PVc9N2F-
Ramos cells MXPGeY5kfGmxbjDhd5NigQ>? NVPBeZVEOSCq MnXETWM2OCB;IECuNFA4PSEQvF2= MnHzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7MUWyPVEoRjJ2OUG1NlkyRC:jPh?=
Sf9 insect cells NGW4WmNHfW6ldHnvckBie3OjeR?= NX:zdWgyPjBibXnudy=> NHfJN5BKSzVyIE2gNE4xODhizszN Ml;jQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh|MUW1PVcoRjJ6M{G1OVk4RC:jPh?=
TMD8 cells NXeyeol{SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[XO|YYm= NUD4eYgxPzJiaB?= MX;JR|UxKD1iMD6wNUDPxE1? MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTdzNUCyN{c,Ojl5MUWwNlM9N2F-
CD19+ B cells M361cGZ2dmO2aX;uJIF{e2G7 NYriNmJ6OSCq NWjuemF2UUN3MDC9JFAvODF{IN88US=> M3;UclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEW3PVgzLz5{OUS1O|k5OjxxYU6=
Sf9 insect cells NF\UfGZHfW6ldHnvckBie3OjeR?= NVy1Xm9PPjBibXnudy=> M3r1eGlEPTBiPTCwMlAyOiEQvF2= Ml3HQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh|MUW1PVcoRjJ6M{G1OVk4RC:jPh?=
Ramos cells NW[0TZhwTnWwY4Tpc44h[XO|YYm= NUfBWI5mOSCq MXXJR|UxKD1iMD6wNVQh|ryP NGTSV2M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEmxOVI6OSd-MkS5NVUzQTF:L3G+
Sf9 insect cells MYLGeY5kfGmxbjDhd5NigQ>? M2j4dlEhcA>? M4TWZ2lEPTBiPTCwMlAyPDRizszN M3nTWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7N{G1NFI{Lz5{OUexOVAzOzxxYU6=
Sf9 insect cells MmTzSpVv[3Srb36gZZN{[Xl? NELLbVE3OCCvaX7z NUjweJhKUUN3MDC9JFAvODF4MTFOwG0> MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTF2NkGzOkc,OjlzNE[xN|Y9N2F-
HCC827 cells NXrHdoxISW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[XO|YYm= Mn;6O|IhcA>? MkDGTWM2OCB;IECuNFM6KM7:TR?= NHXaSFE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEezOFU5OSd-Mki3N|Q2QDF:L3G+
PC9 cells M4LNZ2Z2dmO2aX;uJIF{e2G7 NYXKcVF5PzJiaB?= MXjHTVUxKD1iMD6wOUDPxE1? NHjCdHc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEK4NlEzOid-MkiyPFIyOjJ:L3G+
Sf9 cells M3n2eWZ2dmO2aX;uJIF{e2G7 MVu2NEBucW6| MVXJR|UxKD1iMD6xJO69VQ>? MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODByNkG0N{c,OzByME[xOFM9N2F-
H3255 cells NGX1eIhHfW6ldHnvckBie3OjeR?= Mmi3O|IhcA>? M3TtbmdKPTBiPTCwMlEyKM7:TR?= MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDJ6MkGyNkc,Ojh{OEKxNlI9N2F-
BaF3 cells MXjGeY5kfGmxbjDhd5NigQ>? NFX4WG04OiCq M2[1VmdKPTBiPTCwMlEzKM7:TR?= MkPOQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ4M{C1OVMoRjJ4NkOwOVU{RC:jPh?=
BAF3 cells M1z2VGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 M1Xqe|czKGh? NHzo[IdIUTVyIE2gNE4yOiEQvF2= NVTuRWtqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki5OVY6OjNpPkK4PVU3QTJ|PD;hQi=>
Sf9 insect cells NFGwRmxHfW6ldHnvckBie3OjeR?= M3LRS|YxKG2rboO= MonLTWM2OCB;IECuNVI{KM7:TR?= MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDNzNUW5O{c,Ojh|MUW1PVc9N2F-
Sf9 insect cells NYjPT4R6TnWwY4Tpc44h[XO|YYm= NH;qZ5A3OCCvaX7z MYTJR|UxKD1iMD6xOFYh|ryP NUnDWZViRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkizNVU2QTdpPkK4N|E2PTl5PD;hQi=>
BAF3 cells Mo\mSpVv[3Srb36gZZN{[Xl? NIrJdWQ4OiCq NIXjWnlIUTVyIE2gNE4yPiEQvF2= Mn\PQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh{OEKxNlIoRjJ6MkiyNVIzRC:jPh?=
Sf9 cells M3n6[WZ2dmO2aX;uJIF{e2G7 NEfscWU3OCCvaX7z MVnJR|UxKD1iMD6yJO69VQ>? NGPMNXo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUm1PFU1Pyd-MkG5OVg2PDd:L3G+
MV411 cells NH21UXZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NFjQSVRIUTVyIE2gNE4zPSEQvF2= NEfpdVE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEOxOVU6Pyd-MkizNVU2QTd:L3G+
MV4-11 cells MW\BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? NFj2fG84OiCq M4jBXGdKPTBiPTCwMlM{KM7:TR?= MoLHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ4M{C1OVMoRjJ4NkOwOVU{RC:jPh?=
MV4-11 cells Mn;mRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZZN{[Xl? NGnwdZc4OiCq NUH2U|F[T0l3MDC9JFAvOzNizszN MmW4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh7NU[5NlMoRjJ6OUW2PVI{RC:jPh?=
DOHH2 cells MUjDfZRwfG:6aXPpeJkh[XO|YYm= NUCzbm5oPzJiaB?= MmjRS2k2OCB;IECuOFEh|ryP MojiQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7MUWyPVEoRjJ2OUG1NlkyRC:jPh?=
HCC827 cells Mm[5RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZZN{[Xl? NGnRVHk6PiCq NWnIVIlSTUN3MDC9JFAvPDVizszN MkLFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh6NUO1O|UoRjJ6OEWzOVc2RC:jPh?=
SU-DHL6 cells MWHDfZRwfG:6aXPpeJkh[XO|YYm= MmK2O|IhcA>? MmjMS2k2OCB;IECuOVgh|ryP MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDlzNUK5NUc,OjR7MUWyPVE9N2F-
M07e cells MXHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NFHGOVBIUTVyIE2gNE42QSEQvF2= NETlbVA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEOxOVU6Pyd-MkizNVU2QTd:L3G+
NCI-H1975 cells MnnwRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZZN{[Xl? MlLWPVYhcA>? M1HXdWVEPTBiPTCwMlY1KM7:TR?= MkHYQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh6NUO1O|UoRjJ6OEWzOVc2RC:jPh?=
SU-DHL-2 cells M4e2XWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MVXHTVUxKD1iMD62OEDPxE1? NGPpWFQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEOxOVU6Pyd-MkizNVU2QTd:L3G+
HEK293T cells MWPGeY5kfGmxbjDhd5NigQ>? MmTaNUBp MXPJR|UxKD1iMD65JO69VQ>? NVnUV45KRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkiyPFAzPjFpPkK4NlgxOjZzPD;hQi=>
Ramos cells M{jhXGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 MmfzO|IhcA>? NGW1cHVKSzVyIE2gNE46OiEQvF2= MnS5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl5MUWwNlMoRjJ7N{G1NFI{RC:jPh?=
BA/F3 cells M2fOemFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 NUH2[nNUPzJiaB?= MYnJR|UxKD1iMTFOwG0> MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjJ3OEWyNUc,OjZ{NUi1NlE9N2F-
WSU-NHL cells M4fyUmN6fG:2b4jpZ4l1gSCjc4PhfS=> MWi3NkBp MYLHTVUxKD1iMT6wPUDPxE1? MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDlzNUK5NUc,OjR7MUWyPVE9N2F-
NCI-H1975 cells M3j5PGZ2dmO2aX;uJIF{e2G7 MV23NkBp MWPHTVUxKD1iMT6yJO69VQ>? MmHGQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh{OEKxNlIoRjJ6MkiyNVIzRC:jPh?=
NCI-H1975 cells MoSxRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZZN{[Xl? M3;2TlczKGh? NH3ZZW1KSzVyIE2gNU4zPyEQvF2= NIP1fmk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEezOFU5OSd-Mki3N|Q2QDF:L3G+
Raji cells NYXrfGJOSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[XO|YYm= NUG5dVk3PDhiaB?= MnuyTWM2OCB;IEGuOFkh|ryP NFLOV5U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUW2O|I6PSd-Mkm1OlczQTV:L3G+
Pfeiffer cells NVvrc5JYT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MVjHTVUxKD1iMT62JO69VQ>? NUH3PXlrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkizNVU2QTdpPkK4N|E2PTl5PD;hQi=>
A431 cells MkG3RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZZN{[Xl? NIi5VVI6PiCq MnjYSWM2OCB;IEKuN|gh|ryP MnXGQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh6NUO1O|UoRjJ6OEWzOVc2RC:jPh?=
BAF3 cells M1G1[mFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 MYK3NkBp M2ftVmdKPTBiPTCyMlUh|ryP M{jFdVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6OUW2PVI{Lz5{OEm1OlkzOzxxYU6=
U937 cells NEnDfpBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NYj1XWlNT0l3MDC9JFIvQSEQvF2= M4TndFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6M{G1OVk4Lz5{OEOxOVU6PzxxYU6=
NB4 cells NWW2SZExT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MnuxS2k2OCB;IEOg{txO NF7vSIk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEOxOVU6Pyd-MkizNVU2QTd:L3G+
Ramos cells NWTVOIFnT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M1[xcWdKPTBiPTCzMlQh|ryP NHrtOGs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEOxOVU6Pyd-MkizNVU2QTd:L3G+
SKM1 cells MX\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MVTHTVUxKD1iMz62JO69VQ>? MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDNzNUW5O{c,Ojh|MUW1PVc9N2F-
U2932 cells NX\zd5o{T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MljqS2k2OCB;IESuOEDPxE1? M33BVVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6M{G1OVk4Lz5{OEOxOVU6PzxxYU6=
Ramos cells MoXRRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZZN{[Xl? MlrkO|IhcA>? MX\JR|UxKD1iNT6xOEDPxE1? NHvCe5Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MECwOlE1Oyd-M{CwNFYyPDN:L3G+
Ramos cells NHHYV5RCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= NWDuPJQ5PDhiaB?= NFSyOmVKSzVyIE2gOU4yPCEQvF2= MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzl3NkCzO{c,Ojd7NU[wN|c9N2F-
Ramos cells MYfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? MXS0PEBp MY\JR|UxKD1iNT64PEDPxE1? NIfER2M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OESzNlk1Pid-Mki0N|I6PDZ:L3G+
Ramos cells MXnBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? MkDGO|IhcA>? MWPJR|UxKD1iNj62NkDPxE1? NULOZlV1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmxOFYyOzZpPkK5NVQ3OTN4PD;hQi=>
K562 cells NIjOUmNCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= MWi0PEBp MXHJR|UxKD1iNz61JO69VQ>? NY\Dc4xWRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CwO|c3ODhpPkOwNFc4PjB6PD;hQi=>
HL60 cells NF;BcYpCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= M4r6NVQ5KGh? Ml3vTWM2OCB;IEig{txO M1LlR|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMEe3OlA5Lz5|MEC3O|YxQDxxYU6=
Ramos cells M3jLSWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 M{f0dFQ5KGh? M2\j[mlEPTBiPTC4MlEyKM7:TR?= M1nkNlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5OUm0O|M3Lz5{N{m5OFc{PjxxYU6=
Ramos cells NV3CR2trSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[XO|YYm= NIrhUFA1QCCq NFzz[nJKSzVyIE2gPE4zPiEQvF2= NFLwdoE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUW2O|I6PSd-Mkm1OlczQTV:L3G+
OCI-AML3 cells MYTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NGjmcmFIUTVyIE2gPU4zKM7:TR?= NXT1d2p4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkizNVU2QTdpPkK4N|E2PTl5PD;hQi=>
BAF3 cells MYLDfZRwfG:6aXPpeJkh[XO|YYm= NVS0TploPzJiaB?= NHHNNJFIUTVyIE2gNVAh|ryP NHXFfoM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nk[zNFU2Oyd-Mk[2N|A2PTN:L3G+
BAF3 cells MUDBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? M17zfVczKGh? MkDuS2k2OCB;IEGwJO69VQ>? MoTMQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh7NU[5NlMoRjJ6OUW2PVI{RC:jPh?=
BAF3 cells MoqwS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NFvZ[JQ4OiCq NFLUdohIUTVyIE2gNVAh|ryP M17GU|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MkiyNVIzLz5{OEK4NlEzOjxxYU6=
NAMALWA cells MUTBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? M4PBPVczKGh? M3nZV2lEPTBiPTCxNE41PSEQvF2= MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTF2NkGzOkc,OjlzNE[xN|Y9N2F-
Ramos cells NHrLUXhCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= NHnteHA1QCCq M4G5d2lEPTBiPTCxNk43KM7:TR?= NX;6UlIyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke5NVIyPzVpPkK3PVEzOTd3PD;hQi=>
Raji cells NFjveYhCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= NYLEVoVZPDhiaB?= NGnBbYNKSzVyIE2gNVQvOiEQvF2= MlTYQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzByN{e2NFgoRjNyMEe3OlA5RC:jPh?=
Raji cells MXzBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? NWHwZW52PDhiaB?= MYfJR|UxKD1iMUWuNkDPxE1? MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzl7NEezOkc,Ojd7OUS3N|Y9N2F-
MIAPaCa2 cells NWjk[5Q{S3m2b4TvfIlkcXS7IHHzd4F6 MUizJIRigXN? NWXBOXJVUUN3MDC9JFE3NjZizszN M1[5eVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MEe3NlI5Lz5{N{C3O|IzQDxxYU6=
HeLa cells NUn0cWhtS3m2b4TvfIlkcXS7IHHzd4F6 MVezJIRigXN? MnvETWM2OCB;IEG2Mlgh|ryP NHHPfFE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{C3O|IzQCd-MkewO|czOjh:L3G+
Raji cells NHK5cVRCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= NIHGZ2k1QCCq NFLRSW5KSzVyIE2gNVkvOyEQvF2= NVizb4VlRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke5NVIyPzVpPkK3PVEzOTd3PD;hQi=>
Raji cells Ml25RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZZN{[Xl? NHHOeYI1QCCq M4TlOWlEPTBiPTCxPU4{KM7:TR?= M2n4S|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6NEOyPVQ3Lz5{OESzNlk1PjxxYU6=
Raji cells M1z4WmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 NF3uc4s4OiCq NH\Xd2pKSzVyIE2gNVkvPSEQvF2= NWT2foJtRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CwNFYyPDNpPkOwNFA3OTR|PD;hQi=>
Raji cells Mnn3RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZZN{[Xl? NFXFV2Q1QCCq M1rwcGlEPTBiPTCxPU42KM7:TR?= M3HR[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5OUW2NFM4Lz5{N{m1OlA{PzxxYU6=
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A2780 cells MonPR5l1d3SxeHnjbZR6KGG|c3H5 MXuzJIRigXN? NHLk[HRGSzVyIE2gNlAvOSEQvF2= M1;YV|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MEe3NlI5Lz5{N{C3O|IzQDxxYU6=
Raji cells NI\BUnJCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= MYO3NkBp M1n5RmlEPTBiPTCyNE45QCEQvF2= MnKxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjlzNE[xN|YoRjJ7MUS2NVM3RC:jPh?=
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SW480 cells MnjUR5l1d3SxeHnjbZR6KGG|c3H5 M{LobFMh\GG7cx?= MmXrTWM2OCB;IEK1MlYh|ryP MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzB5N{KyPEc,OjdyN{eyNlg9N2F-
Ramos cells MVzDfZRwfG:6aXPpeJkh[XO|YYm= MWKyOEBp NXXZVIRPUUN3MDC9JFI5NjdizszN MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDJ5NE[3OUc,Ojh{N{S2O|U9N2F-

... 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 MSDS / 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 MSDS / 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
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

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.

  • * Indicates a Required Field

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