Ibrutinib (PCI-32765)

For research use only.

Catalog No.S2680

421 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 421 publications

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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 MomwSpVv[3Srb36gZZN{[Xl? NGnTcHczNjVizszN MlTXOkBp NWfYbIdbUW6qaXLpeIlwdiCxZjDMfY4heGixc4Doc5J6dGG2aX;uJIlvKGi3bXHuJHJm[zFiY3XscJMh[XRiMj61JJVOKGmwY4XiZZRm\CCob4KgOkBpenNiYomgW4V{fGW{bjDicI91fGmwZzDt[ZRpd2R? NHLxeGY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUKyNlg4Pyd-MkWyNlI5Pzd:L3G+
human WSU-NHL cells NUPLTXg1S3m2b4TvfIlkyqCjc4PhfS=> NY\VPXNsPzJiaB?= Moe4R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gW3NWNU6KTDDj[YxteyCjc4Pld5Nm\CCjczDndo94fGhiaX7obYJqfGmxbjDh[pRmeiB5MjDodpMh[nliQ3XscHRqfGW{LVfsc{BtfW2rbnXzZ4VvfCClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zLkC5JO69VQ>? NFT0dXg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEmxOVI6OSd-MkS5NVUzQTF:L3G+
human SU-DHL6 cells MUnDfZRwfG:6aXRCpIF{e2G7 M2\E[FczKGh? M4jUeWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHNWNUSKTE[gZ4VtdHNiYYPz[ZN{\WRiYYOg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiN{KgbJJ{KGK7IFPlcIxVcXSncj3HcI8hdHWvaX7ld4NmdnRiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD61PEDPxE1w NITMT5I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEmxOVI6OSd-MkS5NVUzQTF:L3G+
human DOHH2 cells Mkf4R5l1d3SxeHnjxsBie3OjeR?= MXu3NkBp Ml3HR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gSG9JUDJiY3XscJMh[XO|ZYPz[YQh[XNiZ4Lve5RpKGmwaHnibZRqd25iYX\0[ZIhPzJiaILzJIJ6KEOnbHzUbZRmei2JbH:gcJVucW6nc3PlcpQh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC52MTFOwG0v MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDlzNUK5NUc,OjR7MUWyPVE9N2F-
Sf9 cells MX7GeY5kfGmxbjDhd5NigQ>? NXn0cXFXOSCq NX30eGVuUW6qaXLpeIlwdiCxZjDMXW4uSSCneIDy[ZN{\WRiaX6gV4Y6KGOnbHzzJIFnfGW{IE[wJI1qdnNiYomgWHIuTlKHVDDBd5NigSxiSVO1NF0xNjJizszNMi=> NFnlRWs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUm1PFU1Pyd-MkG5OVg2PDd:L3G+
human Ramos cells Mn;pSpVv[3Srb36gZZN{[Xl? M1HmclEhcA>? M2TyWGlvcGmkaYTpc44hd2ZiQoTrJIlvKGi3bXHuJHJidW:|IHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhWEyFLXfhcY1iOiCyaH;zdIhwenmuYYTpc44h[XRiVInyNVIyPyCjZoTldkAyKGi{IHL5JHdme3Sncn6gZoxwfCCjbnHsfZNqeyxiSVO1NF0yPCCwTT6= MoHxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7MUWyPVEoRjJ2OUG1NlkyRC:jPh?=
human Pfeiffer cells MlP6SpVv[3Srb36gZZN{[Xl? MVO3NkBp MYLDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDQ[oVq\m[ncjDj[YxteyCjc4Pld5Nm\CCjczDndo94fGhiaX7obYJqfGmxbjDh[pRmeiB5MjDodpMh[nliQ3XscHRqfGW{LVfsc{BtfW2rbnXzZ4VvfCClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1{IH7NMi=> NEL4dlc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEmxOVI6OSd-MkS5NVUzQTF:L3G+
Sf9 cells M3f0RmZ2dmO2aX;uJIF{e2G7 MmPSNUBp MYPJcohq[mm2aX;uJI9nKGi3bXHuJIZ2dGxvbHXu[5RpKEKWSzDlfJBz\XO|ZXSgbY4hW2Z7IHPlcIx{KHW|aX7nJGZCVS2VcnP0bYRmKHCncITp[IUh[XNic4Xid5Rz[XSnIHHmeIVzKDZyIH3pcpMh[nliVGKtSnJGXCCDc4Phfg+9lCCLQ{WwQVAvPSCwTT6= NVGwOlhbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG5OVg2PDdpPkKxPVU5PTR5PD;hQi=>
Sf9 insect cells M3jNfmZ2dmO2aX;uJIF{e2G7 MofVOlAhdWmwcx?= MV7JR|UxKD1iMD6wNFA{KM7:TR?= NHfwcIY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUG0OlE{Pid-MkmxOFYyOzZ:L3G+
sf9 cells MnfhSpVv[3Srb36gZZN{[Xl? M4nBT2lEPTBiPTCwMlAxODNizszN NUju[4RtRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke5PVQ4OzZpPkK3PVk1PzN4PD;hQi=>
Sf9 insect cells MVnGeY5kfGmxbjDhd5NigQ>? MUC2NEBucW6| NFfXV4FKSzVyIE2gNE4xODB|NDFOwG0> MnmwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd7MUKxO|UoRjJ5OUGyNVc2RC:jPh?=
Sf9 insect cells MkXUSpVv[3Srb36gZZN{[Xl? NF;hco43OCCvaX7z MmO3TWM2OCB;IECuNFAxOzRizszN NVfYb49kRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki0N|I6PDZpPkK4OFMzQTR4PD;hQi=>
Sf9 insect cells MmSySpVv[3Srb36gZZN{[Xl? Mn[4OlAhdWmwcx?= MWXJR|UxKD1iMD6wNFA{PCEQvF2= MljzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd7NU[wN|coRjJ5OUW2NFM4RC:jPh?=
Sf9 cells MnfESpVv[3Srb36gZZN{[Xl? MYq2NEBucW6| M3TXO2lEPTBiPTCwMlAxODRizszN NWq1XpF{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CwNFYyPDNpPkOwNFA3OTR|PD;hQi=>
Sf9 cells M3uyXmZ2dmO2aX;uJIF{e2G7 NFLGbY43OCCvaX7z M1rtNmlEPTBiPTCwMlAxODVizszN NV7oTpdDRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG5OVg2PDdpPkKxPVU5PTR5PD;hQi=>
Ramos cells NITZZ3hHfW6ldHnvckBie3OjeR?= NHq1WXYyKGh? M1jBWGlEPTBiPTCwMlAxODVizszN NULiZYlHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkiyPFAzPjFpPkK4NlgxOjZzPD;hQi=>
Sf9 cells NEHUV3BHfW6ldHnvckBie3OjeR?= MlK3OlAhdWmwcx?= M1fxNGlEPTBiPTCwMlAxOSEQvF2= NYr1W5Q3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CwO|c3ODhpPkOwNFc4PjB6PD;hQi=>
Pfeiffer cells MnLjR5l1d3SxeHnjbZR6KGG|c3H5 MWS3NkBp NUCwV3BoT0l3MDC9JFAvODB{IN88US=> M2jN[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUG1NlkyLz5{NEmxOVI6OTxxYU6=
B cells NV\UcHV5TnWwY4Tpc44h[XO|YYm= NH:zfHgyKGh? MWDJR|UxKD1iMD6wNFQ3KM7:TR?= MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODJ7MEm4PEc,OzB{OUC5PFg9N2F-
Sf9 insect cells NHzh[2dHfW6ldHnvckBie3OjeR?= NHXDNoEzKHSxIE[wJI1qdnN? MXnLbUA:KDBwMEC0PEDPxE1? Ml3CQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh|MUW1PVcoRjJ6M{G1OVk4RC:jPh?=
Ramos cells NE\6UldHfW6ldHnvckBie3OjeR?= NYjqRYl[OSCq NID2WIdKSzVyIE2gNE4xODd3IN88US=> NXTBVI5zRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5NVUzQTFpPkK0PVE2OjlzPD;hQi=>
Sf9 insect cells NG\IflVHfW6ldHnvckBie3OjeR?= MX[2NEBucW6| NV3nZ5o2UUN3MDC9JFAvODB6IN88US=> M3Pmd|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6M{G1OVk4Lz5{OEOxOVU6PzxxYU6=
TMD8 cells NHL0WoJCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= NHXoTYo4OiCq MYPJR|UxKD1iMD6wNUDPxE1? M{ntWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7N{G1NFI{Lz5{OUexOVAzOzxxYU6=
CD19+ B cells MmfwSpVv[3Srb36gZZN{[Xl? NH;yPHAyKGh? MYfJR|UxKD1iMD6wNVIh|ryP MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR3N{m4Nkc,Ojl2NUe5PFI9N2F-
Sf9 insect cells M1[zPWZ2dmO2aX;uJIF{e2G7 NIK0dZc3OCCvaX7z MmqwTWM2OCB;IECuNFEzKM7:TR?= MkG0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh|MUW1PVcoRjJ6M{G1OVk4RC:jPh?=
Ramos cells NFn6dFJHfW6ldHnvckBie3OjeR?= MmTMNUBp NV\pRZlsUUN3MDC9JFAvODF2IN88US=> NW\2dGQ4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5NVUzQTFpPkK0PVE2OjlzPD;hQi=>
Sf9 insect cells MWTGeY5kfGmxbjDhd5NigQ>? NVfVZ5dkOSCq M4rJWmlEPTBiPTCwMlAyPDRizszN M3XodVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7N{G1NFI{Lz5{OUexOVAzOzxxYU6=
Sf9 insect cells M3fRcGZ2dmO2aX;uJIF{e2G7 MoiyOlAhdWmwcx?= MoPRTWM2OCB;IECuNFE3OSEQvF2= NX25WGh5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmxOFYyOzZpPkK5NVQ3OTN4PD;hQi=>
HCC827 cells Mmm5RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZZN{[Xl? MlSzO|IhcA>? M3vTOmlEPTBiPTCwMlA{QSEQvF2= NULVOYlmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki3N|Q2QDFpPkK4O|M1PThzPD;hQi=>
PC9 cells NWXneJhmTnWwY4Tpc44h[XO|YYm= Mm\6O|IhcA>? MV7HTVUxKD1iMD6wOUDPxE1? M1z3RVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MkiyNVIzLz5{OEK4NlEzOjxxYU6=
Sf9 cells M3zkTmZ2dmO2aX;uJIF{e2G7 Mn3kOlAhdWmwcx?= MnrHTWM2OCB;IECuNUDPxE1? MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODByNkG0N{c,OzByME[xOFM9N2F-
H3255 cells MoPiSpVv[3Srb36gZZN{[Xl? M2HIVlczKGh? M3v0O2dKPTBiPTCwMlEyKM7:TR?= NVW1Z4pDRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkiyPFIyOjJpPkK4NlgzOTJ{PD;hQi=>
BaF3 cells MYDGeY5kfGmxbjDhd5NigQ>? Mn7yO|IhcA>? MV;HTVUxKD1iMD6xNkDPxE1? M17kdFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NkOwOVU{Lz5{Nk[zNFU2OzxxYU6=
BAF3 cells NVnkZm5bSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[XO|YYm= M4jr[lczKGh? MVXHTVUxKD1iMD6xNkDPxE1? NEjNOZU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEm1OlkzOyd-Mki5OVY6OjN:L3G+
Sf9 insect cells NGnodXhHfW6ldHnvckBie3OjeR?= MkTqOlAhdWmwcx?= NV7WbZBQUUN3MDC9JFAvOTJ|IN88US=> Mk\0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh|MUW1PVcoRjJ6M{G1OVk4RC:jPh?=
Sf9 insect cells MVjGeY5kfGmxbjDhd5NigQ>? M3vvfFYxKG2rboO= MWTJR|UxKD1iMD6xOFYh|ryP NWTmNJZjRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkizNVU2QTdpPkK4N|E2PTl5PD;hQi=>
BAF3 cells MmrnSpVv[3Srb36gZZN{[Xl? MXS3NkBp M{f5XmdKPTBiPTCwMlE3KM7:TR?= M3O0RVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MkiyNVIzLz5{OEK4NlEzOjxxYU6=
Sf9 cells NVq0WGg{TnWwY4Tpc44h[XO|YYm= MXG2NEBucW6| M17vc2lEPTBiPTCwMlIh|ryP NG[wNpc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUm1PFU1Pyd-MkG5OVg2PDd:L3G+
MV411 cells NETLfpZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MmnwS2k2OCB;IECuNlUh|ryP NXvZRpppRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkizNVU2QTdpPkK4N|E2PTl5PD;hQi=>
MV4-11 cells NHTPR4pCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= MlPOO|IhcA>? NVGwVVNNT0l3MDC9JFAvOzNizszN M3;YelxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NkOwOVU{Lz5{Nk[zNFU2OzxxYU6=
MV4-11 cells NYCwdmx1SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[XO|YYm= Mo\nO|IhcA>? NFH4WVJIUTVyIE2gNE4{OyEQvF2= M13tT|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6OUW2PVI{Lz5{OEm1OlkzOzxxYU6=
DOHH2 cells NH;VVHlEgXSxdH;4bYNqfHliYYPzZZk> MYG3NkBp MXvHTVUxKD1iMD60NUDPxE1? MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDlzNUK5NUc,OjR7MUWyPVE9N2F-
HCC827 cells NVnY[mtFSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[XO|YYm= NGTHVYE6PiCq NHzRb2pGSzVyIE2gNE41PSEQvF2= MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDh3M{W3OUc,Ojh6NUO1O|U9N2F-
SU-DHL6 cells MlHPR5l1d3SxeHnjbZR6KGG|c3H5 MXS3NkBp NWDWVHZlT0l3MDC9JFAvPThizszN NITrd4I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEmxOVI6OSd-MkS5NVUzQTF:L3G+
M07e cells NHv5bYhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NGH5NJpIUTVyIE2gNE42QSEQvF2= NVTZOINuRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkizNVU2QTdpPkK4N|E2PTl5PD;hQi=>
NCI-H1975 cells NH\pdJNCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= MkG5PVYhcA>? MmnYSWM2OCB;IECuOlQh|ryP NUD3OlNyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki4OVM2PzVpPkK4PFU{PTd3PD;hQi=>
SU-DHL-2 cells NIrJdnhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MofXS2k2OCB;IECuOlQh|ryP NGHQVmU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEOxOVU6Pyd-MkizNVU2QTd:L3G+
HEK293T cells NYHyfFk{TnWwY4Tpc44h[XO|YYm= NX3mT4dOOSCq M37mVWlEPTBiPTCwMlkh|ryP NUjMR2g1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkiyPFAzPjFpPkK4NlgxOjZzPD;hQi=>
Ramos cells MmfERY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZZN{[Xl? M3LSe|czKGh? NYDrZpFYUUN3MDC9JFAvQTJizszN NEPyVYo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUexOVAzOyd-Mkm3NVUxOjN:L3G+
BA/F3 cells NFzxfmFCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= MX[3NkBp NWT0dVFrUUN3MDC9JFEh|ryP NGTKbG89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkK1PFUzOSd-Mk[yOVg2OjF:L3G+
WSU-NHL cells NIKxSHpEgXSxdH;4bYNqfHliYYPzZZk> M1;1e|czKGh? MVjHTVUxKD1iMT6wPUDPxE1? M{f0SFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUG1NlkyLz5{NEmxOVI6OTxxYU6=
NCI-H1975 cells M13vUmZ2dmO2aX;uJIF{e2G7 NYTIVIVrPzJiaB?= NFe2SpNIUTVyIE2gNU4zKM7:TR?= Ml3CQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh{OEKxNlIoRjJ6MkiyNVIzRC:jPh?=
NCI-H1975 cells M1OxWmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 MXS3NkBp MmPzTWM2OCB;IEGuNlch|ryP Mnm2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh5M{S1PFEoRjJ6N{O0OVgyRC:jPh?=
Raji cells NITMeZhCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= MoHYOFghcA>? NGnnNWRKSzVyIE2gNU41QSEQvF2= MlLSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl3NkeyPVUoRjJ7NU[3Nlk2RC:jPh?=
Pfeiffer cells MlfJS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NX7Z[3cxT0l3MDC9JFEvPiEQvF2= NX20RWV6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkizNVU2QTdpPkK4N|E2PTl5PD;hQi=>
A431 cells MVzBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? NHy3T5o6PiCq MWjFR|UxKD1iMj6zPEDPxE1? NW\QeHlNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki4OVM2PzVpPkK4PFU{PTd3PD;hQi=>
BAF3 cells NXT2VnM3SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[XO|YYm= NIr1RVk4OiCq M13XS2dKPTBiPTCyMlUh|ryP M3z5NFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6OUW2PVI{Lz5{OEm1OlkzOzxxYU6=
U937 cells NYLZTIl7T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NF7IbYNIUTVyIE2gNk46KM7:TR?= M4DPfVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6M{G1OVk4Lz5{OEOxOVU6PzxxYU6=
NB4 cells M4CxNWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MoOxS2k2OCB;IEOg{txO NXnubGV2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkizNVU2QTdpPkK4N|E2PTl5PD;hQi=>
Ramos cells NUjqTHdbT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M4XJeWdKPTBiPTCzMlQh|ryP MojwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh|MUW1PVcoRjJ6M{G1OVk4RC:jPh?=
SKM1 cells NEP0bWFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NVLFbIFJT0l3MDC9JFMvPiEQvF2= NXfIXWY1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkizNVU2QTdpPkK4N|E2PTl5PD;hQi=>
U2932 cells M361fGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MlnXS2k2OCB;IESuOEDPxE1? MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDNzNUW5O{c,Ojh|MUW1PVc9N2F-
Ramos cells MYrBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? MVO3NkBp NFHEcmtKSzVyIE2gOU4yPCEQvF2= MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODByNkG0N{c,OzByME[xOFM9N2F-
Ramos cells MXPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? MojCOFghcA>? M4PQOWlEPTBiPTC1MlE1KM7:TR?= MnHDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd7NU[wN|coRjJ5OUW2NFM4RC:jPh?=
Ramos cells MonjRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZZN{[Xl? NGTDWm41QCCq NF3ON|JKSzVyIE2gOU45QCEQvF2= MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDR|Mkm0Okc,Ojh2M{K5OFY9N2F-
Ramos cells NYnHSGp{SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[XO|YYm= MVq3NkBp M1\kWWlEPTBiPTC2MlYzKM7:TR?= NInxTWo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUG0OlE{Pid-MkmxOFYyOzZ:L3G+
K562 cells M{jNemFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 MnnzOFghcA>? MkPCTWM2OCB;IEeuOUDPxE1? NUPiXY9oRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CwO|c3ODhpPkOwNFc4PjB6PD;hQi=>
HL60 cells M1\xTWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 MmXkOFghcA>? M2nX[WlEPTBiPTC4JO69VQ>? NFrvemE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEC3O|YxQCd-M{CwO|c3ODh:L3G+
Ramos cells MoL5RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZZN{[Xl? MXq0PEBp MXrJR|UxKD1iOD6xNUDPxE1? NVvkPXc{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke5PVQ4OzZpPkK3PVk1PzN4PD;hQi=>
Ramos cells MUTBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? MVK0PEBp M1e5O2lEPTBiPTC4MlI3KM7:TR?= NUO3Rox1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm1OlczQTVpPkK5OVY4Ojl3PD;hQi=>
OCI-AML3 cells Ml7pS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M4T5OWdKPTBiPTC5MlIh|ryP NI\ZeIY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEOxOVU6Pyd-MkizNVU2QTd:L3G+
BAF3 cells MnzoR5l1d3SxeHnjbZR6KGG|c3H5 NXu1ToJZPzJiaB?= M4D3XWdKPTBiPTCxNEDPxE1? MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjZ|MEW1N{c,OjZ4M{C1OVM9N2F-
BAF3 cells M3nnW2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 NYXQS5gzPzJiaB?= MlewS2k2OCB;IEGwJO69VQ>? MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDl3NkmyN{c,Ojh7NU[5NlM9N2F-
BAF3 cells M1XGSWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NYruPZlbPzJiaB?= MmjiS2k2OCB;IEGwJO69VQ>? NEPYSHk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEK4NlEzOid-MkiyPFIyOjJ:L3G+
NAMALWA cells Mo\IRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZZN{[Xl? NEfaSWY4OiCq MkHGTWM2OCB;IEGwMlQ2KM7:TR?= NXrSXGFLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmxOFYyOzZpPkK5NVQ3OTN4PD;hQi=>
Ramos cells NHTaXHVCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= Mn\JOFghcA>? MkLOTWM2OCB;IEGyMlYh|ryP Ml\YQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd7MUKxO|UoRjJ5OUGyNVc2RC:jPh?=
Raji cells NFqyUotCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= M3zTVlQ5KGh? NGjqUmZKSzVyIE2gNVQvOiEQvF2= MnvaQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzByN{e2NFgoRjNyMEe3OlA5RC:jPh?=
Raji cells MYfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? MV[0PEBp M3;BZmlEPTBiPTCxOU4zKM7:TR?= M2nBblxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5OUm0O|M3Lz5{N{m5OFc{PjxxYU6=
MIAPaCa2 cells M1HNSmN6fG:2b4jpZ4l1gSCjc4PhfS=> NXjQd4Y1OyCmYYnz NYHLeJFiUUN3MDC9JFE3NjZizszN NFXTNog9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{C3O|IzQCd-MkewO|czOjh:L3G+
HeLa cells MYDDfZRwfG:6aXPpeJkh[XO|YYm= M3j6cVMh\GG7cx?= NWW0TnBtUUN3MDC9JFE3NjhizszN MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzB5N{KyPEc,OjdyN{eyNlg9N2F-
Raji cells M4HhbGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 NYTjdIpFPDhiaB?= NFrzPWFKSzVyIE2gNVkvOyEQvF2= MkS0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd7MUKxO|UoRjJ5OUGyNVc2RC:jPh?=
Raji cells M2fuOGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 MmfEOFghcA>? NULY[GdKUUN3MDC9JFE6NjNizszN MknrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh2M{K5OFYoRjJ6NEOyPVQ3RC:jPh?=
Raji cells NHL5OndCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= NEPHeWE4OiCq M3rxbGlEPTBiPTCxPU42KM7:TR?= NV36PGZJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CwNFYyPDNpPkOwNFA3OTR|PD;hQi=>
Raji cells MmHKRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZZN{[Xl? MkmzOFghcA>? M3HvNGlEPTBiPTCxPU42KM7:TR?= NH3KPWU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{m1OlA{Pyd-Mke5OVYxOzd:L3G+
NAMALWA cells NILNSFJCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= NVPxNVJqPzJiaB?= MYPJR|UxKD1iMUmuOkDPxE1? M1vOeVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMEC2NVQ{Lz5|MECwOlE1OzxxYU6=
A2780 cells Mn;wR5l1d3SxeHnjbZR6KGG|c3H5 NYTBWFVbOyCmYYnz M4q1SWVEPTBiPTCyNE4yKM7:TR?= NVraRVQ3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkewO|czOjhpPkK3NFc4OjJ6PD;hQi=>
Raji cells NXLmbWZWSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[XO|YYm= M2X5O|czKGh? M3v6N2lEPTBiPTCyNE45QCEQvF2= MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTF2NkGzOkc,OjlzNE[xN|Y9N2F-
A549 cells MY\BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? MorBO|IhcA>? MnjJTWM2OCB;IEKxMlc6KM7:TR?= M1j1Z|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6N{O0OVgyLz5{OEezOFU5OTxxYU6=
SW480 cells NGrCPYhEgXSxdH;4bYNqfHliYYPzZZk> NGe4T4s{KGSjeYO= MoLsTWM2OCB;IEK1MlYh|ryP NWL6RYRvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkewO|czOjhpPkK3NFc4OjJ6PD;hQi=>
Ramos cells MVvDfZRwfG:6aXPpeJkh[XO|YYm= MXSyOEBp M{LNd2lEPTBiPTCyPE44KM7:TR?= NWrQcZFNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkiyO|Q3PzVpPkK4Nlc1Pjd3PD;hQi=>

... 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