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 476 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 MmnLSpVv[3Srb36gZZN{[Xl? MVWyMlUh|ryP NXe2flhEPiCq MWHJcohq[mm2aX;uJI9nKEy7bjDwbI9{eGixconsZZRqd25iaX6gbJVu[W5iUnXjNUBk\WyuczDheEAzNjVidV2gbY5kfWKjdHXkJIZweiB4IHjyd{BjgSCZZYP0[ZJvKGKub4T0bY5oKG2ndHjv[C=> MmjKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{MkK4O|coRjJ3MkKyPFc4RC:jPh?=
human WSU-NHL cells MXLDfZRwfG:6aXRCpIF{e2G7 MWW3NkBp MULDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDXV3UuVkiOIHPlcIx{KGG|c3Xzd4VlKGG|IHfyc5d1cCCrbnjpZol1cW:wIHHmeIVzKDd{IHjyd{BjgSCFZXzsWIl1\XJvR3zvJIx2dWmwZYPj[Y51KGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTFwMEmg{txO NWLVb2FJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5NVUzQTFpPkK0PVE2OjlzPD;hQi=>
human SU-DHL6 cells NWfzd4NRS3m2b4TvfIlkyqCjc4PhfS=> NUTueGh6PzJiaB?= NVz6RXE2S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hW1VvRFjMOkBk\WyuczDhd5Nme3OnZDDhd{Boem:5dHigbY5pcWKrdHnvckBi\nSncjC3NkBpenNiYomgR4VtdFSrdHXyMWdtdyCudX3pcoV{[2WwdDDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlU5KM7:TT6= NFe5NFk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEmxOVI6OSd-MkS5NVUzQTF:L3G+
human DOHH2 cells Ml\xR5l1d3SxeHnjxsBie3OjeR?= MmTCO|IhcA>? MojlR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gSG9JUDJiY3XscJMh[XO|ZYPz[YQh[XNiZ4Lve5RpKGmwaHnibZRqd25iYX\0[ZIhPzJiaILzJIJ6KEOnbHzUbZRmei2JbH:gcJVucW6nc3PlcpQh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC52MTFOwG0v MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDlzNUK5NUc,OjR7MUWyPVE9N2F-
Sf9 cells NFW3dHpHfW6ldHnvckBie3OjeR?= MmXmNUBp M4PkeWlvcGmkaYTpc44hd2ZiTGnOMWEh\XiycnXzd4VlKGmwIGPmPUBk\WyuczDh[pRmeiB4MDDtbY5{KGK7IGTSMWZTTVRiQYPzZZktKEmFNUC9NE4zKM7:TT6= M{TpSFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzOUW4OVQ4Lz5{MUm1PFU1PzxxYU6=
human Ramos cells M4HKbWZ2dmO2aX;uJIF{e2G7 NHTaeI4yKGh? M4juZWlvcGmkaYTpc44hd2ZiQoTrJIlvKGi3bXHuJHJidW:|IHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhWEyFLXfhcY1iOiCyaH;zdIhwenmuYYTpc44h[XRiVInyNVIyPyCjZoTldkAyKGi{IHL5JHdme3Sncn6gZoxwfCCjbnHsfZNqeyxiSVO1NF0yPCCwTT6= NFn0[JM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEmxOVI6OSd-MkS5NVUzQTF:L3G+
human Pfeiffer cells MoDGSpVv[3Srb36gZZN{[Xl? M{HGelczKGh? NVzPbHl2S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hWG[naX\m[ZIh[2WubIOgZZN{\XO|ZXSgZZMh\3Kxd4ToJIlvcGmkaYTpc44h[W[2ZYKgO|IhcHK|IHL5JGNmdGyWaYTldk1IdG9ibIXtbY5me2OnboSgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NkBvVS5? NUHKboliRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5NVUzQTFpPkK0PVE2OjlzPD;hQi=>
Sf9 cells NW[3TYw2TnWwY4Tpc44h[XO|YYm= NV;4SFFKOSCq MUDJcohq[mm2aX;uJI9nKGi3bXHuJIZ2dGxvbHXu[5RpKEKWSzDlfJBz\XO|ZXSgbY4hW2Z7IHPlcIx{KHW|aX7nJGZCVS2VcnP0bYRmKHCncITp[IUh[XNic4Xid5Rz[XSnIHHmeIVzKDZyIH3pcpMh[nliVGKtSnJGXCCDc4Phfg+9lCCLQ{WwQVAvPSCwTT6= NFjz[4I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUm1PFU1Pyd-MkG5OVg2PDd:L3G+
Sf9 insect cells MWLGeY5kfGmxbjDhd5NigQ>? MX22NEBucW6| NIXIfJZKSzVyIE2gNE4xODB|IN88US=> NILwNIw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUG0OlE{Pid-MkmxOFYyOzZ:L3G+
sf9 cells MWrGeY5kfGmxbjDhd5NigQ>? M4ntNWlEPTBiPTCwMlAxODNizszN NGHqc4s9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{m5OFc{Pid-Mke5PVQ4OzZ:L3G+
Sf9 insect cells MYXGeY5kfGmxbjDhd5NigQ>? NXjQT2dtPjBibXnudy=> MV\JR|UxKD1iMD6wNFA{PCEQvF2= MmDrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd7MUKxO|UoRjJ5OUGyNVc2RC:jPh?=
Sf9 insect cells MVHGeY5kfGmxbjDhd5NigQ>? Mo\HOlAhdWmwcx?= NFnpcoxKSzVyIE2gNE4xODB|NDFOwG0> MmXtQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh2M{K5OFYoRjJ6NEOyPVQ3RC:jPh?=
Sf9 insect cells NFPwW|hHfW6ldHnvckBie3OjeR?= MnjDOlAhdWmwcx?= M1PwOWlEPTBiPTCwMlAxODN2IN88US=> NEfkUm49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{m1OlA{Pyd-Mke5OVYxOzd:L3G+
Sf9 cells NXzuTXNoTnWwY4Tpc44h[XO|YYm= NYqwPGI6PjBibXnudy=> NIXMV5VKSzVyIE2gNE4xODB2IN88US=> M3jKR|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMEC2NVQ{Lz5|MECwOlE1OzxxYU6=
Sf9 cells M37vcWZ2dmO2aX;uJIF{e2G7 NF7SfIM3OCCvaX7z NHzvR2ZKSzVyIE2gNE4xODB3IN88US=> NUj6em5WRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG5OVg2PDdpPkKxPVU5PTR5PD;hQi=>
Ramos cells MXHGeY5kfGmxbjDhd5NigQ>? MmX1NUBp MoX2TWM2OCB;IECuNFAxPSEQvF2= MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDJ6MEK2NUc,Ojh{OECyOlE9N2F-
Sf9 cells NXPwcFdOTnWwY4Tpc44h[XO|YYm= M3\aTlYxKG2rboO= M33iTGlEPTBiPTCwMlAxOSEQvF2= Mn\SQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzByN{e2NFgoRjNyMEe3OlA5RC:jPh?=
Pfeiffer cells M3X3R2N6fG:2b4jpZ4l1gSCjc4PhfS=> MlXhO|IhcA>? NVHFXnVtT0l3MDC9JFAvODB{IN88US=> MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDlzNUK5NUc,OjR7MUWyPVE9N2F-
B cells M4\WeWZ2dmO2aX;uJIF{e2G7 NX\JNYk{OSCq M3jzTGlEPTBiPTCwMlAxPDZizszN MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODJ7MEm4PEc,OzB{OUC5PFg9N2F-
Sf9 insect cells M4XadmZ2dmO2aX;uJIF{e2G7 NYTlT5dEOiC2bzC2NEBucW6| MoPtT4khRSByLkCwOFgh|ryP NF;BZYE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEOxOVU6Pyd-MkizNVU2QTd:L3G+
Ramos cells NHXpRYhHfW6ldHnvckBie3OjeR?= MUGxJIg> MVvJR|UxKD1iMD6wNFc2KM7:TR?= MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDlzNUK5NUc,OjR7MUWyPVE9N2F-
Sf9 insect cells MmDOSpVv[3Srb36gZZN{[Xl? MnrFOlAhdWmwcx?= NEDlR5RKSzVyIE2gNE4xODhizszN MnK2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh|MUW1PVcoRjJ6M{G1OVk4RC:jPh?=
TMD8 cells MXfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? NH7TUHc4OiCq MV;JR|UxKD1iMD6wNUDPxE1? NHLXNIw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUexOVAzOyd-Mkm3NVUxOjN:L3G+
CD19+ B cells MlmxSpVv[3Srb36gZZN{[Xl? MXqxJIg> NE\LZ49KSzVyIE2gNE4xOTJizszN MmjFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2NUe5PFIoRjJ7NEW3PVgzRC:jPh?=
Sf9 insect cells NHe5dJVHfW6ldHnvckBie3OjeR?= MW[2NEBucW6| MnK5TWM2OCB;IECuNFEzKM7:TR?= NE\HOm49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEOxOVU6Pyd-MkizNVU2QTd:L3G+
Ramos cells NIH3[XhHfW6ldHnvckBie3OjeR?= M1HZTlEhcA>? NXjXS5dvUUN3MDC9JFAvODF2IN88US=> M4jBelxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUG1NlkyLz5{NEmxOVI6OTxxYU6=
Sf9 insect cells M1TRSGZ2dmO2aX;uJIF{e2G7 MkO4NUBp MV;JR|UxKD1iMD6wNVQ1KM7:TR?= M122NFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7N{G1NFI{Lz5{OUexOVAzOzxxYU6=
Sf9 insect cells NV[xd4Z1TnWwY4Tpc44h[XO|YYm= NHT5cpc3OCCvaX7z MVzJR|UxKD1iMD6wNVYyKM7:TR?= Mom1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjlzNE[xN|YoRjJ7MUS2NVM3RC:jPh?=
HCC827 cells MV7BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? MYi3NkBp M3n5OWlEPTBiPTCwMlA{QSEQvF2= M4rZV|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6N{O0OVgyLz5{OEezOFU5OTxxYU6=
PC9 cells M1PuRmZ2dmO2aX;uJIF{e2G7 NEHTdWk4OiCq MYPHTVUxKD1iMD6wOUDPxE1? Mn\YQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh{OEKxNlIoRjJ6MkiyNVIzRC:jPh?=
Sf9 cells MoW1SpVv[3Srb36gZZN{[Xl? Ml;DOlAhdWmwcx?= MkfnTWM2OCB;IECuNUDPxE1? NHr2bng9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MECwOlE1Oyd-M{CwNFYyPDN:L3G+
H3255 cells NWLqPVQ5TnWwY4Tpc44h[XO|YYm= MV23NkBp MWHHTVUxKD1iMD6xNUDPxE1? Ml\4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh{OEKxNlIoRjJ6MkiyNVIzRC:jPh?=
BaF3 cells NX7yS4M1TnWwY4Tpc44h[XO|YYm= M3TVNFczKGh? NX3xZ2hxT0l3MDC9JFAvOTJizszN M2HqTFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NkOwOVU{Lz5{Nk[zNFU2OzxxYU6=
BAF3 cells NH61V|ZCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= MnTLO|IhcA>? NXf0NYpDT0l3MDC9JFAvOTJizszN MkD5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh7NU[5NlMoRjJ6OUW2PVI{RC:jPh?=
Sf9 insect cells NWO4WVdJTnWwY4Tpc44h[XO|YYm= M4HROlYxKG2rboO= M1XIbGlEPTBiPTCwMlEzOyEQvF2= MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDNzNUW5O{c,Ojh|MUW1PVc9N2F-
Sf9 insect cells MnjmSpVv[3Srb36gZZN{[Xl? NYW2dWdEPjBibXnudy=> M{fXdWlEPTBiPTCwMlE1PiEQvF2= MlnhQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh|MUW1PVcoRjJ6M{G1OVk4RC:jPh?=
BAF3 cells Mom0SpVv[3Srb36gZZN{[Xl? MXy3NkBp MV7HTVUxKD1iMD6xOkDPxE1? NHK1dJY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEK4NlEzOid-MkiyPFIyOjJ:L3G+
Sf9 cells NXPzXVZVTnWwY4Tpc44h[XO|YYm= NX7oemh5PjBibXnudy=> NYrGe|FqUUN3MDC9JFAvOiEQvF2= MkDhQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF7NUi1OFcoRjJzOUW4OVQ4RC:jPh?=
MV411 cells M4\yN2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M1nWTWdKPTBiPTCwMlI2KM7:TR?= NV;yPXJkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkizNVU2QTdpPkK4N|E2PTl5PD;hQi=>
MV4-11 cells NGPEZ4hCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= MoO5O|IhcA>? NXPGTHFlT0l3MDC9JFAvOzNizszN MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjZ|MEW1N{c,OjZ4M{C1OVM9N2F-
MV4-11 cells NFTl[5VCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= NHXJTIQ4OiCq MlnHS2k2OCB;IECuN|Mh|ryP M2L2XlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6OUW2PVI{Lz5{OEm1OlkzOzxxYU6=
DOHH2 cells MlHVR5l1d3SxeHnjbZR6KGG|c3H5 MknYO|IhcA>? MkPHS2k2OCB;IECuOFEh|ryP NUDNZZlGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5NVUzQTFpPkK0PVE2OjlzPD;hQi=>
HCC827 cells Ml7jRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZZN{[Xl? MWW5OkBp MWTFR|UxKD1iMD60OUDPxE1? MW[8ZUB1[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

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

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
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

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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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