Ibrutinib (PCI-32765)

For research use only.

Catalog No.S2680

460 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 460 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 MmTHSpVv[3Srb36gZZN{[Xl? M3zLZVIvPSEQvF2= MlTpOkBp NI\TfGFKdmirYnn0bY9vKG:oIFz5ckBxcG:|cHjvdplt[XSrb36gbY4hcHWvYX6gVoVkOSClZXzsd{BifCB{LkWgeW0hcW6ldXLheIVlKG[xcjC2JIhzeyCkeTDX[ZN1\XKwIHLsc5R1cW6pIH3leIhw\A>? NFzrcHE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUKyNlg4Pyd-MkWyNlI5Pzd:L3G+
human WSU-NHL cells MkDlR5l1d3SxeHnjxsBie3OjeR?= M{C5WFczKGh? MYLDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDXV3UuVkiOIHPlcIx{KGG|c3Xzd4VlKGG|IHfyc5d1cCCrbnjpZol1cW:wIHHmeIVzKDd{IHjyd{BjgSCFZXzsWIl1\XJvR3zvJIx2dWmwZYPj[Y51KGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTFwMEmg{txO MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDlzNUK5NUc,OjR7MUWyPVE9N2F-
human SU-DHL6 cells M{\We2N6fG:2b4jpZ:Kh[XO|YYm= NUHwRpBXPzJiaB?= M{\CZ2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHNWNUSKTE[gZ4VtdHNiYYPz[ZN{\WRiYYOg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiN{KgbJJ{KGK7IFPlcIxVcXSncj3HcI8hdHWvaX7ld4NmdnRiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD61PEDPxE1w M3n4dlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUG1NlkyLz5{NEmxOVI6OTxxYU6=
human DOHH2 cells MmPRR5l1d3SxeHnjxsBie3OjeR?= NFPZWHY4OiCq NHrGflREgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBFV0iKMjDj[YxteyCjc4Pld5Nm\CCjczDndo94fGhiaX7obYJqfGmxbjDh[pRmeiB5MjDodpMh[nliQ3XscHRqfGW{LVfsc{BtfW2rbnXzZ4VvfCClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkSxJO69VS5? NEXyeJA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEmxOVI6OSd-MkS5NVUzQTF:L3G+
Sf9 cells M1nuSWZ2dmO2aX;uJIF{e2G7 MXixJIg> MljSTY5pcWKrdHnvckBw\iCOWV6tRUBmgHC{ZYPz[YQhcW5iU3[5JINmdGy|IHHmeIVzKDZyIH3pcpMh[nliVGKtSnJGXCCDc4PhfUwhUUN3ME2wMlIh|ryPLh?= MkLWQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF7NUi1OFcoRjJzOUW4OVQ4RC:jPh?=
human Ramos cells M2P5cGZ2dmO2aX;uJIF{e2G7 M3\PT|EhcA>? MYDJcohq[mm2aX;uJI9nKEK2azDpckBpfW2jbjDSZY1weyClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJHBNSy2pYX3tZVIheGixc4Doc5J6dGG2aX;uJIF1KFS7ckGyNVch[W[2ZYKgNUBpeiCkeTDX[ZN1\XKwIHLsc5Qh[W6jbInzbZMtKEmFNUC9NVQhdk1w NYP6T2ZrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5NVUzQTFpPkK0PVE2OjlzPD;hQi=>
human Pfeiffer cells MUHGeY5kfGmxbjDhd5NigQ>? M4S4dFczKGh? NXrhb49ZS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hWG[naX\m[ZIh[2WubIOgZZN{\XO|ZXSgZZMh\3Kxd4ToJIlvcGmkaYTpc44h[W[2ZYKgO|IhcHK|IHL5JGNmdGyWaYTldk1IdG9ibIXtbY5me2OnboSgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NkBvVS5? NF\pSFY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEmxOVI6OSd-MkS5NVUzQTF:L3G+
Sf9 cells M3rifGZ2dmO2aX;uJIF{e2G7 Ml3rNUBp NWHLOmhvUW6qaXLpeIlwdiCxZjDoeY1idiCodXzsMYxmdme2aDDCWGsh\XiycnXzd4VlKGmwIGPmPUBk\WyuczD1d4lv\yCIQV2tV5JkfGmmZTDw[ZB1cWSnIHHzJJN2[nO2cnH0[UBi\nSncjC2NEBucW6|IHL5JHRTNU[URWSgRZN{[XoxvJygTWM2OD1yLkWgcm0v NEXxVXQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUm1PFU1Pyd-MkG5OVg2PDd:L3G+
Sf9 insect cells M3j3SWZ2dmO2aX;uJIF{e2G7 M{POOlYxKG2rboO= MYPJR|UxKD1iMD6wNFA{KM7:TR?= MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTF2NkGzOkc,OjlzNE[xN|Y9N2F-
sf9 cells NHvzTG9HfW6ldHnvckBie3OjeR?= NYq2TGdFUUN3MDC9JFAvODByMzFOwG0> MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzl7NEezOkc,Ojd7OUS3N|Y9N2F-
Sf9 insect cells MWnGeY5kfGmxbjDhd5NigQ>? M1O4dlYxKG2rboO= NH3VOIdKSzVyIE2gNE4xODB|NDFOwG0> NVfqXJZERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke5NVIyPzVpPkK3PVEzOTd3PD;hQi=>
Sf9 insect cells M3nhZWZ2dmO2aX;uJIF{e2G7 NHqwVZI3OCCvaX7z MkDCTWM2OCB;IECuNFAxOzRizszN Mnn6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh2M{K5OFYoRjJ6NEOyPVQ3RC:jPh?=
Sf9 insect cells MWPGeY5kfGmxbjDhd5NigQ>? NVvVZYZ{PjBibXnudy=> NXjveYdJUUN3MDC9JFAvODByM{Sg{txO MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzl3NkCzO{c,Ojd7NU[wN|c9N2F-
Sf9 cells M2PjbmZ2dmO2aX;uJIF{e2G7 MlXxOlAhdWmwcx?= M2P0RmlEPTBiPTCwMlAxODRizszN NWjqXVlNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CwNFYyPDNpPkOwNFA3OTR|PD;hQi=>
Sf9 cells NIrvWpFHfW6ldHnvckBie3OjeR?= NUPVR3lwPjBibXnudy=> MYXJR|UxKD1iMD6wNFA2KM7:TR?= MmH5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF7NUi1OFcoRjJzOUW4OVQ4RC:jPh?=
Ramos cells Mn;tSpVv[3Srb36gZZN{[Xl? NULWXpVDOSCq NIfrWmpKSzVyIE2gNE4xODB3IN88US=> NWjtPIhSRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkiyPFAzPjFpPkK4NlgxOjZzPD;hQi=>
Sf9 cells NV3Zd5QzTnWwY4Tpc44h[XO|YYm= NFzze2M3OCCvaX7z NIPW[GpKSzVyIE2gNE4xODFizszN M2TOTFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMEe3OlA5Lz5|MEC3O|YxQDxxYU6=
Pfeiffer cells NUjV[3M1S3m2b4TvfIlkcXS7IHHzd4F6 MmHXO|IhcA>? M4TnW2dKPTBiPTCwMlAxOiEQvF2= NI\ue3A9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEmxOVI6OSd-MkS5NVUzQTF:L3G+
B cells M{XBZ2Z2dmO2aX;uJIF{e2G7 MVixJIg> Mn;PTWM2OCB;IECuNFA1PiEQvF2= NGiyUZY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEK5NFk5QCd-M{CyPVA6QDh:L3G+
Sf9 insect cells M172SmZ2dmO2aX;uJIF{e2G7 MV[yJJRwKDZyIH3pcpM> NF7lVVJMcSB;IECuNFA1QCEQvF2= NVW2T4RoRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkizNVU2QTdpPkK4N|E2PTl5PD;hQi=>
Ramos cells MXHGeY5kfGmxbjDhd5NigQ>? NVvxTVhvOSCq MmLoTWM2OCB;IECuNFA4PSEQvF2= NGfOOYU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEmxOVI6OSd-MkS5NVUzQTF:L3G+
Sf9 insect cells NXrlbVRXTnWwY4Tpc44h[XO|YYm= MnX5OlAhdWmwcx?= NH3L[VBKSzVyIE2gNE4xODhizszN Mn21QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh|MUW1PVcoRjJ6M{G1OVk4RC:jPh?=
TMD8 cells M4fLSGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 NWXvS3l5PzJiaB?= MlHuTWM2OCB;IECuNFEh|ryP M1X3N|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7N{G1NFI{Lz5{OUexOVAzOzxxYU6=
CD19+ B cells M2\DT2Z2dmO2aX;uJIF{e2G7 MWSxJIg> MmX0TWM2OCB;IECuNFEzKM7:TR?= MmHMQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2NUe5PFIoRjJ7NEW3PVgzRC:jPh?=
Sf9 insect cells NV\TbZVsTnWwY4Tpc44h[XO|YYm= MkTVOlAhdWmwcx?= MVPJR|UxKD1iMD6wNVIh|ryP MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDNzNUW5O{c,Ojh|MUW1PVc9N2F-
Ramos cells NVvxVnlQTnWwY4Tpc44h[XO|YYm= MUexJIg> M4LuPGlEPTBiPTCwMlAyPCEQvF2= MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDlzNUK5NUc,OjR7MUWyPVE9N2F-
Sf9 insect cells M4\V[WZ2dmO2aX;uJIF{e2G7 MY[xJIg> NGTKNWxKSzVyIE2gNE4xOTR2IN88US=> NULlb5M3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm3NVUxOjNpPkK5O|E2ODJ|PD;hQi=>
Sf9 insect cells M2DJNWZ2dmO2aX;uJIF{e2G7 NVj1bWNUPjBibXnudy=> NGDmbIFKSzVyIE2gNE4xOTZzIN88US=> M4XxRVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7MUS2NVM3Lz5{OUG0OlE{PjxxYU6=
HCC827 cells M33zNGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 MXq3NkBp MnvRTWM2OCB;IECuNFM6KM7:TR?= NXG4fJp{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki3N|Q2QDFpPkK4O|M1PThzPD;hQi=>
PC9 cells MnPNSpVv[3Srb36gZZN{[Xl? M{n0c|czKGh? NHv1T4xIUTVyIE2gNE4xPSEQvF2= MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDJ6MkGyNkc,Ojh{OEKxNlI9N2F-
Sf9 cells MmLzSpVv[3Srb36gZZN{[Xl? M1z5UFYxKG2rboO= NVTLdIxiUUN3MDC9JFAvOSEQvF2= Mne5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzByME[xOFMoRjNyMEC2NVQ{RC:jPh?=
H3255 cells NHq4WWZHfW6ldHnvckBie3OjeR?= NX7nd2tpPzJiaB?= MnHCS2k2OCB;IECuNVEh|ryP MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDJ6MkGyNkc,Ojh{OEKxNlI9N2F-
BaF3 cells MYrGeY5kfGmxbjDhd5NigQ>? MVW3NkBp NHHlW41IUTVyIE2gNE4yOiEQvF2= NFTm[no9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nk[zNFU2Oyd-Mk[2N|A2PTN:L3G+
BAF3 cells M17YV2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 MX:3NkBp MWHHTVUxKD1iMD6xNkDPxE1? MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDl3NkmyN{c,Ojh7NU[5NlM9N2F-
Sf9 insect cells MmrtSpVv[3Srb36gZZN{[Xl? Mmf5OlAhdWmwcx?= MVLJR|UxKD1iMD6xNlMh|ryP MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDNzNUW5O{c,Ojh|MUW1PVc9N2F-
Sf9 insect cells MoW3SpVv[3Srb36gZZN{[Xl? NUK1UWhCPjBibXnudy=> M1W2W2lEPTBiPTCwMlE1PiEQvF2= MlfDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh|MUW1PVcoRjJ6M{G1OVk4RC:jPh?=
BAF3 cells M1jDTmZ2dmO2aX;uJIF{e2G7 NEDDUHg4OiCq M3\DbWdKPTBiPTCwMlE3KM7:TR?= M1fWdFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MkiyNVIzLz5{OEK4NlEzOjxxYU6=
Sf9 cells NI\aNpVHfW6ldHnvckBie3OjeR?= NXTPXFl[PjBibXnudy=> M1PpN2lEPTBiPTCwMlIh|ryP NUXMPYhuRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG5OVg2PDdpPkKxPVU5PTR5PD;hQi=>
MV411 cells NHPiVZVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NInOOlNIUTVyIE2gNE4zPSEQvF2= Mn74QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh|MUW1PVcoRjJ6M{G1OVk4RC:jPh?=
MV4-11 cells Ml3BRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZZN{[Xl? NIf3fms4OiCq M1\ObGdKPTBiPTCwMlM{KM7:TR?= NFruPVE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nk[zNFU2Oyd-Mk[2N|A2PTN:L3G+
MV4-11 cells MVTBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? MnTYO|IhcA>? NH;D[3RIUTVyIE2gNE4{OyEQvF2= NUW5fVh1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki5OVY6OjNpPkK4PVU3QTJ|PD;hQi=>
DOHH2 cells MoHCR5l1d3SxeHnjbZR6KGG|c3H5 M2flXFczKGh? Mn2wS2k2OCB;IECuOFEh|ryP MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDlzNUK5NUc,OjR7MUWyPVE9N2F-
HCC827 cells M{PvNGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 M{nRUVk3KGh? NHXueppGSzVyIE2gNE41PSEQvF2= M{XMV|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6OEWzOVc2Lz5{OEi1N|U4PTxxYU6=
SU-DHL6 cells M1nrOGN6fG:2b4jpZ4l1gSCjc4PhfS=> MoXJO|IhcA>? M3:3PGdKPTBiPTCwMlU5KM7:TR?= MnPUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7MUWyPVEoRjJ2OUG1NlkyRC:jPh?=
M07e cells MkLTS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NIrUdmxIUTVyIE2gNE42QSEQvF2= Moi4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh|MUW1PVcoRjJ6M{G1OVk4RC:jPh?=
NCI-H1975 cells MUHBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? MmXXPVYhcA>? M{[4fWVEPTBiPTCwMlY1KM7:TR?= Mn70QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh6NUO1O|UoRjJ6OEWzOVc2RC:jPh?=
SU-DHL-2 cells NXLvOodjT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NUPIbpFnT0l3MDC9JFAvPjRizszN NY[yUYdXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkizNVU2QTdpPkK4N|E2PTl5PD;hQi=>
HEK293T cells M2HaV2Z2dmO2aX;uJIF{e2G7 NWnYV|Y5OSCq NX[3dmx2UUN3MDC9JFAvQSEQvF2= MlzPQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh{OECyOlEoRjJ6MkiwNlYyRC:jPh?=
Ramos cells MnOyRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZZN{[Xl? Mm\DO|IhcA>? M2XOb2lEPTBiPTCwMlkzKM7:TR?= MkjYQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl5MUWwNlMoRjJ7N{G1NFI{RC:jPh?=
BA/F3 cells MWrBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? NIXKZWU4OiCq NV7INmhLUUN3MDC9JFEh|ryP NX7TZ3hCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[yOVg2OjFpPkK2NlU5PTJzPD;hQi=>
WSU-NHL cells MlLpR5l1d3SxeHnjbZR6KGG|c3H5 NH7qbVM4OiCq M2qxXmdKPTBiPTCxMlA6KM7:TR?= MnP3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7MUWyPVEoRjJ2OUG1NlkyRC:jPh?=
NCI-H1975 cells NGjzfVFHfW6ldHnvckBie3OjeR?= NFfqSHc4OiCq Mm\WS2k2OCB;IEGuNkDPxE1? MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDJ6MkGyNkc,Ojh{OEKxNlI9N2F-
NCI-H1975 cells M1;2XWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 NXvqNWpWPzJiaB?= M174Z2lEPTBiPTCxMlI4KM7:TR?= NX:5ZXZ3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki3N|Q2QDFpPkK4O|M1PThzPD;hQi=>
Raji cells MV3BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? MW[0PEBp NWfSXolIUUN3MDC9JFEvPDlizszN MkHRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl3NkeyPVUoRjJ7NU[3Nlk2RC:jPh?=
Pfeiffer cells MmfvS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NILTNGNIUTVyIE2gNU43KM7:TR?= MlPPQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh|MUW1PVcoRjJ6M{G1OVk4RC:jPh?=
A431 cells NIjGS|ZCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= NYLhe5VPQTZiaB?= MmnjSWM2OCB;IEKuN|gh|ryP M2fGelxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6OEWzOVc2Lz5{OEi1N|U4PTxxYU6=
BAF3 cells NHPLS5VCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= MW[3NkBp MYDHTVUxKD1iMj61JO69VQ>? MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDl3NkmyN{c,Ojh7NU[5NlM9N2F-
U937 cells M4PQO2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MWrHTVUxKD1iMj65JO69VQ>? NYj6eIhDRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkizNVU2QTdpPkK4N|E2PTl5PD;hQi=>
NB4 cells Mmq3S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXnm[lZkT0l3MDC9JFMh|ryP Mnq0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh|MUW1PVcoRjJ6M{G1OVk4RC:jPh?=
Ramos cells NFjBPHJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3;ud2dKPTBiPTCzMlQh|ryP NV7KVmh3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkizNVU2QTdpPkK4N|E2PTl5PD;hQi=>
SKM1 cells M2Pw[Gdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MXrHTVUxKD1iMz62JO69VQ>? NFrHW5k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEOxOVU6Pyd-MkizNVU2QTd:L3G+
U2932 cells MVLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NGHTd3VIUTVyIE2gOE41KM7:TR?= MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDNzNUW5O{c,Ojh|MUW1PVc9N2F-
Ramos cells NF;6co9CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= MnXHO|IhcA>? M4LhcGlEPTBiPTC1MlE1KM7:TR?= MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODByNkG0N{c,OzByME[xOFM9N2F-
Ramos cells M2TYc2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 NX7hZ5dPPDhiaB?= NXPuS|d1UUN3MDC9JFUvOTRizszN MoXPQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd7NU[wN|coRjJ5OUW2NFM4RC:jPh?=
Ramos cells M1qxV2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 NHrESIU1QCCq NIPTdYRKSzVyIE2gOU45QCEQvF2= NYfvUGI1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki0N|I6PDZpPkK4OFMzQTR4PD;hQi=>
Ramos cells MWPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? MnezO|IhcA>? M3LRbGlEPTBiPTC2MlYzKM7:TR?= NILLPFM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUG0OlE{Pid-MkmxOFYyOzZ:L3G+
K562 cells M2\zfWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 NF60fJU1QCCq MYfJR|UxKD1iNz61JO69VQ>? NGXQ[VA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEC3O|YxQCd-M{CwO|c3ODh:L3G+
HL60 cells NHPrc3RCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= NFz5[FA1QCCq NInxToZKSzVyIE2gPEDPxE1? Moi4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzByN{e2NFgoRjNyMEe3OlA5RC:jPh?=
Ramos cells M3ezXWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 MYO0PEBp NUfjcJNmUUN3MDC9JFgvOTFizszN MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzl7NEezOkc,Ojd7OUS3N|Y9N2F-
Ramos cells MVvBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? NVzYXmxtPDhiaB?= MlS1TWM2OCB;IEiuNlYh|ryP NEfnbow9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUW2O|I6PSd-Mkm1OlczQTV:L3G+
OCI-AML3 cells MW\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NIXFXFZIUTVyIE2gPU4zKM7:TR?= NGi0UGQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEOxOVU6Pyd-MkizNVU2QTd:L3G+
BAF3 cells NYDuZmE{S3m2b4TvfIlkcXS7IHHzd4F6 NX:4OpVoPzJiaB?= MofWS2k2OCB;IEGwJO69VQ>? NVjJTnlQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[2N|A2PTNpPkK2OlMxPTV|PD;hQi=>
BAF3 cells NF;WRoJCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= NHrJcIw4OiCq MVXHTVUxKD1iMUCg{txO NELpXIE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEm1OlkzOyd-Mki5OVY6OjN:L3G+
BAF3 cells NH\PfppIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M4r0SFczKGh? M3mzUWdKPTBiPTCxNEDPxE1? MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDJ6MkGyNkc,Ojh{OEKxNlI9N2F-
NAMALWA cells NVrMNmRwSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[XO|YYm= MnztO|IhcA>? NXrMNopYUUN3MDC9JFExNjR3IN88US=> MkfnQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjlzNE[xN|YoRjJ7MUS2NVM3RC:jPh?=
Ramos cells Mn3DRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZZN{[Xl? M{TlfFQ5KGh? MoTrTWM2OCB;IEGyMlYh|ryP MoTVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd7MUKxO|UoRjJ5OUGyNVc2RC:jPh?=
Raji cells M1vX[GFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 MofrOFghcA>? NIrEZ49KSzVyIE2gNVQvOiEQvF2= NVjKPWRORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CwO|c3ODhpPkOwNFc4PjB6PD;hQi=>
Raji cells MXLBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? M2npWFQ5KGh? MYDJR|UxKD1iMUWuNkDPxE1? NHfte5o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{m5OFc{Pid-Mke5PVQ4OzZ:L3G+
MIAPaCa2 cells NUXabFlXS3m2b4TvfIlkcXS7IHHzd4F6 MYezJIRigXN? MW\JR|UxKD1iMU[uOkDPxE1? MlyxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdyN{eyNlgoRjJ5MEe3NlI5RC:jPh?=
HeLa cells MWXDfZRwfG:6aXPpeJkh[XO|YYm= M4TmXFMh\GG7cx?= M1LYbWlEPTBiPTCxOk45KM7:TR?= M3r6clxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MEe3NlI5Lz5{N{C3O|IzQDxxYU6=
Raji cells MUDBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? M3zFb|Q5KGh? MUfJR|UxKD1iMUmuN{DPxE1? NF\TO449[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{mxNlE4PSd-Mke5NVIyPzV:L3G+
Raji cells MYrBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? MYS0PEBp NX\rZow5UUN3MDC9JFE6NjNizszN NHnIPYo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OESzNlk1Pid-Mki0N|I6PDZ:L3G+
Raji cells NUfiOm1ySW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[XO|YYm= MnWxO|IhcA>? MoPETWM2OCB;IEG5MlUh|ryP NV7oU5FQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CwNFYyPDNpPkOwNFA3OTR|PD;hQi=>
Raji cells M1XwU2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 NWjDVJBCPDhiaB?= NWPFeo1qUUN3MDC9JFE6NjVizszN NIjtZ5I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{m1OlA{Pyd-Mke5OVYxOzd:L3G+
NAMALWA cells M{XTXWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 MlX3O|IhcA>? M{PqNGlEPTBiPTCxPU43KM7:TR?= NWPuXWd5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CwNFYyPDNpPkOwNFA3OTR|PD;hQi=>
A2780 cells MmLnR5l1d3SxeHnjbZR6KGG|c3H5 M3WwcFMh\GG7cx?= NVXzOYJnTUN3MDC9JFIxNjFizszN NG\tSpg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{C3O|IzQCd-MkewO|czOjh:L3G+
Raji cells NF3ISVlCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= M{TxUFczKGh? MXjJR|UxKD1iMkCuPFgh|ryP M2\6[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7MUS2NVM3Lz5{OUG0OlE{PjxxYU6=
A549 cells MmfrRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZZN{[Xl? M4HUUFczKGh? NGTJdoZKSzVyIE2gNlEvPzlizszN NXjM[4NKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki3N|Q2QDFpPkK4O|M1PThzPD;hQi=>
SW480 cells NWrSTohXS3m2b4TvfIlkcXS7IHHzd4F6 MX6zJIRigXN? NVyzOGhSUUN3MDC9JFI2NjZizszN NX3YTJRvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkewO|czOjhpPkK3NFc4OjJ6PD;hQi=>
Ramos cells M4XJemN6fG:2b4jpZ4l1gSCjc4PhfS=> NHT3eJkzPCCq NYX4b3lZUUN3MDC9JFI5NjdizszN MWG8ZUB1[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)
Water Insoluble
Ethanol '45 mg/mL warmed
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.

  • * 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