Ibrutinib (PCI-32765)

For research use only.

Catalog No.S2680

439 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 439 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 MmLiSpVv[3Srb36gZZN{[Xl? NIrscFYzNjVizszN NVy4S3ZRPiCq NITXOVlKdmirYnn0bY9vKG:oIFz5ckBxcG:|cHjvdplt[XSrb36gbY4hcHWvYX6gVoVkOSClZXzsd{BifCB{LkWgeW0hcW6ldXLheIVlKG[xcjC2JIhzeyCkeTDX[ZN1\XKwIHLsc5R1cW6pIH3leIhw\A>? NVLsbZkyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyNlI5PzdpPkK1NlIzQDd5PD;hQi=>
human WSU-NHL cells M1\RS2N6fG:2b4jpZ:Kh[XO|YYm= NYrjXm5IPzJiaB?= NX7GdYFlS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hX1OXLV7IUEBk\WyuczDhd5Nme3OnZDDhd{Boem:5dHigbY5pcWKrdHnvckBi\nSncjC3NkBpenNiYomgR4VtdFSrdHXyMWdtdyCudX3pcoV{[2WwdDDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlA6KM7:TR?= MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDlzNUK5NUc,OjR7MUWyPVE9N2F-
human SU-DHL6 cells M4\3NWN6fG:2b4jpZ:Kh[XO|YYm= MUW3NkBp MXXDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTWU1FUEx4IHPlcIx{KGG|c3Xzd4VlKGG|IHfyc5d1cCCrbnjpZol1cW:wIHHmeIVzKDd{IHjyd{BjgSCFZXzsWIl1\XJvR3zvJIx2dWmwZYPj[Y51KGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwNUig{txONg>? NX35c4ZQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5NVUzQTFpPkK0PVE2OjlzPD;hQi=>
human DOHH2 cells NWW1bo9JS3m2b4TvfIlkyqCjc4PhfS=> MlrSO|IhcA>? NFXNVnBEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBFV0iKMjDj[YxteyCjc4Pld5Nm\CCjczDndo94fGhiaX7obYJqfGmxbjDh[pRmeiB5MjDodpMh[nliQ3XscHRqfGW{LVfsc{BtfW2rbnXzZ4VvfCClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkSxJO69VS5? M1LodVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUG1NlkyLz5{NEmxOVI6OTxxYU6=
Sf9 cells NXOwVIR3TnWwY4Tpc44h[XO|YYm= MXmxJIg> NWLiW3NJUW6qaXLpeIlwdiCxZjDMXW4uSSCneIDy[ZN{\WRiaX6gV4Y6KGOnbHzzJIFnfGW{IE[wJI1qdnNiYomgWHIuTlKHVDDBd5NigSxiSVO1NF0xNjJizszNMi=> M4fLR|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzOUW4OVQ4Lz5{MUm1PFU1PzxxYU6=
human Ramos cells M4Xz[2Z2dmO2aX;uJIF{e2G7 NH\kZ5oyKGh? NXruRnRJUW6qaXLpeIlwdiCxZjDCeIshcW5iaIXtZY4hWmGvb4OgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCSTFOt[4FudWF{IIDoc5NxcG:{eXzheIlwdiCjdDDUfZIyOjF5IHHmeIVzKDFiaIKgZpkhX2W|dHXyckBjdG:2IHHuZYx6e2m|LDDJR|UxRTF2IH7NMi=> MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDlzNUK5NUc,OjR7MUWyPVE9N2F-
human Pfeiffer cells M4\4WWZ2dmO2aX;uJIF{e2G7 MX63NkBp NVXKSHFpS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hWG[naX\m[ZIh[2WubIOgZZN{\XO|ZXSgZZMh\3Kxd4ToJIlvcGmkaYTpc44h[W[2ZYKgO|IhcHK|IHL5JGNmdGyWaYTldk1IdG9ibIXtbY5me2OnboSgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NkBvVS5? M3\GSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUG1NlkyLz5{NEmxOVI6OTxxYU6=
Sf9 cells NGm3[XhHfW6ldHnvckBie3OjeR?= Mn7MNUBp MnvBTY5pcWKrdHnvckBw\iCqdX3hckBnfWyuLXzlcod1cCCEVFug[ZhxemW|c3XkJIlvKFOoOTDj[YxteyC3c3nu[{BHSU1vU4LjeIll\SCyZYD0bYRmKGG|IIP1ZpN1emG2ZTDh[pRmeiB4MDDtbY5{KGK7IGTSMWZTTVRiQYPzZZnwxIxiSVO1NF0xNjVibl2u Ml7nQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF7NUi1OFcoRjJzOUW4OVQ4RC:jPh?=
Sf9 insect cells NHXwSIhHfW6ldHnvckBie3OjeR?= MVG2NEBucW6| Mn62TWM2OCB;IECuNFAxOyEQvF2= M3vpcFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7MUS2NVM3Lz5{OUG0OlE{PjxxYU6=
sf9 cells NH;zW25HfW6ldHnvckBie3OjeR?= M1rpS2lEPTBiPTCwMlAxODNizszN M1[2c|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5OUm0O|M3Lz5{N{m5OFc{PjxxYU6=
Sf9 insect cells NIL6VI5HfW6ldHnvckBie3OjeR?= NH6xOlg3OCCvaX7z MV;JR|UxKD1iMD6wNFA{PCEQvF2= MnezQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd7MUKxO|UoRjJ5OUGyNVc2RC:jPh?=
Sf9 insect cells NHe4W5FHfW6ldHnvckBie3OjeR?= NV7ibFlKPjBibXnudy=> NFzPcmpKSzVyIE2gNE4xODB|NDFOwG0> MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDR|Mkm0Okc,Ojh2M{K5OFY9N2F-
Sf9 insect cells MYjGeY5kfGmxbjDhd5NigQ>? M1TpT|YxKG2rboO= MnrtTWM2OCB;IECuNFAxOzRizszN MkH2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd7NU[wN|coRjJ5OUW2NFM4RC:jPh?=
Sf9 cells NU[5R5ZYTnWwY4Tpc44h[XO|YYm= MlTvOlAhdWmwcx?= NVzlXY81UUN3MDC9JFAvODByNDFOwG0> MlXTQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzByME[xOFMoRjNyMEC2NVQ{RC:jPh?=
Sf9 cells MYTGeY5kfGmxbjDhd5NigQ>? NIKxbYk3OCCvaX7z MorvTWM2OCB;IECuNFAxPSEQvF2= MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTl3OEW0O{c,OjF7NUi1OFc9N2F-
Ramos cells NXfodXFDTnWwY4Tpc44h[XO|YYm= NILXepEyKGh? MoH1TWM2OCB;IECuNFAxPSEQvF2= NYXSN4t4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkiyPFAzPjFpPkK4NlgxOjZzPD;hQi=>
Sf9 cells Mm\pSpVv[3Srb36gZZN{[Xl? MVy2NEBucW6| M2SwdGlEPTBiPTCwMlAxOSEQvF2= NXvJcnZFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CwO|c3ODhpPkOwNFc4PjB6PD;hQi=>
Pfeiffer cells MlvRR5l1d3SxeHnjbZR6KGG|c3H5 MnWyO|IhcA>? NVmycpFkT0l3MDC9JFAvODB{IN88US=> NYLMbHZJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5NVUzQTFpPkK0PVE2OjlzPD;hQi=>
B cells M4TneWZ2dmO2aX;uJIF{e2G7 NFfCdXQyKGh? MUnJR|UxKD1iMD6wNFQ3KM7:TR?= MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODJ7MEm4PEc,OzB{OUC5PFg9N2F-
Sf9 insect cells MWHGeY5kfGmxbjDhd5NigQ>? MWGyJJRwKDZyIH3pcpM> NVnpb4lxU2liPTCwMlAxPDhizszN M{m1b|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6M{G1OVk4Lz5{OEOxOVU6PzxxYU6=
Ramos cells M4frXmZ2dmO2aX;uJIF{e2G7 NFXaOnUyKGh? NVPJTFNrUUN3MDC9JFAvODB5NTFOwG0> NEHGSmk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEmxOVI6OSd-MkS5NVUzQTF:L3G+
Sf9 insect cells MUTGeY5kfGmxbjDhd5NigQ>? Mk\UOlAhdWmwcx?= MlfTTWM2OCB;IECuNFA5KM7:TR?= M4DYdFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6M{G1OVk4Lz5{OEOxOVU6PzxxYU6=
TMD8 cells NFzSWmtCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= NWXMXXlNPzJiaB?= NYrVfHNKUUN3MDC9JFAvODFizszN NGLkeJo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUexOVAzOyd-Mkm3NVUxOjN:L3G+
CD19+ B cells MkW2SpVv[3Srb36gZZN{[Xl? NYXNZYVuOSCq M1[5[2lEPTBiPTCwMlAyOiEQvF2= NFTD[2o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUS1O|k5Oid-Mkm0OVc6QDJ:L3G+
Sf9 insect cells MoHPSpVv[3Srb36gZZN{[Xl? NIjvT5M3OCCvaX7z NH20fYhKSzVyIE2gNE4xOTJizszN NInjNFU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEOxOVU6Pyd-MkizNVU2QTd:L3G+
Ramos cells M3O5bWZ2dmO2aX;uJIF{e2G7 NV[ydXRjOSCq NILPWGlKSzVyIE2gNE4xOTRizszN M{LBT|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUG1NlkyLz5{NEmxOVI6OTxxYU6=
Sf9 insect cells MYTGeY5kfGmxbjDhd5NigQ>? Mk\oNUBp MWnJR|UxKD1iMD6wNVQ1KM7:TR?= Mmm5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl5MUWwNlMoRjJ7N{G1NFI{RC:jPh?=
Sf9 insect cells NFHHWmRHfW6ldHnvckBie3OjeR?= MYC2NEBucW6| NF;ES21KSzVyIE2gNE4xOTZzIN88US=> M4PT[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7MUS2NVM3Lz5{OUG0OlE{PjxxYU6=
HCC827 cells Mny4RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZZN{[Xl? NH;uV4c4OiCq M4LIeGlEPTBiPTCwMlA{QSEQvF2= MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDd|NEW4NUc,Ojh5M{S1PFE9N2F-
PC9 cells M3K2TGZ2dmO2aX;uJIF{e2G7 MV63NkBp M{HM[2dKPTBiPTCwMlA2KM7:TR?= MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDJ6MkGyNkc,Ojh{OEKxNlI9N2F-
Sf9 cells NUTRRm11TnWwY4Tpc44h[XO|YYm= M1fz[lYxKG2rboO= MlHiTWM2OCB;IECuNUDPxE1? NHfoNpg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MECwOlE1Oyd-M{CwNFYyPDN:L3G+
H3255 cells M3TSS2Z2dmO2aX;uJIF{e2G7 MWi3NkBp MYPHTVUxKD1iMD6xNUDPxE1? NXXG[GhiRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkiyPFIyOjJpPkK4NlgzOTJ{PD;hQi=>
BaF3 cells M17tSmZ2dmO2aX;uJIF{e2G7 NWfZUVRZPzJiaB?= MV3HTVUxKD1iMD6xNkDPxE1? NVrLZ2pORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[2N|A2PTNpPkK2OlMxPTV|PD;hQi=>
BAF3 cells MmfGRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZZN{[Xl? M{DKclczKGh? MlHYS2k2OCB;IECuNVIh|ryP MnzjQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh7NU[5NlMoRjJ6OUW2PVI{RC:jPh?=
Sf9 insect cells NXi1SnhTTnWwY4Tpc44h[XO|YYm= M{K0dlYxKG2rboO= MUXJR|UxKD1iMD6xNlMh|ryP MoDNQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh|MUW1PVcoRjJ6M{G1OVk4RC:jPh?=
Sf9 insect cells NH7DeW1HfW6ldHnvckBie3OjeR?= MX:2NEBucW6| NIjxXHhKSzVyIE2gNE4yPDZizszN NYTOWIp3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkizNVU2QTdpPkK4N|E2PTl5PD;hQi=>
BAF3 cells NWPmbpVCTnWwY4Tpc44h[XO|YYm= MXu3NkBp MV\HTVUxKD1iMD6xOkDPxE1? NGrNbIQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEK4NlEzOid-MkiyPFIyOjJ:L3G+
Sf9 cells M1nvPWZ2dmO2aX;uJIF{e2G7 M1PQeFYxKG2rboO= MlPNTWM2OCB;IECuNkDPxE1? MlvaQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF7NUi1OFcoRjJzOUW4OVQ4RC:jPh?=
MV411 cells MVzHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M2rwW2dKPTBiPTCwMlI2KM7:TR?= NYXQOWZMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkizNVU2QTdpPkK4N|E2PTl5PD;hQi=>
MV4-11 cells NF\LSFdCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= MXe3NkBp MYPHTVUxKD1iMD6zN{DPxE1? NX3WepFGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[2N|A2PTNpPkK2OlMxPTV|PD;hQi=>
MV4-11 cells NH:zPIdCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= NHTDUZk4OiCq NHXnT2hIUTVyIE2gNE4{OyEQvF2= MoTvQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh7NU[5NlMoRjJ6OUW2PVI{RC:jPh?=
DOHH2 cells NF;ZdpNEgXSxdH;4bYNqfHliYYPzZZk> NIHLSnE4OiCq NUXhVGZFT0l3MDC9JFAvPDFizszN NF;teFc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEmxOVI6OSd-MkS5NVUzQTF:L3G+
HCC827 cells MWLBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? MV[5OkBp MonrSWM2OCB;IECuOFUh|ryP M3nve|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6OEWzOVc2Lz5{OEi1N|U4PTxxYU6=
SU-DHL6 cells Mnu4R5l1d3SxeHnjbZR6KGG|c3H5 MU[3NkBp MoPZS2k2OCB;IECuOVgh|ryP Mn61QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7MUWyPVEoRjJ2OUG1NlkyRC:jPh?=
M07e cells M3HBOWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MoPFS2k2OCB;IECuOVkh|ryP NIPHNo49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEOxOVU6Pyd-MkizNVU2QTd:L3G+
NCI-H1975 cells M2LiUWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 NVL1VmxPQTZiaB?= NHfGSVRGSzVyIE2gNE43PCEQvF2= M3PpdFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6OEWzOVc2Lz5{OEi1N|U4PTxxYU6=
SU-DHL-2 cells NH\yToVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MmXZS2k2OCB;IECuOlQh|ryP NX;sNolmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkizNVU2QTdpPkK4N|E2PTl5PD;hQi=>
HEK293T cells MnWySpVv[3Srb36gZZN{[Xl? M1m4VVEhcA>? NHexeYNKSzVyIE2gNE46KM7:TR?= M{jHO|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MkiwNlYyLz5{OEK4NFI3OTxxYU6=
Ramos cells M3PteWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 NXXySW1UPzJiaB?= MlvyTWM2OCB;IECuPVIh|ryP NVnvXWdLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm3NVUxOjNpPkK5O|E2ODJ|PD;hQi=>
BA/F3 cells MV7BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? M1v3ZVczKGh? MkXuTWM2OCB;IEGg{txO NGTm[Xo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkK1PFUzOSd-Mk[yOVg2OjF:L3G+
WSU-NHL cells NHS0dlhEgXSxdH;4bYNqfHliYYPzZZk> MXO3NkBp MoXES2k2OCB;IEGuNFkh|ryP M{S2blxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUG1NlkyLz5{NEmxOVI6OTxxYU6=
NCI-H1975 cells M13iZ2Z2dmO2aX;uJIF{e2G7 NF[4T4w4OiCq MojES2k2OCB;IEGuNkDPxE1? MmW2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh{OEKxNlIoRjJ6MkiyNVIzRC:jPh?=
NCI-H1975 cells NYm0R|hvSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[XO|YYm= NUH2RWZuPzJiaB?= MX3JR|UxKD1iMT6yO{DPxE1? M{PCcVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6N{O0OVgyLz5{OEezOFU5OTxxYU6=
Raji cells MlTkRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZZN{[Xl? MXS0PEBp M1;GPGlEPTBiPTCxMlQ6KM7:TR?= NXjkOIpJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm1OlczQTVpPkK5OVY4Ojl3PD;hQi=>
Pfeiffer cells NH7rVG5Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= MWHHTVUxKD1iMT62JO69VQ>? MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDNzNUW5O{c,Ojh|MUW1PVc9N2F-
A431 cells NETxdWtCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= MkX5PVYhcA>? NWKxeox{TUN3MDC9JFIvOzhizszN MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDh3M{W3OUc,Ojh6NUO1O|U9N2F-
BAF3 cells NEDI[YdCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= NYfuVnV[PzJiaB?= NVHtZotlT0l3MDC9JFIvPSEQvF2= MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDl3NkmyN{c,Ojh7NU[5NlM9N2F-
U937 cells MW\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NVH4[Y5wT0l3MDC9JFIvQSEQvF2= MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDNzNUW5O{c,Ojh|MUW1PVc9N2F-
NB4 cells NVizVWV{T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NGXzXIxIUTVyIE2gN{DPxE1? MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDNzNUW5O{c,Ojh|MUW1PVc9N2F-
Ramos cells M3;Ncmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MkT0S2k2OCB;IEOuOEDPxE1? NVLUcZZoRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkizNVU2QTdpPkK4N|E2PTl5PD;hQi=>
SKM1 cells NX30TVhtT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Mmr3S2k2OCB;IEOuOkDPxE1? NVnse5NpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkizNVU2QTdpPkK4N|E2PTl5PD;hQi=>
U2932 cells NFHkXYFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= Mn3wS2k2OCB;IESuOEDPxE1? M2m3WFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6M{G1OVk4Lz5{OEOxOVU6PzxxYU6=
Ramos cells MW\BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? Mny1O|IhcA>? NGHZOVRKSzVyIE2gOU4yPCEQvF2= NVHiblN6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CwNFYyPDNpPkOwNFA3OTR|PD;hQi=>
Ramos cells MXfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? NH3YTno1QCCq MkfxTWM2OCB;IEWuNVQh|ryP MlT1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd7NU[wN|coRjJ5OUW2NFM4RC:jPh?=
Ramos cells NVO0clB4SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[XO|YYm= MmfrOFghcA>? NEi5bZhKSzVyIE2gOU45QCEQvF2= NYHYVlBVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki0N|I6PDZpPkK4OFMzQTR4PD;hQi=>
Ramos cells NIXpeXZCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= M2XTZVczKGh? MlTBTWM2OCB;IE[uOlIh|ryP NGHjO2E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUG0OlE{Pid-MkmxOFYyOzZ:L3G+
K562 cells NVrQO3hoSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[XO|YYm= MmnrOFghcA>? M4TyVWlEPTBiPTC3MlUh|ryP NEDSO|I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEC3O|YxQCd-M{CwO|c3ODh:L3G+
HL60 cells M3Xze2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 MlzyOFghcA>? NVTpZpRPUUN3MDC9JFgh|ryP MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODB5N{[wPEc,OzByN{e2NFg9N2F-
Ramos cells M{XaNmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 M3LUTFQ5KGh? MXjJR|UxKD1iOD6xNUDPxE1? M4DqSVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5OUm0O|M3Lz5{N{m5OFc{PjxxYU6=
Ramos cells NYi2VGh1SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[XO|YYm= M4LGRVQ5KGh? M1LHcWlEPTBiPTC4MlI3KM7:TR?= M3L6OVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NU[3Nlk2Lz5{OUW2O|I6PTxxYU6=
OCI-AML3 cells MXTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MkP6S2k2OCB;IEmuNkDPxE1? NFnNR5c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEOxOVU6Pyd-MkizNVU2QTd:L3G+
BAF3 cells NVSxWpJSS3m2b4TvfIlkcXS7IHHzd4F6 Mn7sO|IhcA>? NXr5RVRRT0l3MDC9JFExKM7:TR?= MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjZ|MEW1N{c,OjZ4M{C1OVM9N2F-
BAF3 cells MVXBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? NH3ZVJU4OiCq MmPKS2k2OCB;IEGwJO69VQ>? NVu4cFg{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki5OVY6OjNpPkK4PVU3QTJ|PD;hQi=>
BAF3 cells NHLDU3RIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MXq3NkBp MlPrS2k2OCB;IEGwJO69VQ>? M1;ydFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MkiyNVIzLz5{OEK4NlEzOjxxYU6=
NAMALWA cells NV\OUnBJSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[XO|YYm= Ml24O|IhcA>? NIS2V2RKSzVyIE2gNVAvPDVizszN M4LRRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7MUS2NVM3Lz5{OUG0OlE{PjxxYU6=
Ramos cells NFzp[ZZCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= M3fyVVQ5KGh? NXj4UHFPUUN3MDC9JFEzNjZizszN MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzlzMkG3OUc,Ojd7MUKxO|U9N2F-
Raji cells MVzBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? NFXPcGw1QCCq NGTq[pVKSzVyIE2gNVQvOiEQvF2= MnTrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzByN{e2NFgoRjNyMEe3OlA5RC:jPh?=
Raji cells MmfWRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZZN{[Xl? M{WxbFQ5KGh? M1LURmlEPTBiPTCxOU4zKM7:TR?= MljFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd7OUS3N|YoRjJ5OUm0O|M3RC:jPh?=
MIAPaCa2 cells MWfDfZRwfG:6aXPpeJkh[XO|YYm= M36xO|Mh\GG7cx?= MljpTWM2OCB;IEG2MlYh|ryP NVT4[ZNMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkewO|czOjhpPkK3NFc4OjJ6PD;hQi=>
HeLa cells MnfYR5l1d3SxeHnjbZR6KGG|c3H5 MlnNN{Bl[Xm| MYnJR|UxKD1iMU[uPEDPxE1? MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzB5N{KyPEc,OjdyN{eyNlg9N2F-
Raji cells MUfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? MV:0PEBp MYHJR|UxKD1iMUmuN{DPxE1? MoLwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd7MUKxO|UoRjJ5OUGyNVc2RC:jPh?=
Raji cells NEWw[lZCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= NIfZ[I01QCCq MnPsTWM2OCB;IEG5MlMh|ryP M3\ZV|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6NEOyPVQ3Lz5{OESzNlk1PjxxYU6=
Raji cells M2LqcGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 NVjBbI5IPzJiaB?= MU\JR|UxKD1iMUmuOUDPxE1? MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODByNkG0N{c,OzByME[xOFM9N2F-
Raji cells MYLBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? MYK0PEBp M2G3dGlEPTBiPTCxPU42KM7:TR?= M1zvbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5OUW2NFM4Lz5{N{m1OlA{PzxxYU6=
NAMALWA cells MXHBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? NV;TcYxuPzJiaB?= NXjZbpV6UUN3MDC9JFE6NjZizszN M4HHTlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMEC2NVQ{Lz5|MECwOlE1OzxxYU6=
A2780 cells NIDZTVJEgXSxdH;4bYNqfHliYYPzZZk> MlrPN{Bl[Xm| M37YemVEPTBiPTCyNE4yKM7:TR?= NX\FV4J1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkewO|czOjhpPkK3NFc4OjJ6PD;hQi=>
Raji cells MWXBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? MUm3NkBp NUnYPIJOUUN3MDC9JFIxNjh6IN88US=> MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTF2NkGzOkc,OjlzNE[xN|Y9N2F-
A549 cells NXznW3l7SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[XO|YYm= NEexTmk4OiCq MXjJR|UxKD1iMkGuO|kh|ryP NEHYS4Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEezOFU5OSd-Mki3N|Q2QDF:L3G+
SW480 cells MVPDfZRwfG:6aXPpeJkh[XO|YYm= M1PsU|Mh\GG7cx?= MXzJR|UxKD1iMkWuOkDPxE1? MnnlQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdyN{eyNlgoRjJ5MEe3NlI5RC:jPh?=
Ramos cells MXPDfZRwfG:6aXPpeJkh[XO|YYm= M4C1elI1KGh? NFPWdVdKSzVyIE2gNlgvPyEQvF2= NGXoNZc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEK3OFY4PSd-MkiyO|Q3PzV:L3G+

... 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]

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

Solubility (25°C)

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

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 440.5
Formula

C25H24N6O2

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

In vivo Formulation Calculator (Clear solution)

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

Bio Calculators

Molarity Calculator

Molarity Calculator

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

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

  • Mass
    Concentration
    Volume
    Molecular Weight

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

Dilution Calculator

Dilution Calculator

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

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

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

  • C1
    V1
    C2
    V2

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

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

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

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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

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

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

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

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
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
NCT04876092 Not yet recruiting Drug: JNJ-67856633|Drug: Ibrutinib Leukemia Lymphocytic Chronic B-Cell|Lymphoma Non-Hodgkin Janssen Research & Development LLC June 11 2021 Phase 1
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
NCT04560322 Not yet recruiting Drug: Venetoclax|Drug: Obinutuzumab|Drug: Ibrutinib Chronic Lymphocytic Leukemia|Small Lymphocytic Lymphoma Massachusetts General Hospital|Genentech Inc. September 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