Ibrutinib (PCI-32765)

Catalog No.S2680

For research use only.

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.

Ibrutinib (PCI-32765) Chemical Structure

CAS No. 936563-96-1

Selleck's Ibrutinib (PCI-32765) has been cited by 487 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)
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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 MX3GeY5kfGmxbjDhd5NigQ>? MVmyMlUh|ryP NHPhcmM3KGh? MkfQTY5pcWKrdHnvckBw\iCOeX6gdIhwe3Cqb4L5cIF1cW:wIHnuJIh2dWGwIGLlZ|Eh[2WubIOgZZQhOi53IIXNJIlv[3WkYYTl[EBnd3JiNjDodpMh[nliV3XzeIVzdiCkbH;0eIlv\yCvZYToc4Q> M3vUTlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MkKyPFc4Lz5{NUKyNlg4PzxxYU6=
human WSU-NHL cells M1PocWN6fG:2b4jpZ:Kh[XO|YYm= MYG3NkBp NXjZ[492S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hX1OXLV7IUEBk\WyuczDhd5Nme3OnZDDhd{Boem:5dHigbY5pcWKrdHnvckBi\nSncjC3NkBpenNiYomgR4VtdFSrdHXyMWdtdyCudX3pcoV{[2WwdDDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlA6KM7:TR?= MnXRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7MUWyPVEoRjJ2OUG1NlkyRC:jPh?=
human SU-DHL6 cells M{H0UWN6fG:2b4jpZ:Kh[XO|YYm= MlO2O|IhcA>? MVjDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTWU1FUEx4IHPlcIx{KGG|c3Xzd4VlKGG|IHfyc5d1cCCrbnjpZol1cW:wIHHmeIVzKDd{IHjyd{BjgSCFZXzsWIl1\XJvR3zvJIx2dWmwZYPj[Y51KGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwNUig{txONg>? NWPhSoRKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5NVUzQTFpPkK0PVE2OjlzPD;hQi=>
human DOHH2 cells Mm\YR5l1d3SxeHnjxsBie3OjeR?= MWi3NkBp MlrZR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gSG9JUDJiY3XscJMh[XO|ZYPz[YQh[XNiZ4Lve5RpKGmwaHnibZRqd25iYX\0[ZIhPzJiaILzJIJ6KEOnbHzUbZRmei2JbH:gcJVucW6nc3PlcpQh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC52MTFOwG0v MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDlzNUK5NUc,OjR7MUWyPVE9N2F-
Sf9 cells M1PVTWZ2dmO2aX;uJIF{e2G7 NWX5PIJ1OSCq NFvQWpVKdmirYnn0bY9vKG:oIFzZUk1CKGW6cILld5Nm\CCrbjDT[lkh[2WubIOgZYZ1\XJiNkCgcYlveyCkeTDUVk1HWkWWIFHzd4F6NCCLQ{WwQVAvOiEQvF2u M{L6fFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzOUW4OVQ4Lz5{MUm1PFU1PzxxYU6=
human Ramos cells MoDVSpVv[3Srb36gZZN{[Xl? NYS5W4FFOSCq MUnJcohq[mm2aX;uJI9nKEK2azDpckBpfW2jbjDSZY1weyClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJHBNSy2pYX3tZVIheGixc4Doc5J6dGG2aX;uJIF1KFS7ckGyNVch[W[2ZYKgNUBpeiCkeTDX[ZN1\XKwIHLsc5Qh[W6jbInzbZMtKEmFNUC9NVQhdk1w MnXOQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7MUWyPVEoRjJ2OUG1NlkyRC:jPh?=
human Pfeiffer cells MoXiSpVv[3Srb36gZZN{[Xl? NH;CVXg4OiCq M3W5R2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHBn\WmoZnXyJINmdGy|IHHzd4V{e2WmIHHzJIdzd3e2aDDpcohq[mm2aX;uJIFnfGW{IEeyJIhzeyCkeTDD[YxtXGm2ZYKtS4xwKGy3bXnu[ZNk\W62IHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUKgcm0v NFP0WIg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEmxOVI6OSd-MkS5NVUzQTF:L3G+
Sf9 cells M4XTPGZ2dmO2aX;uJIF{e2G7 NVO2N5NTOSCq Mm\hTY5pcWKrdHnvckBw\iCqdX3hckBnfWyuLXzlcod1cCCEVFug[ZhxemW|c3XkJIlvKFOoOTDj[YxteyC3c3nu[{BHSU1vU4LjeIll\SCyZYD0bYRmKGG|IIP1ZpN1emG2ZTDh[pRmeiB4MDDtbY5{KGK7IGTSMWZTTVRiQYPzZZnwxIxiSVO1NF0xNjVibl2u NGnLc|M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUm1PFU1Pyd-MkG5OVg2PDd:L3G+
Sf9 insect cells NVzzOYxjTnWwY4Tpc44h[XO|YYm= M2DuPVYxKG2rboO= MnnnTWM2OCB;IECuNFAxOyEQvF2= MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTF2NkGzOkc,OjlzNE[xN|Y9N2F-
sf9 cells M1qycmZ2dmO2aX;uJIF{e2G7 MUTJR|UxKD1iMD6wNFA{KM7:TR?= NXPYcHVvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke5PVQ4OzZpPkK3PVk1PzN4PD;hQi=>
Sf9 insect cells Mo[ySpVv[3Srb36gZZN{[Xl? Ml;SOlAhdWmwcx?= NIG2S3hKSzVyIE2gNE4xODB|NDFOwG0> NGfEXJQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{mxNlE4PSd-Mke5NVIyPzV:L3G+
Sf9 insect cells MlXXSpVv[3Srb36gZZN{[Xl? NYnveol4PjBibXnudy=> MXvJR|UxKD1iMD6wNFA{PCEQvF2= MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDR|Mkm0Okc,Ojh2M{K5OFY9N2F-
Sf9 insect cells NW\KZ2ZKTnWwY4Tpc44h[XO|YYm= MX:2NEBucW6| MWnJR|UxKD1iMD6wNFA{PCEQvF2= MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzl3NkCzO{c,Ojd7NU[wN|c9N2F-
Sf9 cells M1H1WGZ2dmO2aX;uJIF{e2G7 M{XJSFYxKG2rboO= MVXJR|UxKD1iMD6wNFA1KM7:TR?= MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODByNkG0N{c,OzByME[xOFM9N2F-
Sf9 cells NILSWYRHfW6ldHnvckBie3OjeR?= NXTlUVczPjBibXnudy=> MXfJR|UxKD1iMD6wNFA2KM7:TR?= MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTl3OEW0O{c,OjF7NUi1OFc9N2F-
Ramos cells NEDlSVNHfW6ldHnvckBie3OjeR?= NYT5XFh6OSCq Mnz2TWM2OCB;IECuNFAxPSEQvF2= NHPFPFY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEK4NFI3OSd-MkiyPFAzPjF:L3G+
Sf9 cells NWSxWYxPTnWwY4Tpc44h[XO|YYm= MlXEOlAhdWmwcx?= MWHJR|UxKD1iMD6wNFEh|ryP Moq4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzByN{e2NFgoRjNyMEe3OlA5RC:jPh?=
Pfeiffer cells M2nYNWN6fG:2b4jpZ4l1gSCjc4PhfS=> NVrGSXZ{PzJiaB?= MojrS2k2OCB;IECuNFAzKM7:TR?= Mor2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7MUWyPVEoRjJ2OUG1NlkyRC:jPh?=
B cells NH\vTohHfW6ldHnvckBie3OjeR?= NVT2PVdnOSCq MVrJR|UxKD1iMD6wNFQ3KM7:TR?= M1u2ZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMkmwPVg5Lz5|MEK5NFk5QDxxYU6=
Sf9 insect cells MV\GeY5kfGmxbjDhd5NigQ>? MkfZNkB1dyB4MDDtbY5{ MXTLbUA:KDBwMEC0PEDPxE1? MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDNzNUW5O{c,Ojh|MUW1PVc9N2F-
Ramos cells M1\W[WZ2dmO2aX;uJIF{e2G7 M2jvPVEhcA>? NXXLR3Z1UUN3MDC9JFAvODB5NTFOwG0> M{\2blxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUG1NlkyLz5{NEmxOVI6OTxxYU6=
Sf9 insect cells NILSTGdHfW6ldHnvckBie3OjeR?= MofPOlAhdWmwcx?= NWPQe|gzUUN3MDC9JFAvODB6IN88US=> MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDNzNUW5O{c,Ojh|MUW1PVc9N2F-
TMD8 cells M2nzWGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 M4ToS|czKGh? M2PpOmlEPTBiPTCwMlAyKM7:TR?= M{PFTVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7N{G1NFI{Lz5{OUexOVAzOzxxYU6=
CD19+ B cells MYXGeY5kfGmxbjDhd5NigQ>? M1X1PVEhcA>? NYXvZmplUUN3MDC9JFAvODF{IN88US=> M3nzc|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEW3PVgzLz5{OUS1O|k5OjxxYU6=
Sf9 insect cells M1jRPGZ2dmO2aX;uJIF{e2G7 MkTXOlAhdWmwcx?= NXnCWI5DUUN3MDC9JFAvODF{IN88US=> M1\oN|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6M{G1OVk4Lz5{OEOxOVU6PzxxYU6=
Ramos cells NYXJO3pzTnWwY4Tpc44h[XO|YYm= MoD6NUBp Mk\wTWM2OCB;IECuNFE1KM7:TR?= MlPuQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7MUWyPVEoRjJ2OUG1NlkyRC:jPh?=
Sf9 insect cells MYPGeY5kfGmxbjDhd5NigQ>? NYDxPGxnOSCq M1HRemlEPTBiPTCwMlAyPDRizszN M2\VUVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7N{G1NFI{Lz5{OUexOVAzOzxxYU6=
Sf9 insect cells NVTx[plXTnWwY4Tpc44h[XO|YYm= NWDhUXlDPjBibXnudy=> NHf0VoVKSzVyIE2gNE4xOTZzIN88US=> MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTF2NkGzOkc,OjlzNE[xN|Y9N2F-
HCC827 cells M3XXXGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 M4ewRVczKGh? Mn3JTWM2OCB;IECuNFM6KM7:TR?= M1nOeVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6N{O0OVgyLz5{OEezOFU5OTxxYU6=
PC9 cells NF3XVIVHfW6ldHnvckBie3OjeR?= M2rXfFczKGh? MnXNS2k2OCB;IECuNFUh|ryP NHyyUGI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEK4NlEzOid-MkiyPFIyOjJ:L3G+
Sf9 cells NH7uTGJHfW6ldHnvckBie3OjeR?= M3\ib|YxKG2rboO= NFe1XpJKSzVyIE2gNE4yKM7:TR?= NFvicXI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MECwOlE1Oyd-M{CwNFYyPDN:L3G+
H3255 cells Mo\0SpVv[3Srb36gZZN{[Xl? NXLhdYtiPzJiaB?= MnTyS2k2OCB;IECuNVEh|ryP NGqxTWo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEK4NlEzOid-MkiyPFIyOjJ:L3G+
BaF3 cells MoLzSpVv[3Srb36gZZN{[Xl? MWq3NkBp MU\HTVUxKD1iMD6xNkDPxE1? NGi0[JQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nk[zNFU2Oyd-Mk[2N|A2PTN:L3G+
BAF3 cells NUH1V411SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[XO|YYm= NUjqOmJ5PzJiaB?= M3vOOmdKPTBiPTCwMlEzKM7:TR?= NHK0dnU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEm1OlkzOyd-Mki5OVY6OjN:L3G+
Sf9 insect cells NEHDbGlHfW6ldHnvckBie3OjeR?= MlnHOlAhdWmwcx?= MmDDTWM2OCB;IECuNVI{KM7:TR?= NYraW3R2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkizNVU2QTdpPkK4N|E2PTl5PD;hQi=>
Sf9 insect cells MYXGeY5kfGmxbjDhd5NigQ>? MknDOlAhdWmwcx?= NILFO3NKSzVyIE2gNE4yPDZizszN MlrGQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh|MUW1PVcoRjJ6M{G1OVk4RC:jPh?=
BAF3 cells MWTGeY5kfGmxbjDhd5NigQ>? Ml3yO|IhcA>? M3S4emdKPTBiPTCwMlE3KM7:TR?= NUW2OYVJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkiyPFIyOjJpPkK4NlgzOTJ{PD;hQi=>
Sf9 cells NYPGXmRCTnWwY4Tpc44h[XO|YYm= NV3pVm17PjBibXnudy=> MnTFTWM2OCB;IECuNkDPxE1? MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTl3OEW0O{c,OjF7NUi1OFc9N2F-
MV411 cells NXz0[4VOT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NV\uPIZkT0l3MDC9JFAvOjVizszN NWnMd|Y3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkizNVU2QTdpPkK4N|E2PTl5PD;hQi=>
MV4-11 cells MnTnRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZZN{[Xl? NEH6ZpI4OiCq NVPUTWNiT0l3MDC9JFAvOzNizszN NW\ofpVNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[2N|A2PTNpPkK2OlMxPTV|PD;hQi=>
MV4-11 cells NHLIPHVCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= MnHKO|IhcA>? NHfHdndIUTVyIE2gNE4{OyEQvF2= M4\TdVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6OUW2PVI{Lz5{OEm1OlkzOzxxYU6=
DOHH2 cells NITvN5NEgXSxdH;4bYNqfHliYYPzZZk> MYW3NkBp NInNclRIUTVyIE2gNE41OSEQvF2= Mnf0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7MUWyPVEoRjJ2OUG1NlkyRC:jPh?=
HCC827 cells MUnBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? NX3JdI1kQTZiaB?= NF20Z|RGSzVyIE2gNE41PSEQvF2= MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDh3M{W3OUc,Ojh6NUO1O|U9N2F-
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Assay
Methods Test Index PMID
Western blot pEGFR(Tyr1068) / EGFR ; pBTK / pPLCγ2 / pAKT / pERK / pJNK 28061447 23940282
Immunofluorescence CD11b ; COX-2 30231870
ELISA hTNFα ; IL-10 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 (from reference)

Kinase Assay:

[1]

  • 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]

  • 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.

Animal Research:

[1]

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

Solubility (25°C)

In vitro

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

Chemical Information

Molecular Weight 440.5
Formula

C25H24N6O2

CAS No. 936563-96-1
Storage 3 years -20°C powder
2 years -80°C in solvent
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)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04665115 Withdrawn 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 2021 Phase 2
NCT05105841 Recruiting Drug: Venetoclax|Drug: Ibrutinib|Drug: Obinutuzumab Chronic Lymphocytic Leukemia (CLL)|Small Lymphocytic Lymphoma (SLL) AbbVie November 8 2021 Phase 2
NCT04876092 Recruiting Drug: JNJ-67856633|Drug: Ibrutinib Leukemia Lymphocytic Chronic B-Cell|Lymphoma Non-Hodgkin Janssen Research & Development LLC July 28 2021 Phase 1
NCT04294641 Recruiting Drug: Ibrutinib Chronic GVHD National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) May 10 2021 Phase 2
NCT05429918 Recruiting -- Mantle Cell Lymphoma Peking University Third Hospital|The Second Affiliated Hospital of Dalian Medical University|Peking University First Hospital|Beijing Hospital|Beijing Tsinghua Changgeng Hospital|China-Japan Friendship Hospital|Chinese PLA General Hospital|First Affiliated Hospital of Harbin Medical University|Baotou Cancer Hospital|Beijing Shijitan Hospital Capital Medical University|Shanxi Province Cancer Hospital|Beijing Naval General Hospital|First Hospital of China Medical University|Jilin Provincial Tumor Hospital|Shengjing Hospital|307 Hospital of PLA|Peking Union Medical College Hospital|Harbin Medical University|Beijing Tongren Hospital December 30 2020 --
NCT05406154 Recruiting -- Mantle Cell Lymphoma (MCL) Peking University Third Hospital|Peking Union Medical College Hospital|The Second Affiliated Hospital of Dalian Medical University|Peking University First Hospital|Beijing Tongren Hospital|Beijing Hospital|Beijing Tsinghua Changgeng Hospital|China-Japan Friendship Hospital|307 Hospital of PLA|Chinese PLA General Hospital|First Affiliated Hospital of Harbin Medical University|Harbin Medical University|Baotou Cancer Hospital|Beijing Shijitan Hospital Capital Medical University|Shanxi Province Cancer Hospital|Beijing Naval General Hospital|First Hospital of China Medical University|Jilin Provincial Tumor Hospital|Shengjing Hospital December 30 2020 --

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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

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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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