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Ibrutinib

(Synonyms: PCI-32765)

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Based on 136 publication(s) in Google Scholar

Ibrutinib (PCI-32765) is a selective, irreversible Btk inhibitor with an IC₅₀ of 0.5 nM.

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Pureté: 99.97%
CAS No.: 936563-96-1
Formule: C₂₅H₂₄N₆O₂
Masse moléculaire:440.50

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* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Ibrutinib Chemical Structure

CAS No.: 936563-96-1

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Publications (136)
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Activité biologique

Description

Ibrutinib (PCI-32765) is a selective, irreversible Btk inhibitor with an IC₅₀ of 0.5 nM^[1].

IC₅₀ & Target

IC50: 0.5 nM (Btk)

Cellular Effect

Cell Line	Type	Value	Description	References
A2780	EC₅₀	20.1 μM Compound: ibrutinib	Cytotoxicity against human A2780 cells assessed as cell growth inhibition after 3 days by presto blue dye based plate reader method Cytotoxicity against human A2780 cells assessed as cell growth inhibition after 3 days by presto blue dye based plate reader method	[PMID: 27077228]
A-431	GI₅₀	>10 μM Compound: 1; PCI-32765	Antiproliferative activity against human A431 cells after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human A431 cells after 72 hrs by CellTiter-Glo assay	[PMID: 28628824]
A-431	EC₅₀	2.38 μM Compound: Ibrutinib	Antiproliferative activity against human A431 cells expressing wild type EGFR incubated for 96 hrs measured on day 5 by CellTiterGlo assay Antiproliferative activity against human A431 cells expressing wild type EGFR incubated for 96 hrs measured on day 5 by CellTiterGlo assay	[PMID: 28853575]
A549	GI₅₀	>10 μM Compound: 1; PCI-32765	Antiproliferative activity against human A549 cells after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human A549 cells after 72 hrs by CellTiter-Glo assay	[PMID: 28628824]
A549	IC₅₀	21.79 μM Compound: Ibrutinib	Antiproliferative activity against human A549 cells harboring wild type EGFR after 72 hrs by MTT assay Antiproliferative activity against human A549 cells harboring wild type EGFR after 72 hrs by MTT assay	[PMID: 28734581]
B cell	IC₅₀	8 nM Compound: 19	Antiproliferative activity against anti-IgM-stimulated human KB cells assessed as cell growth inhibition pretreated for 30 mins followed by anti-IgM stimulation for 72 hrs by celltiter-glo reagent based assay Antiproliferative activity against anti-IgM-stimulated human KB cells assessed as cell growth inhibition pretreated for 30 mins followed by anti-IgM stimulation for 72 hrs by celltiter-glo reagent based assay	[PMID: 33540357]
BaF3	IC₅₀	>1 μM Compound: 7	Antiproliferative activity against mouse BA/F3 cells expressing TEL-JAK3 after 72 hrs by cell titer glo assay Antiproliferative activity against mouse BA/F3 cells expressing TEL-JAK3 after 72 hrs by cell titer glo assay	[PMID: 26258521]
BaF3	GI₅₀	>10 μM Compound: 1; PCI-32765	Cytotoxicity against mouse BAF3 cells assessed as cell proliferation after 72 hrs by CelltiterGlo assay Cytotoxicity against mouse BAF3 cells assessed as cell proliferation after 72 hrs by CelltiterGlo assay	[PMID: 26630553]
BaF3	GI₅₀	0.12 μM Compound: 1; PCI-32765	Inhibition of FLT3 ITD mutant (unknown origin) expressed in BaF3 cells assessed as inhibition of cell proliferation after 72 hrs by CelltiterGlo assay Inhibition of FLT3 ITD mutant (unknown origin) expressed in BaF3 cells assessed as inhibition of cell proliferation after 72 hrs by CelltiterGlo assay	[PMID: 26630553]
BaF3	GI₅₀	>10 μM Compound: 9; PCI-32765	Growth inhibition of mouse BAF3 cells after 72 hrs by CellTiter-Glo assay Growth inhibition of mouse BAF3 cells after 72 hrs by CellTiter-Glo assay	[PMID: 28282122]
BaF3	GI₅₀	>10 μM Compound: 1; PCI-32765	Antiproliferative activity against mouse BA/F3 cells after 72 hrs by CellTiter-Glo assay Antiproliferative activity against mouse BA/F3 cells after 72 hrs by CellTiter-Glo assay	[PMID: 28628824]
BaF3	GI₅₀	>10 μM Compound: 9	Antiproliferative activity against mouse BAF3 cells after 72 hrs by CellTiter-Glo assay Antiproliferative activity against mouse BAF3 cells after 72 hrs by CellTiter-Glo assay	[PMID: 28956923]
BaF3	GI₅₀	0.12 μM Compound: 9	Antiproliferative activity against mouse BAF3 cells harboring FLT3-ITD mutation after 72 hrs by CellTiter-Glo assay Antiproliferative activity against mouse BAF3 cells harboring FLT3-ITD mutation after 72 hrs by CellTiter-Glo assay	[PMID: 28956923]
BaF3	GI₅₀	2.5 μM Compound: 9	Antiproliferative activity against mouse BAF3 cells harboring FLT3-ITD-F691L mutation after 72 hrs by CellTiter-Glo assay Antiproliferative activity against mouse BAF3 cells harboring FLT3-ITD-F691L mutation after 72 hrs by CellTiter-Glo assay	[PMID: 28956923]
BaF3	IC₅₀	1546 nM Compound: PCI-32765	Antiproliferative activity against mouse BaF3 cells expressing BTK C481S mutant assessed as inhibition of cell growth measured after 3 days by CCK-8 assay Antiproliferative activity against mouse BaF3 cells expressing BTK C481S mutant assessed as inhibition of cell growth measured after 3 days by CCK-8 assay	[PMID: 37119666]
BaF3	IC₅₀	1425 nM Compound: Ibrutinib	Antiproliferative activity against mouse BaF3 cells expressing JAK3 mutant assessed as inhibition of cell growth incubated for 72 hrs by Cell Titer-Glo assay Antiproliferative activity against mouse BaF3 cells expressing JAK3 mutant assessed as inhibition of cell growth incubated for 72 hrs by Cell Titer-Glo assay	[PMID: 37944414]
CMK	GI₅₀	>10 μM Compound: 1; PCI-32765	Antiproliferative activity against human CMK cells after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human CMK cells after 72 hrs by CellTiter-Glo assay	[PMID: 28628824]
Daudi	IC₅₀	3.92 μM Compound: 1	Antiproliferative activity against human Daudi cells Antiproliferative activity against human Daudi cells	[PMID: 30875504]
Daudi	IC₅₀	655.6 nM Compound: Ibrutinib	Antiproliferative activity against human Daudi cells assessed as inhibition of cell growth incubated for 72 hrs by Cell Titer-Glo assay Antiproliferative activity against human Daudi cells assessed as inhibition of cell growth incubated for 72 hrs by Cell Titer-Glo assay	[PMID: 37944414]
DOHH-2	GI₅₀	0.41 μM Compound: Ibrutinib	Cytotoxicity against human DOHH2 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo luminescent cell viability assay Cytotoxicity against human DOHH2 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo luminescent cell viability assay	[PMID: 24915291]
DOHH-2	IC₅₀	0.0334 μM Compound: Ibrutinib	Antiproliferative activity against human DOHH2 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay Antiproliferative activity against human DOHH2 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay	[PMID: 30522954]
DOHH-2	IC₅₀	0.023 μM Compound: Ibrutinib	Cytotoxicity against human DOHH-2 cells expressing BTK and PI3kdelta assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Cytotoxicity against human DOHH-2 cells expressing BTK and PI3kdelta assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 35247756]
DOHH-2	IC₅₀	0.5062 μM Compound: Ibrutinib	Antiproliferative activity against human DOHH-2 cells incubated for 72 hrs by CellTiter-Glo assay Antiproliferative activity against human DOHH-2 cells incubated for 72 hrs by CellTiter-Glo assay	[PMID: 35939993]
DU-145	GI₅₀	>10 μM Compound: 1; PCI-32765	Antiproliferative activity against human DU145 cells after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human DU145 cells after 72 hrs by CellTiter-Glo assay	[PMID: 28628824]
DU-145	CC₅₀	>20 μM Compound: 35; PCI-32765	Cytotoxicity against human DU-145 cells Cytotoxicity against human DU-145 cells	[PMID: 33539089]
DU-145	IC₅₀	2 μM Compound: Ibrutinib	Antiproliferative activity against human DU-145 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay Antiproliferative activity against human DU-145 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay	[PMID: 34237622]
Granta-519	IC₅₀	9.7 μM Compound: IBN	Antiproliferative activity against human GRANTA-519 cells assessed as reduction in viability after 72 hrs by CellTiter-Glo luminescent assay Antiproliferative activity against human GRANTA-519 cells assessed as reduction in viability after 72 hrs by CellTiter-Glo luminescent assay	[PMID: 31229421]
HBL1	GI₅₀	700 nM Compound: Ibrutinib	Antiproliferative activity against human HBL1 cells expressing BTK C481S mutant assessed as growth inhibition Antiproliferative activity against human HBL1 cells expressing BTK C481S mutant assessed as growth inhibition	[PMID: 32698111]
HCC 2998	IC₅₀	15.85 μM Compound: Ibrutinib	Antiproliferative activity against human HCC 2998 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay Antiproliferative activity against human HCC 2998 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay	[PMID: 34237622]
HCC827	IC₅₀	0.039 μM Compound: Ibrutinib	Antiproliferative activity against human HCC827 cells harboring EGFR Del19 mutant after 72 hrs by MTT assay Antiproliferative activity against human HCC827 cells harboring EGFR Del19 mutant after 72 hrs by MTT assay	[PMID: 28734581]
HCC827	EC₅₀	0.45 μM Compound: Ibrutinib	Antiproliferative activity against human HCC827 cells harboring EGFR-delE746_A750 mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay Antiproliferative activity against human HCC827 cells harboring EGFR-delE746_A750 mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay	[PMID: 28853575]
HCT-116	GI₅₀	>10 μM Compound: 1; PCI-32765	Antiproliferative activity against human HCT116 cells after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human HCT116 cells after 72 hrs by CellTiter-Glo assay	[PMID: 28628824]
HEK293	IC₅₀	19.3 μM Compound: Ibrutinib	Cytotoxicity against human HEK293 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human HEK293 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 29324347]
HEK293	IC₅₀	46.7 nM Compound: 1a	Inhibition of TEC phosphorylation in HEK293 cells peincubated for 3 hrs followed by pervanadate stimulation and measured after 20 mins by MSD assay Inhibition of TEC phosphorylation in HEK293 cells peincubated for 3 hrs followed by pervanadate stimulation and measured after 20 mins by MSD assay	[PMID: 31381333]
HEK293	IC₅₀	7.9 μM Compound: ibrutinib	Inhibition of the Organic Cation Transporter 3 (OCT3, SLC22A3) as assessed by a phenotypic impedance-based assay detecting changes in cell morphology by MPP+ uptake in HEK-293 JumpIN-SLC22A3 cells Inhibition of the Organic Cation Transporter 3 (OCT3, SLC22A3) as assessed by a phenotypic impedance-based assay detecting changes in cell morphology by MPP+ uptake in HEK-293 JumpIN-SLC22A3 cells	[PMID: 35163125]
HEK293	IC₅₀	7.9 μM Compound: ibrutinib	Inhibition of the Organic Cation Transporter 3 (OCT3, SLC22A3) as assessed by a phenotypic impedance-based assay detecting changes in cell morphology by MPP+ uptake in HEK-293 JumpIN-SLC22A3 cells (PubChem AID: 1745861) Inhibition of the Organic Cation Transporter 3 (OCT3, SLC22A3) as assessed by a phenotypic impedance-based assay detecting changes in cell morphology by MPP+ uptake in HEK-293 JumpIN-SLC22A3 cells (PubChem AID: 1745861)	[PMID: 35163125]
HEK-293T	IC₅₀	0.9 μM Compound: Ibrutinib	Inhibition of PF-06658607 binding to recombinant C-terminal FLAG-tagged FAM213A (unknown origin) expressed in HEK293T cells after 1 hr by gel-based ABPP assay Inhibition of PF-06658607 binding to recombinant C-terminal FLAG-tagged FAM213A (unknown origin) expressed in HEK293T cells after 1 hr by gel-based ABPP assay	[PMID: 28280261]
HEL	GI₅₀	4 μM Compound: 1; PCI-32765	Antiproliferative activity against human HEL cells after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human HEL cells after 72 hrs by CellTiter-Glo assay	[PMID: 28628824]
HEL	IC₅₀	>20 μM Compound: Ibrutinib	Antiproliferative activity against human HEL cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human HEL cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 31843459]
HeLa	IC₅₀	16.8 μM Compound: ibrutinib	Cytotoxicity against human HeLa cells expressing GFP assessed as cell growth inhibition after 3 days by presto blue dye based plate reader method Cytotoxicity against human HeLa cells expressing GFP assessed as cell growth inhibition after 3 days by presto blue dye based plate reader method	[PMID: 27077228]
HeLa	GI₅₀	>10 μM Compound: 1; PCI-32765	Antiproliferative activity against human HeLa cells after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human HeLa cells after 72 hrs by CellTiter-Glo assay	[PMID: 28628824]
HL-60	GI₅₀	3.5 μM Compound: 1; PCI-32765	Antiproliferative activity against human HL60 cells after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human HL60 cells after 72 hrs by CellTiter-Glo assay	[PMID: 28628824]
HL-60	IC₅₀	8 μM Compound: Ibrutinib	Antiproliferative activity against human HL60 cells after 48 hrs by MTT assay Antiproliferative activity against human HL60 cells after 48 hrs by MTT assay	[PMID: 30077608]
HL-60	IC₅₀	3.57 μM Compound: Ibrutinib	Antiproliferative activity against human HL60 cells after 48 hrs by MTT assay Antiproliferative activity against human HL60 cells after 48 hrs by MTT assay	[PMID: 30881616]
HL-60(TB)	IC₅₀	19.95 μM Compound: Ibrutinib	Antiproliferative activity against human HL-60(TB) cells assessed as cell growth inhibition measured after 48 hrs by SRB assay Antiproliferative activity against human HL-60(TB) cells assessed as cell growth inhibition measured after 48 hrs by SRB assay	[PMID: 34237622]
HT	GI₅₀	15.9 μM Compound: Ibrutinib	Antiproliferative activity against human HT cells measured after 72 hrs by calcein AM dye-based fluorescence assay Antiproliferative activity against human HT cells measured after 72 hrs by calcein AM dye-based fluorescence assay	[PMID: 30943029]
JeKo-1	IC₅₀	1.5 μM Compound: IBN	Antiproliferative activity against human JeKo1 cells assessed as inhibition of cell proliferation incubated for 72 hrs by Cell-titer-Glo luminescent cell viability assay Antiproliferative activity against human JeKo1 cells assessed as inhibition of cell proliferation incubated for 72 hrs by Cell-titer-Glo luminescent cell viability assay	[PMID: 30857748]
JeKo-1	IC₅₀	1.05 μM Compound: 1	Antiproliferative activity against human JeKo1 cells Antiproliferative activity against human JeKo1 cells	[PMID: 30875504]
JeKo-1	IC₅₀	20 μM Compound: IBN	Antiproliferative activity against human resistant Jeko cells assessed as reduction in viability after 72 hrs by CellTiter-Glo luminescent assay Antiproliferative activity against human resistant Jeko cells assessed as reduction in viability after 72 hrs by CellTiter-Glo luminescent assay	[PMID: 31229421]
JeKo-1	IC₅₀	3 μM Compound: Ibrutinib	Antiproliferative activity against human JeKo1 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human JeKo1 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 31843459]
JeKo-1	IC₅₀	207.47 nM Compound: Ibrutinib	Antiproliferative activity against human JeKo-1 cells assessed as inhibition of cell growth incubated for 3 to 7 days by MTS assay Antiproliferative activity against human JeKo-1 cells assessed as inhibition of cell growth incubated for 3 to 7 days by MTS assay	[PMID: 35671249]
JeKo-1	IC₅₀	330.2 nM Compound: Ibrutinib	Antiproliferative activity against CRBN knockout human JeKo-1 cells assessed as inhibition of cell growth incubated for 3 to 7 days by MTS assay Antiproliferative activity against CRBN knockout human JeKo-1 cells assessed as inhibition of cell growth incubated for 3 to 7 days by MTS assay	[PMID: 35671249]
JeKo-1	IC₅₀	1.1 μM Compound: 24	Antiproliferative activity against human JeKo-1 cells assessed as reduction cell viability measured after 24 hrs by Cell Titer-Glo Luminescent Cell Viability Assay Antiproliferative activity against human JeKo-1 cells assessed as reduction cell viability measured after 24 hrs by Cell Titer-Glo Luminescent Cell Viability Assay	[PMID: 36324498]
JeKo-1	IC₅₀	1680 nM Compound: 1; IBN	Antiproliferative activity against human JeKo-1 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against human JeKo-1 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 36399923]
JeKo-1	IC₅₀	79.8 nM Compound: PCI-32765	Antiproliferative activity against human JeKo-1 cells assessed as inhibition of cell growth measured after 3 days by CCK-8 assay Antiproliferative activity against human JeKo-1 cells assessed as inhibition of cell growth measured after 3 days by CCK-8 assay	[PMID: 37119666]
Jurkat	IC₅₀	76.9 nM Compound: 1a	Inhibition of ITK in human Jurkat cells assessed as reduction in PLCgamma1 phosphorylation at Y783 residues preincubated for 2 hrs followed by H2O2 addition and measured after 10 mins by Western blot analysis Inhibition of ITK in human Jurkat cells assessed as reduction in PLCgamma1 phosphorylation at Y783 residues preincubated for 2 hrs followed by H2O2 addition and measured after 10 mins by Western blot analysis	[PMID: 31381333]
JVM-2	GI₅₀	>10 μM Compound: 1; PCI-32765	Antiproliferative activity against human JVM2 cells after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human JVM2 cells after 72 hrs by CellTiter-Glo assay	[PMID: 28628824]
K562	GI₅₀	>10 μM Compound: 1; PCI-32765	Antiproliferative activity against human K562 cells after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human K562 cells after 72 hrs by CellTiter-Glo assay	[PMID: 28628824]
K562	IC₅₀	7.5 μM Compound: Ibrutinib	Antiproliferative activity against human K562 cells after 48 hrs by MTT assay Antiproliferative activity against human K562 cells after 48 hrs by MTT assay	[PMID: 30077608]
K562	IC₅₀	5566 nM Compound: 1; IBN	Antiproliferative activity against human K562 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against human K562 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 36399923]
L02	IC₅₀	17.4 μM Compound: Ibrutinib	Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 29324347]
LNCaP C4-2	GI₅₀	>10 μM Compound: 1; PCI-32765	Antiproliferative activity against human C4-2 cells after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human C4-2 cells after 72 hrs by CellTiter-Glo assay	[PMID: 28628824]
Maver1	IC₅₀	10.4 μM Compound: IBN	Antiproliferative activity against human Maver1 cells assessed as inhibition of cell proliferation incubated for 72 hrs by Cell-titer-Glo luminescent cell viability assay Antiproliferative activity against human Maver1 cells assessed as inhibition of cell proliferation incubated for 72 hrs by Cell-titer-Glo luminescent cell viability assay	[PMID: 30857748]
Maver1	IC₅₀	14.4 μM Compound: IBN	Antiproliferative activity against human Maver1 cells assessed as reduction in viability after 72 hrs by CellTiter-Glo luminescent assay Antiproliferative activity against human Maver1 cells assessed as reduction in viability after 72 hrs by CellTiter-Glo luminescent assay	[PMID: 31229421]
Maver1	IC₅₀	7.8 μM Compound: 24	Antiproliferative activity against human MAVER-1 cells assessed as reduction cell viability measured after 24 hrs by Cell Titer-Glo Luminescent Cell Viability Assay Antiproliferative activity against human MAVER-1 cells assessed as reduction cell viability measured after 24 hrs by Cell Titer-Glo Luminescent Cell Viability Assay	[PMID: 36324498]
MDA-MB-468	IC₅₀	0.03 μM Compound: Ibrutinib	Antiproliferative activity against human MDA-MB-468 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay Antiproliferative activity against human MDA-MB-468 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay	[PMID: 34237622]
MIA PaCa-2	IC₅₀	16.6 μM Compound: ibrutinib	Cytotoxicity against human MIAPaCa2 cells assessed as cell growth inhibition after 3 days by presto blue dye based plate reader method Cytotoxicity against human MIAPaCa2 cells assessed as cell growth inhibition after 3 days by presto blue dye based plate reader method	[PMID: 27077228]
MM1.S	IC₅₀	>20000 nM Compound: Ibrutinib	Antiproliferative activity against human MM1.S cells assessed as inhibition of cell growth incubated for 3 to 7 days by MTS assay Antiproliferative activity against human MM1.S cells assessed as inhibition of cell growth incubated for 3 to 7 days by MTS assay	[PMID: 35671249]
MOLM-13	GI₅₀	1.3 μM Compound: 1; PCI-32765	Antiproliferative activity against human MOLM13 cells after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human MOLM13 cells after 72 hrs by CellTiter-Glo assay	[PMID: 28628824]
MOLM-14	GI₅₀	1.8 μM Compound: 1; PCI-32765	Antiproliferative activity against human MOLM14 cells after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human MOLM14 cells after 72 hrs by CellTiter-Glo assay	[PMID: 28628824]
MOLT-4	IC₅₀	3.98 μM Compound: Ibrutinib	Antiproliferative activity against human MOLT-4 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay Antiproliferative activity against human MOLT-4 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay	[PMID: 34237622]
MOLT-4	IC₅₀	3519 nM Compound: 1; IBN	Antiproliferative activity against human MOLT-4 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against human MOLT-4 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 36399923]
MV4-11	GI₅₀	0.33 μM Compound: 1; PCI-32765	Antiproliferative activity against human MV4-11 cells after 72 hrs by CelltiterGlo assay Antiproliferative activity against human MV4-11 cells after 72 hrs by CelltiterGlo assay	[PMID: 26630553]
MV4-11	GI₅₀	0.25 μM Compound: 1; PCI-32765	Growth inhibition of human MV411 cells Growth inhibition of human MV411 cells	[PMID: 28315597]
MV4-11	GI₅₀	0.33 μM Compound: 9	Antiproliferative activity against human MV4-11 cells after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human MV4-11 cells after 72 hrs by CellTiter-Glo assay	[PMID: 28956923]
MV4-11	IC₅₀	423 nM Compound: 1; IBN	Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 36399923]
NALM-6	GI₅₀	>10 μM Compound: 1; PCI-32765	Antiproliferative activity against human NALM6 cells after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human NALM6 cells after 72 hrs by CellTiter-Glo assay	[PMID: 28628824]
NAMALVA	GI₅₀	6 μM Compound: 1; PCI-32765	Antiproliferative activity against human NAMALWA cells after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human NAMALWA cells after 72 hrs by CellTiter-Glo assay	[PMID: 28628824]
NAMALVA	IC₅₀	10.45 μM Compound: Ibrutinib	Antiproliferative activity against human NAMALWA cells after 72 hrs by CCK-8 assay Antiproliferative activity against human NAMALWA cells after 72 hrs by CCK-8 assay	[PMID: 29146136]
NAMALVA	IC₅₀	19.6 μM Compound: Ibrutinib	Antiproliferative activity against human NAMALWA cells after 72 hrs by CCK8 assay Antiproliferative activity against human NAMALWA cells after 72 hrs by CCK8 assay	[PMID: 30006143]
NB-4	GI₅₀	3 μM Compound: 1; PCI-32765	Growth inhibition of human NB4 cells Growth inhibition of human NB4 cells	[PMID: 28315597]
NB-4	GI₅₀	7.5 μM Compound: 1; PCI-32765	Antiproliferative activity against human NB4 cells after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human NB4 cells after 72 hrs by CellTiter-Glo assay	[PMID: 28628824]
NCI-H1975	GI₅₀	1.2 μM Compound: 1; PCI-32765	Antiproliferative activity against human NCI-H1975 cells after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human NCI-H1975 cells after 72 hrs by CellTiter-Glo assay	[PMID: 28628824]
NCI-H1975	IC₅₀	1.27 μM Compound: Ibrutinib	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant after 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant after 72 hrs by MTT assay	[PMID: 28734581]
NCI-H1975	EC₅₀	0.64 μM Compound: Ibrutinib	Antiproliferative activity against human NCI-H1975 cells harboring EGFR-L858R/T790M double mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR-L858R/T790M double mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay	[PMID: 28853575]
NCI-H322M	IC₅₀	0.1 μM Compound: Ibrutinib	Antiproliferative activity against human NCI-H322M cells assessed as cell growth inhibition measured after 48 hrs by SRB assay Antiproliferative activity against human NCI-H322M cells assessed as cell growth inhibition measured after 48 hrs by SRB assay	[PMID: 34237622]
NCI-H358	GI₅₀	>10 μM Compound: 1; PCI-32765	Antiproliferative activity against human NCI-H358 cells after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human NCI-H358 cells after 72 hrs by CellTiter-Glo assay	[PMID: 28628824]
NCI-H460	GI₅₀	>10 μM Compound: 1; PCI-32765	Antiproliferative activity against human NCI-H460 cells after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human NCI-H460 cells after 72 hrs by CellTiter-Glo assay	[PMID: 28628824]
NCI-H522	IC₅₀	0.06 μM Compound: Ibrutinib	Antiproliferative activity against human NCI-H522 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay Antiproliferative activity against human NCI-H522 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay	[PMID: 34237622]
NOMO-1	GI₅₀	>10 μM Compound: 1; PCI-32765	Antiproliferative activity against human NOMO1 cells after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human NOMO1 cells after 72 hrs by CellTiter-Glo assay	[PMID: 28628824]
OCI-AML2	GI₅₀	>10 μM Compound: 1; PCI-32765	Antiproliferative activity against human OCI-AML2 cells after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human OCI-AML2 cells after 72 hrs by CellTiter-Glo assay	[PMID: 28628824]
OCI-AML-3	GI₅₀	9.2 μM Compound: 1; PCI-32765	Growth inhibition of human OCI-AML3 cells Growth inhibition of human OCI-AML3 cells	[PMID: 28315597]
OCI-AML-3	GI₅₀	>10 μM Compound: 1; PCI-32765	Antiproliferative activity against human OCI-AML3 cells after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human OCI-AML3 cells after 72 hrs by CellTiter-Glo assay	[PMID: 28628824]
OCI-Ly10	IC₅₀	0.3 nM Compound: 1a	Antiproliferative activity against human OCI-LY10 cells after 6 days by Celltiter-glo luminescent cell viability assay Antiproliferative activity against human OCI-LY10 cells after 6 days by Celltiter-glo luminescent cell viability assay	[PMID: 31381333]
OCI-Ly10	IC₅₀	1 μM Compound: Ibrutinib	Antiproliferative activity against human OCI-LY10 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human OCI-LY10 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 31843459]
OCI-Ly10	IC₅₀	0.35 nM Compound: 1; PCI-32765	Antiproliferative activity against human OCILY10 cells assessed as inhibition of cell growth Antiproliferative activity against human OCILY10 cells assessed as inhibition of cell growth	[PMID: 34479103]
OCI-Ly10	IC₅₀	1030 nM Compound: Ibrutinib	Antiproliferative activity against human OCILY10 cells harboring BTK C481S mutant knockout gene assessed as reduction in cell viability after 96 hrs Antiproliferative activity against human OCILY10 cells harboring BTK C481S mutant knockout gene assessed as reduction in cell viability after 96 hrs	[PMID: 34529443]
OCI-Ly10	IC₅₀	2.29 nM Compound: Ibrutinib	Antiproliferative activity against human OCILY10 cells assessed as inhibition of cell growth incubated for 3 to 7 days by MTS assay Antiproliferative activity against human OCILY10 cells assessed as inhibition of cell growth incubated for 3 to 7 days by MTS assay	[PMID: 35671249]
OCI-Ly10	IC₅₀	4.5 nM Compound: PCI-32765	Antiproliferative activity against human OCILY10 cells assessed as inhibition of cell growth measured after 3 days by CCK-8 assay Antiproliferative activity against human OCILY10 cells assessed as inhibition of cell growth measured after 3 days by CCK-8 assay	[PMID: 37119666]
OCI-Ly3	IC₅₀	>10 μM Compound: Ibrutinib	Antiproliferative activity against human OCILY3 cells incubated for 72 hrs by CellTiter-Glo assay Antiproliferative activity against human OCILY3 cells incubated for 72 hrs by CellTiter-Glo assay	[PMID: 35939993]
OVCAR-4	IC₅₀	7.94 μM Compound: Ibrutinib	Antiproliferative activity against human OVCAR-4 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay Antiproliferative activity against human OVCAR-4 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay	[PMID: 34237622]
PBMC	IC₅₀	22.6 nM Compound: Ibrutinib	Antiinflammatory activity in human PBMC assessed as inhibition of anti-IgM induced CD69 expression incubated for 2 hrs followed by goat F(ab') 2 anti-human IgM addition measured after 18 hrs by flow cytometry analysis Antiinflammatory activity in human PBMC assessed as inhibition of anti-IgM induced CD69 expression incubated for 2 hrs followed by goat F(ab') 2 anti-human IgM addition measured after 18 hrs by flow cytometry analysis	[PMID: 36462441]
PC-3	CC₅₀	>20 μM Compound: 35; PCI-32765	Cytotoxicity against human PC-3 cells Cytotoxicity against human PC-3 cells	[PMID: 33539089]
Pfeiffer	GI₅₀	0.002 μM Compound: Ibrutinib	Cytotoxicity against human Pfeiffer cells assessed as growth inhibition after 72 hrs by CellTiter-Glo luminescent cell viability assay Cytotoxicity against human Pfeiffer cells assessed as growth inhibition after 72 hrs by CellTiter-Glo luminescent cell viability assay	[PMID: 24915291]
Pfeiffer	GI₅₀	1.6 μM Compound: 1; PCI-32765	Growth inhibition of human Pfeiffer cells Growth inhibition of human Pfeiffer cells	[PMID: 28315597]
Pfeiffer	GI₅₀	8.4 μM Compound: 1; PCI-32765	Antiproliferative activity against human Pfeiffer cells after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human Pfeiffer cells after 72 hrs by CellTiter-Glo assay	[PMID: 28628824]
Pfeiffer	IC₅₀	1.652 μM Compound: Ibrutinib	Antiproliferative activity against human Pfeiffer cells incubated for 72 hrs by CellTiter-Glo assay Antiproliferative activity against human Pfeiffer cells incubated for 72 hrs by CellTiter-Glo assay	[PMID: 35939993]
Raji	IC₅₀	19.3 μM Compound: 1	Antiproliferative activity against human Raji cells after 48 hrs by CCK-8 assay Antiproliferative activity against human Raji cells after 48 hrs by CCK-8 assay	[PMID: 27912175]
Raji	IC₅₀	19.5 μM Compound: Ibrutinib	Antiproliferative activity against human Raji cells measured after 48 hrs by CCK-8 assay Antiproliferative activity against human Raji cells measured after 48 hrs by CCK-8 assay	[PMID: 27956037]
Raji	IC₅₀	15.2 μM Compound: Ibrutinib	Antiproliferative activity against human Raji cells after 48 hrs by CCK-8 assay Antiproliferative activity against human Raji cells after 48 hrs by CCK-8 assay	[PMID: 27994736]
Raji	IC₅₀	19.3 μM Compound: 1	Antiproliferative activity against human Raji cells over expressing BTK after 48 hrs by CCK-8 assay Antiproliferative activity against human Raji cells over expressing BTK after 48 hrs by CCK-8 assay	[PMID: 28432946]
Raji	IC₅₀	20.88 μM Compound: Ibrutinib	Antiproliferative activity against human Raji cells after 72 hrs by CCK-8 assay Antiproliferative activity against human Raji cells after 72 hrs by CCK-8 assay	[PMID: 29146136]
Raji	IC₅₀	1.49 μM Compound: 1	Antiproliferative activity against human Raji cells after 48 hrs by CCK8-based assay Antiproliferative activity against human Raji cells after 48 hrs by CCK8-based assay	[PMID: 29567295]
Raji	IC₅₀	19.5 μM Compound: Ibrutinib	Antiproliferative activity against human Raji cells after 72 hrs by CCK8 assay Antiproliferative activity against human Raji cells after 72 hrs by CCK8 assay	[PMID: 30006143]
Raji	IC₅₀	14.2 μM Compound: Ibrutinib	Antiproliferative activity against human Raji cells after 48 hrs by MTT assay Antiproliferative activity against human Raji cells after 48 hrs by MTT assay	[PMID: 30077608]
Raji	IC₅₀	1.49 μM Compound: Ibrutinib	Antiproliferative activity against human Raji cells after 48 hrs by CCK8 assay Antiproliferative activity against human Raji cells after 48 hrs by CCK8 assay	[PMID: 30522954]
Raji	IC₅₀	14.5 μM Compound: Ibrutinib	Antiproliferative activity against human Raji cells after 48 hrs by CCK8 assay Antiproliferative activity against human Raji cells after 48 hrs by CCK8 assay	[PMID: 30605829]
Raji	IC₅₀	14.5 μM Compound: Ibrutinib	Antiproliferative activity against human Raji cells after 48 hrs by MTT assay Antiproliferative activity against human Raji cells after 48 hrs by MTT assay	[PMID: 30881616]
Raji	IC₅₀	15.99 μM Compound: Ibrutinib	Antiproliferative activity against human Raji cells measured after 72 hrs by CCK-8 assay Antiproliferative activity against human Raji cells measured after 72 hrs by CCK-8 assay	[PMID: 31234030]
Raji	IC₅₀	17.7 μM Compound: 1	Antiproliferative activity against human Raji cells assessed as reduction in cell growth incubated for 48 hrs by MTS assay Antiproliferative activity against human Raji cells assessed as reduction in cell growth incubated for 48 hrs by MTS assay	[PMID: 31395509]
Raji	IC₅₀	>20 μM Compound: Ibrutinib	Antiproliferative activity against human Raji cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human Raji cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 31843459]
Raji	IC₅₀	12.56 μM Compound: Ibrutinib	Antiproliferative activity against human Raji cells assessed as reduction in cell viability incubated for 24 hrs by CCK-8 assay Antiproliferative activity against human Raji cells assessed as reduction in cell viability incubated for 24 hrs by CCK-8 assay	[PMID: 32402933]
Raji	IC₅₀	>10 μM Compound: Ibrutinib	Antiproliferative activity against human Raji cells incubated for 72 hrs by CellTiter-Glo assay Antiproliferative activity against human Raji cells incubated for 72 hrs by CellTiter-Glo assay	[PMID: 35939993]
Ramos	IC₅₀	>7.5 nM Compound: Ibrutinib	Inhibition of Btk phosphorylation at Tyr551 in human Ramos cells after 1 hr by Western blot analysis Inhibition of Btk phosphorylation at Tyr551 in human Ramos cells after 1 hr by Western blot analysis	[PMID: 24915291]
Ramos	IC₅₀	14 nM Compound: Ibrutinib	Inhibition of Btk in human Ramos cells assessed as inhibition of PLC-gamma2 phosphorylation at Tyr1217 after 1 hr by Western blot analysis Inhibition of Btk in human Ramos cells assessed as inhibition of PLC-gamma2 phosphorylation at Tyr1217 after 1 hr by Western blot analysis	[PMID: 24915291]
Ramos	IC₅₀	12.6 μM Compound: 1	Antiproliferative activity against human Ramos cells after 48 hrs by CCK-8 assay Antiproliferative activity against human Ramos cells after 48 hrs by CCK-8 assay	[PMID: 27912175]
Ramos	IC₅₀	5.14 μM Compound: Ibrutinib	Antiproliferative activity against human Ramos cells measured after 48 hrs by CCK-8 assay Antiproliferative activity against human Ramos cells measured after 48 hrs by CCK-8 assay	[PMID: 27956037]
Ramos	IC₅₀	8.11 μM Compound: Ibrutinib	Antiproliferative activity against human Ramos cells after 48 hrs by CCK-8 assay Antiproliferative activity against human Ramos cells after 48 hrs by CCK-8 assay	[PMID: 27994736]
Ramos	IC₅₀	28.7 μM Compound: Ibrutinib	Cytotoxicity against human Ramos cells assessed as decrease in cell viability after 24 hrs by CellTiter-Glo assay Cytotoxicity against human Ramos cells assessed as decrease in cell viability after 24 hrs by CellTiter-Glo assay	[PMID: 28274675]
Ramos	IC₅₀	0.5 nM Compound: Ibrutinib	Inhibition of PF-06658607 binding to BTK in human Ramos cells after 1 hr by gel-based ABPP assay Inhibition of PF-06658607 binding to BTK in human Ramos cells after 1 hr by gel-based ABPP assay	[PMID: 28280261]
Ramos	GI₅₀	3.4 μM Compound: 1; PCI-32765	Growth inhibition of human Ramos cells Growth inhibition of human Ramos cells	[PMID: 28315597]
Ramos	IC₅₀	5.88 μM Compound: 1	Antiproliferative activity against human Ramos cells over expressing BTK after 48 hrs by CCK-8 assay Antiproliferative activity against human Ramos cells over expressing BTK after 48 hrs by CCK-8 assay	[PMID: 28432946]
Ramos	GI₅₀	3.9 μM Compound: 1; PCI-32765	Antiproliferative activity against human Ramos cells after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human Ramos cells after 72 hrs by CellTiter-Glo assay	[PMID: 28628824]
Ramos	IC₅₀	6.62 μM Compound: Ibrutinib	Antiproliferative activity against human Ramos cells after 72 hrs by CCK-8 assay Antiproliferative activity against human Ramos cells after 72 hrs by CCK-8 assay	[PMID: 29146136]
Ramos	IC₅₀	8.26 μM Compound: 1	Antiproliferative activity against human Ramos cells after 48 hrs by CCK8-based assay Antiproliferative activity against human Ramos cells after 48 hrs by CCK8-based assay	[PMID: 29567295]
Ramos	IC₅₀	0.92 μM Compound: 1; PCI-32765	Antiproliferative activity against human Ramos cells after 72 hrs by MTT assay Antiproliferative activity against human Ramos cells after 72 hrs by MTT assay	[PMID: 29715023]
Ramos	IC₅₀	5.14 μM Compound: Ibrutinib	Antiproliferative activity against human Ramos cells after 72 hrs by CCK8 assay Antiproliferative activity against human Ramos cells after 72 hrs by CCK8 assay	[PMID: 30006143]
Ramos	IC₅₀	6.18 μM Compound: Ibrutinib	Antiproliferative activity against human Ramos cells after 72 hrs by MTT assay Antiproliferative activity against human Ramos cells after 72 hrs by MTT assay	[PMID: 30108960]
Ramos	IC₅₀	8.26 μM Compound: Ibrutinib	Antiproliferative activity against human Ramos cells after 48 hrs by CCK8 assay Antiproliferative activity against human Ramos cells after 48 hrs by CCK8 assay	[PMID: 30522954]
Ramos	IC₅₀	5.8 μM Compound: Ibrutinib	Antiproliferative activity against human Ramos cells after 48 hrs by CCK8 assay Antiproliferative activity against human Ramos cells after 48 hrs by CCK8 assay	[PMID: 30605829]
Ramos	IC₅₀	5.01 μM Compound: 1	Antiproliferative activity against human Ramos cells Antiproliferative activity against human Ramos cells	[PMID: 30875504]
Ramos	IC₅₀	2.31 μM Compound: Ibrutinib	Antiproliferative activity against human Ramos cells after 48 hrs by MTT assay Antiproliferative activity against human Ramos cells after 48 hrs by MTT assay	[PMID: 30881616]
Ramos	IC₅₀	14 nM Compound: 1a	Inhibition of BTK in human Ramos B cells assessed as reduction in BCR-stimulated calcium flux after 1 hr in dark condition measured for 180 sec Inhibition of BTK in human Ramos B cells assessed as reduction in BCR-stimulated calcium flux after 1 hr in dark condition measured for 180 sec	[PMID: 30893553]
Ramos	IC₅₀	6.66 μM Compound: PCI-32765	Antiproliferative activity against human Ramos cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human Ramos cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 31221612]
Ramos	IC₅₀	14.69 μM Compound: Ibrutinib	Antiproliferative activity against human Ramos cells measured after 72 hrs by CCK-8 assay Antiproliferative activity against human Ramos cells measured after 72 hrs by CCK-8 assay	[PMID: 31234030]
Ramos	IC₅₀	3.5 nM Compound: 1a	Inhibition of BTK in human Ramos cells assessed as reduction in BTK phosphorylation at Tyr223 residue preincubated for 1 hr followed by pervanadate or Na3VO4 stimulation for 20 mins by HTRF assay Inhibition of BTK in human Ramos cells assessed as reduction in BTK phosphorylation at Tyr223 residue preincubated for 1 hr followed by pervanadate or Na3VO4 stimulation for 20 mins by HTRF assay	[PMID: 31381333]
Ramos	IC₅₀	1.88 μM Compound: 1	Antiproliferative activity against human Ramos cells assessed as reduction in cell growth incubated for 48 hrs by MTS assay Antiproliferative activity against human Ramos cells assessed as reduction in cell growth incubated for 48 hrs by MTS assay	[PMID: 31395509]
Ramos	IC₅₀	2.4 μM Compound: Ibrutinib	Antiproliferative activity against human Ramos cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human Ramos cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 31843459]
Ramos	IC₅₀	1.35 μM Compound: Ibrutinib	Antiproliferative activity against human Ramos cells assessed as reduction in cell viability incubated for 24 hrs by CCK-8 assay Antiproliferative activity against human Ramos cells assessed as reduction in cell viability incubated for 24 hrs by CCK-8 assay	[PMID: 32402933]
Ramos	IC₅₀	10 nM Compound: 1; PCI-32765	Antiproliferative activity against human Ramos cells assessed as inhibition of cell growth Antiproliferative activity against human Ramos cells assessed as inhibition of cell growth	[PMID: 34479103]
Ramos	IC₅₀	2.088 μM Compound: Ibrutinib	Antiproliferative activity against human Ramos cells incubated for 72 hrs by CellTiter-Glo assay Antiproliferative activity against human Ramos cells incubated for 72 hrs by CellTiter-Glo assay	[PMID: 35939993]
Ramos	IC₅₀	10 nM Compound: 19	Antiproliferative activity against human Ramos cells assessed as inhibition of cell growth Antiproliferative activity against human Ramos cells assessed as inhibition of cell growth	[PMID: 36155354]
Rec1	GI₅₀	>10 μM Compound: 1; PCI-32765	Antiproliferative activity against human Rec1 cells after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human Rec1 cells after 72 hrs by CellTiter-Glo assay	[PMID: 28628824]
Rec1	IC₅₀	1.1 μM Compound: IBN	Antiproliferative activity against human Rec1 cells assessed as inhibition of cell proliferation incubated for 72 hrs by Cell-titer-Glo luminescent cell viability assay Antiproliferative activity against human Rec1 cells assessed as inhibition of cell proliferation incubated for 72 hrs by Cell-titer-Glo luminescent cell viability assay	[PMID: 30857748]
Rec1	IC₅₀	0.0008 μM Compound: Ibrutinib	Antiproliferative activity against human REC1 cells incubated for 72 hrs by CellTiter-Glo assay Antiproliferative activity against human REC1 cells incubated for 72 hrs by CellTiter-Glo assay	[PMID: 35939993]
Rec1	IC₅₀	0.8 nM Compound: Ibrutinib	Antiproliferative activity against human REC1 cells incubated for 72 hrs by CellTiter-Glo assay Antiproliferative activity against human REC1 cells incubated for 72 hrs by CellTiter-Glo assay	[PMID: 35939993]
Sf9	IC₅₀	0.5 nM Compound: PCI-32765	Inhibition of human full-length BTK expressed in Sf9 cells using FAM-Srctide peptide as substrate after 60 mins by TR-FRET Assay Inhibition of human full-length BTK expressed in Sf9 cells using FAM-Srctide peptide as substrate after 60 mins by TR-FRET Assay	[PMID: 21958547]
Sf9	IC₅₀	200 nM Compound: PCI-32765	Inhibition of LYN-A expressed in Sf9 cells after 60 mins by TR-FRET Assay Inhibition of LYN-A expressed in Sf9 cells after 60 mins by TR-FRET Assay	[PMID: 21958547]
Sf9	IC₅₀	0.34 nM Compound: Ibrutinib	Inhibition of human recombinant full-length N-terminal His-tagged BTK expressed in baculovirus infected Sf9 insect cells measured after 60 mins by ADP-Glo kinase assay Inhibition of human recombinant full-length N-terminal His-tagged BTK expressed in baculovirus infected Sf9 insect cells measured after 60 mins by ADP-Glo kinase assay	[PMID: 27956037]
Sf9	IC₅₀	0.3 nM Compound: Ibrutinib	Inhibition of recombinant human N-terminal His-tagged BTK expressed in baculovirus infected sf9 cells using poly(4:1 Glu,Tyr) as substrate by ADP-Glo kinase assay Inhibition of recombinant human N-terminal His-tagged BTK expressed in baculovirus infected sf9 cells using poly(4:1 Glu,Tyr) as substrate by ADP-Glo kinase assay	[PMID: 27994736]
Sf9	IC₅₀	3.4 nM Compound: 1	Inhibition of full-length human C-terminal His6-tagged BTK C481S mutant expressed in Sf9 insect cells using FAM-Srctide peptide as substrate preincubated for 1 hr followed by substrate addition and measured after 1 hr by TR-FRET Lanthascreen assay Inhibition of full-length human C-terminal His6-tagged BTK C481S mutant expressed in Sf9 insect cells using FAM-Srctide peptide as substrate preincubated for 1 hr followed by substrate addition and measured after 1 hr by TR-FRET Lanthascreen assay	[PMID: 30655951]
Sf9	IC₅₀	>25 μM Compound: Ibrutinib	Inhibition of His-tagged CDK2/Cyclin-E1 (unknown origin) expressed in baculovirus infected Sf9 insect cells using histone H1 as substrate measured in presence of [gamma-33P]ATP Inhibition of His-tagged CDK2/Cyclin-E1 (unknown origin) expressed in baculovirus infected Sf9 insect cells using histone H1 as substrate measured in presence of [gamma-33P]ATP	[PMID: 30943029]
Sf9	IC₅₀	0.0018 μM Compound: Ibrutinib	Inhibition of human recombinant full length N-terminal His tagged BTK expressed in baculovirus infected Sf9 cells using poly (Glu,Tyr) 4:1 as substrate measured after 60 mins in presence of ATP by ADP-Glo kinase assay Inhibition of human recombinant full length N-terminal His tagged BTK expressed in baculovirus infected Sf9 cells using poly (Glu,Tyr) 4:1 as substrate measured after 60 mins in presence of ATP by ADP-Glo kinase assay	[PMID: 31234030]
Sf9	IC₅₀	0.017 μM Compound: Ibrutinib	Inhibition of human recombinant full length N-terminal His tagged BTK C481S mutant expressed in baculovirus infected Sf9 cells using poly (Glu,Tyr) 4:1 as substrate measured after 60 mins in presence of ATP by ADP-Glo kinase assay Inhibition of human recombinant full length N-terminal His tagged BTK C481S mutant expressed in baculovirus infected Sf9 cells using poly (Glu,Tyr) 4:1 as substrate measured after 60 mins in presence of ATP by ADP-Glo kinase assay	[PMID: 31234030]
Sf9	IC₅₀	3.89 nM Compound: 1	Inhibition of human recombinant full length BTK expressed in baculovirus in Sf9 insect cells using Poly (4:1 Glu, Tyr) as substrate incubated for 1 hr by ADP-Glo assay Inhibition of human recombinant full length BTK expressed in baculovirus in Sf9 insect cells using Poly (4:1 Glu, Tyr) as substrate incubated for 1 hr by ADP-Glo assay	[PMID: 31395509]
Sf9	IC₅₀	16.1 nM Compound: Ibrutinib	Inhibition of recombinant human N-terminal GST-tagged JAK3 (781 to end residues) expressed in baculovirus infected Sf9 cells using poly (Glu,Tyr) 4:1 as substrate incubated for 60 mins in presence of ATP by ADP-Glo kinase assay Inhibition of recombinant human N-terminal GST-tagged JAK3 (781 to end residues) expressed in baculovirus infected Sf9 cells using poly (Glu,Tyr) 4:1 as substrate incubated for 60 mins in presence of ATP by ADP-Glo kinase assay	[PMID: 31866272]
SKM-1	GI₅₀	3.6 μM Compound: 1; PCI-32765	Growth inhibition of human SKM1 cells Growth inhibition of human SKM1 cells	[PMID: 28315597]
SKM-1	GI₅₀	3.9 μM Compound: 1; PCI-32765	Antiproliferative activity against human SKM1 cells after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human SKM1 cells after 72 hrs by CellTiter-Glo assay	[PMID: 28628824]
SK-MEL-5	IC₅₀	6.31 μM Compound: Ibrutinib	Antiproliferative activity against human SK-MEL-5 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay Antiproliferative activity against human SK-MEL-5 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay	[PMID: 34237622]
SNB-75	IC₅₀	3.16 μM Compound: Ibrutinib	Antiproliferative activity against human SNB-75 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay Antiproliferative activity against human SNB-75 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay	[PMID: 34237622]
SUD4	IC₅₀	0.804 μM Compound: Ibrutinib	Antiproliferative activity against human SU-DHL-4 cells incubated for 72 hrs by CellTiter-Glo assay Antiproliferative activity against human SU-DHL-4 cells incubated for 72 hrs by CellTiter-Glo assay	[PMID: 35939993]
SU-DHL-2	GI₅₀	0.64 μM Compound: 1; PCI-32765	Growth inhibition of human SU-DHL-2 cells Growth inhibition of human SU-DHL-2 cells	[PMID: 28315597]
SU-DHL-2	GI₅₀	2.2 μM Compound: 1; PCI-32765	Antiproliferative activity against human SUDHL2 cells after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human SUDHL2 cells after 72 hrs by CellTiter-Glo assay	[PMID: 28628824]
SU-DHL-6	GI₅₀	0.58 μM Compound: Ibrutinib	Cytotoxicity against human SU-DHL6 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo luminescent cell viability assay Cytotoxicity against human SU-DHL6 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo luminescent cell viability assay	[PMID: 24915291]
SU-DHL-6	IC₅₀	0.8742 μM Compound: Ibrutinib	Antiproliferative activity against human SU-DHL6 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay Antiproliferative activity against human SU-DHL6 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay	[PMID: 30522954]
SU-DHL-6	IC₅₀	1.498 μM Compound: Ibrutinib	Antiproliferative activity against human SU-DHL-6 cells incubated for 72 hrs by CellTiter-Glo assay Antiproliferative activity against human SU-DHL-6 cells incubated for 72 hrs by CellTiter-Glo assay	[PMID: 35939993]
SW480	IC₅₀	25.6 μM Compound: ibrutinib	Cytotoxicity against human SW480 cells assessed as cell growth inhibition after 3 days by presto blue dye based plate reader method Cytotoxicity against human SW480 cells assessed as cell growth inhibition after 3 days by presto blue dye based plate reader method	[PMID: 27077228]
THP-1	IC₅₀	20.1 μM Compound: Ibrutinib	Cytotoxicity against human THP-1 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human THP-1 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 29324347]
TMD8	IC₅₀	0.01 μM Compound: 1; PCI-32765	Antiproliferative activity against human TMD8 cells after 72 hrs by MTT assay Antiproliferative activity against human TMD8 cells after 72 hrs by MTT assay	[PMID: 29715023]
TMD8	IC₅₀	0.01 μM Compound: PCI-32765	Antiproliferative activity against human TMD8 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human TMD8 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 31221612]
TMD8	IC₅₀	0.01 nM Compound: Ibrutinib	Antiproliferative activity against human TMD8 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human TMD8 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 33740548]
TMD8	IC₅₀	6.4 nM Compound: Ibrutinib	Antiproliferative activity against human TMD8 cells assessed as inhibition of cell growth incubated for 3 to 7 days by MTS assay Antiproliferative activity against human TMD8 cells assessed as inhibition of cell growth incubated for 3 to 7 days by MTS assay	[PMID: 35671249]
TMD8	IC₅₀	2.7 nM Compound: Ibrutinib	Antiproliferative activity against human TMD8 cells incubated for 72 hrs by CellTiter-Glo assay Antiproliferative activity against human TMD8 cells incubated for 72 hrs by CellTiter-Glo assay	[PMID: 35939993]
TMD8	IC₅₀	4.7 nM Compound: PCI-32765	Antiproliferative activity against human TMD8 cells assessed as inhibition of cell growth measured after 3 days by CCK-8 assay Antiproliferative activity against human TMD8 cells assessed as inhibition of cell growth measured after 3 days by CCK-8 assay	[PMID: 37119666]
U-251	IC₅₀	6.31 μM Compound: Ibrutinib	Antiproliferative activity against human U-251 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay Antiproliferative activity against human U-251 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay	[PMID: 34237622]
U2932	GI₅₀	4.4 μM Compound: 1; PCI-32765	Growth inhibition of human U2932 cells Growth inhibition of human U2932 cells	[PMID: 28315597]
U2932	GI₅₀	4 μM Compound: 1; PCI-32765	Antiproliferative activity against human U2932 cells after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human U2932 cells after 72 hrs by CellTiter-Glo assay	[PMID: 28628824]
U-937	GI₅₀	2.9 μM Compound: 1; PCI-32765	Growth inhibition of human U937 cells Growth inhibition of human U937 cells	[PMID: 28315597]
U-937	GI₅₀	8.5 μM Compound: 1; PCI-32765	Antiproliferative activity against human U937 cells after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human U937 cells after 72 hrs by CellTiter-Glo assay	[PMID: 28628824]
U-937	IC₅₀	4.4 μM Compound: 1; PCI-32765	Antiproliferative activity against human U-937 cells assessed as reduction in cell viability incubated for 48 hrs by CCK8 assay Antiproliferative activity against human U-937 cells assessed as reduction in cell viability incubated for 48 hrs by CCK8 assay	[PMID: 35099969]
UO-31	IC₅₀	1.26 μM Compound: Ibrutinib	Antiproliferative activity against human UO-31 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay Antiproliferative activity against human UO-31 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay	[PMID: 34237622]
WSU-NHL	GI₅₀	1.09 μM Compound: Ibrutinib	Cytotoxicity against human WSU-NHL cells assessed as growth inhibition after 72 hrs by CellTiter-Glo luminescent cell viability assay Cytotoxicity against human WSU-NHL cells assessed as growth inhibition after 72 hrs by CellTiter-Glo luminescent cell viability assay	[PMID: 24915291]
Z-138	GI₅₀	>10 μM Compound: 1; PCI-32765	Antiproliferative activity against human Z138 cells after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human Z138 cells after 72 hrs by CellTiter-Glo assay	[PMID: 28628824]
Z-138	IC₅₀	11.3 μM Compound: IBN	Antiproliferative activity against human Z138 cells assessed as inhibition of cell proliferation incubated for 72 hrs by Cell-titer-Glo luminescent cell viability assay Antiproliferative activity against human Z138 cells assessed as inhibition of cell proliferation incubated for 72 hrs by Cell-titer-Glo luminescent cell viability assay	[PMID: 30857748]
Z-138	IC₅₀	14.4 μM Compound: IBN	Antiproliferative activity against human Z138 cells assessed as reduction in viability after 72 hrs by CellTiter-Glo luminescent assay Antiproliferative activity against human Z138 cells assessed as reduction in viability after 72 hrs by CellTiter-Glo luminescent assay	[PMID: 31229421]
Z-138	IC₅₀	9.7 nM Compound: 24	Antiproliferative activity against human Z138 cells assessed as reduction cell viability measured after 24 hrs by Cell Titer-Glo Luminescent Cell Viability Assay Antiproliferative activity against human Z138 cells assessed as reduction cell viability measured after 24 hrs by Cell Titer-Glo Luminescent Cell Viability Assay	[PMID: 36324498]

In Vitro

Ibrutinib (PCI-32765) selectively inhibits B-cell signaling and activation. It inhibits autophosphorylation of Btk (IC₅₀=11 nM), phosphorylation of Btk's physiological substrate PLCγ (IC₅₀=29 nM), and phosphorylation of a further downstream kinase, ERK (IC₅₀=13 nM)^[1].
Ibrutinib (PCI-32765) inhibits BCR-activated primary B cell proliferation (IC₅₀=8 nM). Following FcγR stimulation, Ibrutinib (PCI-32765) inhibits TNFα, IL-1β and IL-6 production in primary monocytes (IC₅₀=2.6, 0.5, 3.9 nM, respectively)^[3].
Ibrutinib binds C481 (Cysteine481) of BTK with an ideal IC₅₀ of 0.5?nM. Ibrutinib cannot form a covalent bond with the hydroxyl group of serine, C481S mutation increases the IC₅₀ against BTK-C481S phosphorylation from 2.2?nM to 1?μM^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Ibrutinib (PCI-32765) (3.125-50 mg/kg, p.o.) reduces the level of circulating autoantibodies and completely suppresses disease in mice with collagen-induced arthritis. Ibrutinib (PCI-32765) inhibits autoantibody production and the development of kidney disease in the MRL-Fas(lpr) lupus model. Ibrutinib (PCI-32765) (3.125-50 mg/kg, p.o.) reduces renal disease and autoantibody production in MRL-Fas(lpr) mice^[1]. Ibrutinib (PCI-32765) (0.1 μM) inhibits activation-induced proliferation of CLL cells, induces selective cytotoxicity in B cells compared with T cells, but alters activation induced T-cell cytokine production^[2]. Ibrutinib (PCI-32765) dose-dependently and potently reverses arthritic inflammation in a therapeutic CIA model with an ED₅₀ of 2.6 mg/kg/day. Ibrutinib (PCI-32765) also prevents clinical arthritis in CAIA models^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 936563-96-1
Appearance Solid
Masse moléculaire 440.50
Formule C₂₅H₂₄N₆O₂
Color White to off-white
SMILES

C=CC(N1C[C@H](N2N=C(C3=CC=C(OC4=CC=CC=C4)C=C3)C5=C(N)N=CN=C52)CCC1)=O
Synonyms

PCI-32765
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Publications (136)

All WBIHC

Sort by:

Journal Impact Factor

Signal Transduct Target Ther

BMX inhibition overcomes small cell lung cancer chemoresistance by stabilizing E2F1 via ERK1/2-Cyclin D1/CDK4/6 axis. [Abstract]

2026 Apr 8;11(1):125. PMID: 41946708
Signal Transduct Target Ther

Discovery of a highly potent and selective Bruton's tyrosine kinase inhibitor avoiding impairment of ADCC effects for B-cell non-Hodgkin lymphoma. [Abstract]

2020 Sep 14;5(1):200. PMID: 32929063
Signal Transduct Target Ther

STAT3 mediates C6-ceramide-induced cell death in chronic lymphocytic leukemia. [Abstract]

2017 Oct 27;2:17051. PMID: 29263930

Ibrutinib purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2017 Oct 27;2:17051. [Abstract]

BTK inhibitors suppress phosphorylation of STAT3 in JVM-3 cells and CLL patient cells. Cells are treated with varying concentrations of Ibrutinib for indicated time periods and western blotting is performed.
Nature

Inhibitors supercharge kinase turnover through native proteolytic circuits. [Abstract]

2026 Jan;649(8098):1032-1041. PMID: 41299171
Cancer Cell

A Probabilistic Classification Tool for Genetic Subtypes of Diffuse Large B Cell Lymphoma with Therapeutic Implications. [Abstract]

2020 Apr 13;37(4):551-568.e14. PMID: 32289277
Mol Cancer

Overexpression of wild type RRAS2, without oncogenic mutations, drives chronic lymphocytic leukemia. [Abstract]

2022 Feb 4;21(1):35. PMID: 35120522
Immunity

Inhibition of the BTK-IDO-mTOR axis promotes differentiation of monocyte-lineage dendritic cells and enhances anti-tumor T cell immunity. [Abstract]

2021 Oct 12;54(10):2354-2371.e8. PMID: 34614413
Blood

The HCK/BTK inhibitor KIN-8194 is active in MYD88-driven lymphomas and overcomes mutated BTKCys481 ibrutinib resistance. [Abstract]

2021 Nov 18;138(20):1966-1979. PMID: 34132782
Blood

HCK is a survival determinant transactivated by mutated MYD88, and a direct target of ibrutinib. [Abstract]

2016 Jun 23;127(25):3237-52. PMID: 27143257
Cancer Res

Osimertinib covalently binds to CD34 and eliminates myeloid leukemia stem/progenitor cells. [Abstract]

2024 Feb 1;84(3):479-492. PMID: 38095536
Cancer Res

Tumor-Derived Pericytes Driven by EGFR Mutations Govern the Vascular and Immune Microenvironment of Gliomas. [Abstract]

2021 Apr 15;81(8):2142-2156. PMID: 33593822
Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
Theranostics

Inhibition of Bruton's tyrosine kinase restricts neuroinflammation following intracerebral hemorrhage. [Abstract]

2025 Jan 1;15(2):494-508. PMID: 39744694
Theranostics

Inhibition of acylglycerol kinase sensitizes DLBCL to venetoclax via upregulation of FOXO1-mediated BCL-2 expression. [Abstract]

2022 Jul 18;12(12):5537-5550. PMID: 35910796
Acta Pharm Sin B

A novel IRAK4/PIM1 inhibitor ameliorates rheumatoid arthritis and lymphoid malignancy by blocking the TLR/MYD88-mediated NF- κ B pathway. [Abstract]

2023 Mar;13(3):1093-1109. PMID: 36970199
J Exp Clin Cancer Res

Combination of Enzastaurin and Ibrutinib synergistically induces anti-tumor effects in diffuse large B cell lymphoma. [Abstract]

2019 Feb 18;38(1):86. PMID: 30777096
J Exp Clin Cancer Res

High expression of Bruton's tyrosine kinase (BTK) is required for EGFR-induced NF-κB activation and predicts poor prognosis in human glioma. [Abstract]

2017 Sep 25;36(1):132. PMID: 28946903

Ibrutinib purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2017 Sep 25;36(1):132. [Abstract]

The effects of Ibrutinib on the expression levels of cell cycle-related protein. U87 and U251 cells are treated with Ibrutinib for 12 h. The protein extracts are examined using Western blot analysis with the indicated antibodies.
Blood Cancer J

Docirbrutinib is a pan-mutant BTK inhibitor and inhibits B-cell receptor signaling in chronic lymphocytic leukemia cells in preclinical and early clinical investigations. [Abstract]

2026 May 7;16(1):107. PMID: 42098067
Biomaterials

Automated discovery of nanomaterials via drug aggregation induced emission. [Abstract]

2022 Oct:289:121800. PMID: 36166893
Cell Mol Biol Lett

ENPP2 promotes progression and lipid accumulation via AMPK/SREBP1/FAS pathway in chronic lymphocytic leukemia. [Abstract]

2024 Dec 27;29(1):159. PMID: 39731014
Cell Death Dis

miR-28-based combination therapy impairs aggressive B cell lymphoma growth by rewiring DNA replication. [Abstract]

2023 Oct 18;14(10):687. PMID: 37852959
Pharmacol Res

Destabilization of ROR1 enhances activity of Ibrutinib against chronic lymphocytic leukemia in vivo. [Abstract]

2020 Jan;151:104512. PMID: 31726100
J Immunother Cancer

1α,25(OH)2D3 reverses exhaustion and enhances antitumor immunity of human cytotoxic T cells. [Abstract]

2022 Mar;10(3):e003477. PMID: 35318258
J Allergy Clin Immunol

Autoantibodies to IgE and FcεRI and the natural variability of spleen tyrosine kinase expression in basophils. [Abstract]

2019 Mar;143(3):1100-1107.e11. PMID: 29859965
J Neuroinflammation

Fenebrutinib, a Bruton's tyrosine kinase inhibitor, blocks distinct human microglial signaling pathways. [Abstract]

2024 Oct 27;21(1):276. PMID: 39465429
Adv Healthc Mater

An Immunomodulator-Boosted Lactococcus Lactis Platform For Enhanced In Situ Tumor Vaccine. [Abstract]

2024 Jul 25:e2401635. PMID: 39054611
Adv Healthc Mater

A Dual-Function CD47-Targeting Nano-Drug Delivery System Used to Regulate Immune and Anti-Inflammatory Activities in the Treatment of Atherosclerosis. [Abstract]

2024 May 24:e2400752. PMID: 38794825
Clin Cancer Res

The novel immunocompetent Eµ-SOX11CCND1 mouse model phenotypically and molecularly resembles human mantle cell lymphoma. [Abstract]

2025 Aug 26. PMID: 40857109
Acta Pharmacol Sin

Activation of unfolded protein response overcomes Ibrutinib resistance in diffuse large B-cell lymphoma. [Abstract]

2021 May;42(5):814-823. PMID: 32855532
J Infection

Ibrutinib suppresses intracellular mycobacterium tuberculosis growth by inducing macrophage autophagy. [Abstract]

2020 Jun;80(6):e19-e26. PMID: 32171871
NPJ Precis Oncol

Integrative profiling strategies to guide personalized therapy in mantle cell lymphoma: a pilot study. [Abstract]

2025 Nov 21;9(1):373. PMID: 41272086
Leukemia

Discovery of a BTK/MNK dual inhibitor for lymphoma and leukemia. [Abstract]

2016 Jan;30(1):173-81. PMID: 26165234
Int J Biol Macromol

CDK1 inhibitor RO-3306 enhances BTKi potency in diffuse large B-cell lymphoma by suppressing JAK2/STAT3 signaling. [Abstract]

2025 Jan 14:139893. PMID: 39818374
Mol Ther Oncolytics

Addition of BTK inhibitor orelabrutinib to rituximab improved anti-tumor effects in B cell lymphoma. [Abstract]

2021 Apr 3:21:158-170. PMID: 33981831
Blood Adv

Zanubrutinib and pirtobrutinib show synergistic killing and suppression of BTK signaling in MYD88-mutated lymphoma cells. [Abstract]

2026 Jul 14;10(13):4450-4454. PMID: 41985014
Blood Adv

PLCG2 Exon-Skipped Variants: Insights into Their Potential Role in Chronic Lymphocytic Leukemia. [Abstract]

2026 Jun 5:bloodadvances.2025019077. PMID: 42263669
Cell Rep

MEF2A suppresses stress responses that trigger DDX41-dependent IFN production. [Abstract]

2023 Jul 18;42(8):112805. PMID: 37467105
Br J Pharmacol

Bruton tyrosine kinase (Btk) in neutrophils is indispensable for initiating and maintaining skin inflammation in a model of pemphigoid diseases. [Abstract]

2026 Jan 18. PMID: 41549045
Br J Pharmacol

A non-covalent inhibitor XMU-MP-3 overrides ibrutinib-resistant BtkC481S mutation in B-cell malignancies. [Abstract]

2019 Dec;176(23):4491-4509. PMID: 31364164
J Med Chem

Exploring 2-Sulfonylpyrimidine Warheads as Acrylamide Surrogates for Targeted Covalent Inhibition: A BTK Story. [Abstract]

2024 Aug 22;67(16):13572-13593. PMID: 39119945
J Med Chem

Discovery of 1-Amino-1 H-imidazole-5-carboxamide Derivatives as Highly Selective, Covalent Bruton's Tyrosine Kinase (BTK) Inhibitors. [Abstract]

2021 Nov 11;64(21):16242-16270. PMID: 34672559
Pharmaceutics

Ibrutinib Inhibits Angiogenesis and Tumorigenesis in a BTK-Independent Manner. [Abstract]

2022 Sep 5;14(9):1876. PMID: 36145624
Eur J Med Chem

Discovery of novel BCL6-Targeting PROTACs with effective antitumor activities against DLBCL in vitro and in vivo. [Abstract]

2024 Aug 23:277:116789. PMID: 39208743
Talanta

Enantioseparation and ecotoxicity evaluation of ibrutinib by Electrokinetic Chromatography using single and dual systems. [Abstract]

2023 Dec 1:265:124783. PMID: 37348354
Eur J Med Chem

Scaffold hopping of the SYK inhibitor entospletinib leads to broader targeting of the BCR signalosome. [Abstract]

2020 Oct 15;204:112636. PMID: 32731189
Ecotoxicol Environ Saf

PPARγ-responsive luciferase reporter system for high-throughput screening of chemical toxins with potential pulmonary fibrosis effects. [Abstract]

2025 Nov 15:307:119433. PMID: 41273832
Biochem Pharmacol

MEK inhibitor induces cardiac complications by preventing ZMYND8-mediated ubiquitination and proteasomal degradation of HMGB1. [Abstract]

2025 Dec 19:245:117660. PMID: 41423035
Acta Neuropathol Commun

Ibrutinib disrupts blood-tumor barrier integrity and prolongs survival in rodent glioma model. [Abstract]

2024 Apr 8;12(1):56. PMID: 38589905
Acta Neuropathol Commun

Bruton's tyrosine kinase inhibition reduces disease severity in a model of secondary progressive autoimmune demyelination. [Abstract]

2023 Jul 12;11(1):115. PMID: 37438842
Biochem Pharmacol

EP4 receptor agonist L-902688 augments cytotoxic activities of ibrutinib, idelalisib, and venetoclax against chronic lymphocytic leukemia cells. [Abstract]

2021 Jan;183:114352. PMID: 33278351
Mol Cell Proteomics

TSLP signaling network revealed by SILAC-based phosphoproteomics. [Abstract]

2012 Jun;11(6):M112.017764. PMID: 22345495

Ibrutinib purchased from MedChemExpress. Usage Cited in: Mol Cell Proteomics. 2012 Jun;11(6):M112.017764. [Abstract]

Btk protein tyrosine kinase is involved in TSLP signaling. Western blotting analysis is performed to demonstrate the roles of Btk in TSLP-induced Stat3 and Stat5 phosphorylation. Exponentially growing Ba/F3-IT cells are pretreated with 0.1% DMSO or 1 μM PCI-32765 or 10 μM PCI-32765 for 1 h at 37 °C and then are stimulated with TSLP for the indicated times at 37 °C. The phosphorylation of Btk, Stat3, and Stat5a is probed with phosphospecific antibodies against p-Btk (Y551), p-Stat3 (Y705), and p-
J Neuroimmune Pharmacol

Inhibition of Bruton's Tyrosine Kinase Modulates Microglial Phagocytosis: Therapeutic Implications for Alzheimer's Disease. [Abstract]

2019 Sep;14(3):448-461. PMID: 30758770

Ibrutinib purchased from MedChemExpress. Usage Cited in: J Neuroimmune Pharmacol. 2019 Sep;14(3):448-461. [Abstract]

Representative confocal microscopy images of BV2 cells incubated with 1 μM of CC-292 or ibrutinib for 2 h followed by incubation with pHrodo zymosan particles for 1 h.

Ibrutinib purchased from MedChemExpress. Usage Cited in: J Neuroimmune Pharmacol. 2019 Sep;14(3):448-461. [Abstract]

Representative confocal microscopy images of human monocyte-derived macrophages incubated with 1 μM of CC-292 or ibrutinib for 24 h followed by incubation with pHrodo zymosan particles for 1 h.
Surfaces and Interfaces

2024 Mar, 46, 104161.
Cells

Ibrutinib in the Treatment of Solid Tumors: Current State of Knowledge and Future Directions. [Abstract]

2022 Apr 14;11(8):1338. PMID: 35456016
Cancer Immunol Immunother

Targeting interleukin-2-inducible T cell kinase ameliorates immune-mediated aplastic anemia. [Abstract]

2025 Apr 29;74(6):188. PMID: 40299061
Commun Biol

Disulfiram treatment suppresses antibody-producing reactions by inhibiting macrophage activation and B cell pyrimidine metabolism. [Abstract]

2024 Apr 22;7(1):488. PMID: 38649462
Cancer Immunol Immunother

BTLA dysregulation correlates with poor outcome and diminished T cell-mediated antitumor responses in chronic lymphocytic leukemia. [Abstract]

2023 Jul;72(7):2529-2539. PMID: 37041226
Int Immunopharmacol

Blockade of Bruton's tyrosine kinase suppresses B cell activation and antibody secretion in systemic lupus erythematosus. [Abstract]

2025 Oct 10:163:115297. PMID: 40763474
Int J Mol Sci

Inhibition of Bruton Tyrosine Kinase Reduces Neuroimmune Cascade and Promotes Recovery after Spinal Cord Injury. [Abstract]

2021 Dec 29;23(1):355. PMID: 35008785
Stem Cell Reports

Ibrutinib Displays Atrial-Specific Toxicity in Human Stem Cell-Derived Cardiomyocytes. [Abstract]

2019 May 14;12(5):996-1006. PMID: 31031187
Front Pharmacol

Influence of YES1 Kinase and Tyrosine Phosphorylation on the Activity of OCT1. [Abstract]

2021 Mar 8;12:644342. PMID: 33790797
Sci Rep

BTK promotes neuroinflammation after intracerebral hemorrhage involving hub genes and alterations in microglial functions. [Abstract]

2026 May 4;16(1):20485. PMID: 42082621
Sci Rep

Cysteine-reactive mitigators of small vessel disease-related NOTCH3 mutants. [Abstract]

2026 Mar 20;16(1):14300. PMID: 41862552
Sci Rep

Dasatinib exacerbates splenomegaly of mice inoculated with Epstein-Barr virus-infected lymphoblastoid cell lines. [Abstract]

2020 Mar 9;10(1):4355. PMID: 32152351
Sci Rep

Irreversible inhibition of BTK kinase by a novel highly selective inhibitor CHMFL-BTK-11 suppresses inflammatory response in rheumatoid arthritis model. [Abstract]

2017 Mar 28;7(1):466. PMID: 28352114
Sci Rep

Cardiac endothelial cell-derived exosomes induce specific regulatory B cells. [Abstract]

2014 Dec 23;4:7583. PMID: 25533220
Cancers (Basel)

Bruton's Tyrosine Kinase Inhibitors Ibrutinib and Acalabrutinib Counteract Anthracycline Resistance in Cancer Cells Expressing AKR1C3. [Abstract]

2020 Dec 11;12(12):3731. PMID: 33322571
Rheumatology (Oxford)

Autophagy inhibitors block pathogenic NET release in immune-mediated inflammatory disease without impairing host defence. [Abstract]

2025 Aug 13:keaf437. PMID: 40802538
Cell Signal

BTK-independent regulation of calcium signalling downstream of the B-cell receptor in malignant B-cells. [Abstract]

2022 Aug:96:110358. PMID: 35597428
Oncol Rep

Evaluation of anticancer agents using patient-derived tumor organoids characteristically similar to source tissues. [Abstract]

2018 Aug;40(2):635-646. PMID: 29917168
iScience

Mechanism-based prediction of drug synergy via network controllability analysis of therapeutic pathways in intractable diseases. [Abstract]

2026 Mar 11;29(4):115339. PMID: 41952985
iScience

Inhibition of proteolytic and ATPase activities of the proteasome by the BTK inhibitor CGI-1746. [Abstract]

2024 Sep 24;27(11):110961. PMID: 39759071
Cytotherapy

Bruton tyrosine kinase inhibitors preserve anti-CD19 chimeric antigen receptor T-cell functionality and reprogram tumor micro-environment in B-cell lymphoma. [Abstract]

2023 Jul;25(7):739-749. PMID: 37074239
Brain Res Bull

Geniposide protects depression through BTK/JAK2/STAT1 signaling pathway in lipopolysaccharide-induced depressive mice. [Abstract]

2021 May:170:65-73. PMID: 33561536
Macromol Biosci

Obinutuzumab-Based Drug-Free Macromolecular Therapeutics Synergizes with Topoisomerase Inhibitors. [Abstract]

2024 Mar;24(3):e2300375. PMID: 37838941
Cancer Innov

Mitigating ibrutinib-induced ventricular arrhythmia and cardiac dysfunction with metformin. [Abstract]

2024 Nov 13;4(1):e151. PMID: 39544722
Front Biosci (Landmark Ed)

Ibrutinib Contributes to Atrial Arrhythmia through the Autophagic Degradation of Connexins by Inhibiting the PI3K-AKT-mTOR Signaling Pathway. [Abstract]

2024 May 22;29(5):201. PMID: 38812314
Clin Immunol

Bruton's tyrosine kinase ablation inhibits B cell responses and antibody production for the prevention of chronic rejection in cardiac transplantation. [Abstract]

2024 Apr:261:109941. PMID: 38365047
BMC Cancer

Distinct BTK inhibitors differentially induce apoptosis but similarly suppress chemotaxis and lipid accumulation in mantle cell lymphoma. [Abstract]

2021 Jun 26;21(1):732. PMID: 34174847
BMC Cancer

2021 Jun 26;21(1):732.
Cancer Res Commun

Cyclin-Dependent Kinase-9 and Oxidative Phosphorylation Inhibition Overcomes Ibrutinib Resistance in Mantle Cell Lymphoma. [Abstract]

2026 May 1;6(5):1192-1205. PMID: 42048618
ACS Pharmacol Transl Sci

Comprehensive Characterization of Bruton's Tyrosine Kinase Inhibitor Specificity, Potency, and Biological Effects: Insights into Covalent and Noncovalent Mechanistic Signatures. [Abstract]

2025 Mar 12;8(4):917-931. PMID: 40242575
J Chromatogr A

Modelling the simultaneous chiral separation of a group of drugs by electrokinetic chromatography using mixtures of cyclodextrins. [Abstract]

2022 Oct 11:1681:463444. PMID: 36075136
Pathogens

Chronic Hepatitis E Virus Infection during Lymphoplasmacytic Lymphoma and Ibrutinib Treatment. [Abstract]

2019 Aug 22;8(3):129. PMID: 31443360
Mol Immunol

Ibrutinib protects against acute lung injury via inhibiting NLRP3/Caspase-1 in septic mice model. [Abstract]

2022 Dec:152:232-239. PMID: 36379131
Toxicol Appl Pharmacol

Effects of tyrosine kinase inhibitors on androgen, estrogen α, glucocorticoid and thyroid receptors. [Abstract]

2022 Jan 1:434:115818. PMID: 34890638
Br J Haematol

The BCL2 antagonist ABT-199 triggers apoptosis, and augments ibrutinib and idelalisib mediated cytotoxicity in CXCR4 Wild-type and CXCR4 WHIM mutated Waldenstrom macroglobulinaemia cells. [Abstract]

2015 Jul;170(1):134-8. PMID: 25582069

Ibrutinib purchased from MedChemExpress. Usage Cited in: Br J Haematol. 2015 Jul;170(1):134-8. [Abstract]

Treatment of CXCR4^WT and CXCR4^S338X BCWM.1 and MWCL-1 cells with Ibrutinib or CAL-101 induced caspase-3 and PARP cleavage at 6 h. Caspase-3 and PAPR cleavage following Ibrutinib (IB), CAL-101 (ID), ABT-199 (ABT), in the presence of absence of CXCL12 (SDF) and AMD3100 (AMD).
Br J Haematol

CXCR4 WHIM-like frameshift and nonsense mutations promote ibrutinib resistance but do not supplant MYD88(L265P) -directed survival signalling in Waldenström macroglobulinaemia cells. [Abstract]

2015 Mar;168(5):701-7. PMID: 25371371
Exp Cell Res

Network-based analysis with primary cells reveals drug response landscape of acute myeloid leukemia. [Abstract]

2020 Aug 1;393(1):112054. PMID: 32376287
J Pharm Biomed Anal

Development and validation of LC-MS/MS method for estimating the pharmacokinetics, protein binding, and metabolic stability of soluble epoxide hydrolase inhibitor EC5026. [Abstract]

2024 Jan 5:237:115797. PMID: 37847987
Psychopharmacology

The protective effect of Geniposide on diabetic cognitive impairment through BTK/TLR4/NF-κB pathway. [Abstract]

2020 Feb;237(2):465-477. PMID: 31811349
Cancer Control

The Serum- and Glucocorticoid-Inducible Kinase 1 (SGK1) as a Novel Therapeutic Target in Mantle Cell Lymphoma. [Abstract]

2022 Jan-Dec:29:10732748221143881. PMID: 36519740
Int J Clin Oncol

Cell-type-specific sensitivity of bortezomib in the methotrexate-resistant primary central nervous system lymphoma cells. [Abstract]

2019 Sep;24(9):1020-1029. PMID: 30993483
PLoS One

A novel small molecule screening assay using normal human chondrocytes toward osteoarthritis drug discovery. [Abstract]

2024 Nov 1;19(11):e0308647. PMID: 39485774
PLoS One

Luxeptinib interferes with LYN-mediated activation of SYK and modulates BCR signaling in lymphoma. [Abstract]

2023 Mar 8;18(3):e0277003. PMID: 36888611
Fundam Clin Pharmacol

Inhibition of organic cation transporter 3 activity by tyrosine kinase inhibitors. [Abstract]

2021 Oct;35(5):919-929. PMID: 33523504
J Invest Surg

Rapamycin Inhibits Nf-ΚB Activation by Autophagy to Reduce Catabolism in Human Chondrocytes. [Abstract]

2020 Oct;33(9):861-873. PMID: 30945580
J Chromatogr B Analyt Technol Biomed Life Sci

Development and validation of an LC-MS/MS assay for the quantification of Miransertib in human plasma and clinical application. [Abstract]

2026 May 29:1281:125161. PMID: 42224880
J Chromatogr B Analyt Technol Biomed Life Sci

Application of newly developed and validated UPLC-MS/MS method for pharmacokinetic study of ROS1/NTRK inhibitor taletrectinib in beagle dog plasma. [Abstract]

2024 Sep 14:1247:124305. PMID: 39293159
Eur J Drug Metab Pharmacokinet

Differential Inhibition of Equilibrative Nucleoside Transporter 1 (ENT1) Activity by Tyrosine Kinase Inhibitors. [Abstract]

2021 Sep;46(5):625-635. PMID: 34275128
Genes Chromosomes Cancer

Establishment and characterization of a MALT lymphoma cell line carrying an API2-MALT1 translocation. [Abstract]

2020 Sep;59(9):517-524. PMID: 32348592
Braz J Med Biol Res

Synergistic effect of venetoclax and ibrutinib on ibrutinib-resistant ABC-type DLBCL cells. [Abstract]

2024 Oct 7:57:e13278. PMID: 39383379
J Toxicol Sci

Validation of a new protocol for a zebrafish MEFL (malformation or embryo-fetal lethality) test method that conforms to the ICH S5 (R3) guideline. [Abstract]

2024;49(8):337-348. PMID: 39098043
Rapid Commun Mass Spectrom

In vitro metabolism of ibrutinib in rat, dog and human hepatocytes using liquid chromatography combined with diode-array detection and Q-Exactive Orbitrap tandem mass spectrometry. [Abstract]

2019 Dec 15;33(23):1804-1815. PMID: 31364190
Biomed Chromatogr

Pharmacokinetics, Bioavailability, and Metabolism of Zongertinib, a Novel HER2-Selective Tyrosine Kinase Inhibitor, in Rat by Liquid Chromatography Hyphenated With Electrospray Ionization Tandem Mass Spectrometry. [Abstract]

2026 May;40(5):e70434. PMID: 41886811
J Orthop Sci

BTK as a novel diagnostic biomarker and therapeutic target in osteosarcoma. [Abstract]

2026 Mar 29:S0949-2658(26)00083-7. PMID: 41912366
Biomed Chromatogr

A Simple and Sensitive LC-MS/MS Method for the Determination of Mobocertinib and Its Metabolite Desmethyl-Mobocertinib in Human Plasma and Its Application to Clinical Pharmacokinetic Study. [Abstract]

2025 Feb;39(2):e6063. PMID: 39748454
Biomed Chromatogr

A rapid UHPLC-MS/MS method for the quantification of ARQ531 in rat plasma: Validation and its application to a pharmacokinetic study. [Abstract]

2020 Nov;34(11):e4937. PMID: 32614971
Res Sq

2026 Apr 27.
bioRxiv

2026 Mar 6.
Jagiellonian University

2026.
bioRxiv

2025 Nov 13.
bioRxiv

2025 Sep 21.
bioRxiv

COOKIE-Pro: Covalent Inhibitor Binding Kinetics Profiling on the Proteome Scale. [Abstract]

2025 Jun 22:2025.06.19.660637. PMID: 40666940
Authorea

2025 Feb 13.
bioRxiv

2024 September 08.
bioRxiv

Rebalancing Viral and Immune Damage versus Tissue Repair Prevents Death from Lethal Influenza Infection. [Abstract]

2024 Jul 7:2024.07.04.601620. PMID: 39372755
Research Square Preprint

2023 Oct 13.
Research Square Preprint

2023 Oct 16.
The Ohio State University

2023 Sep.
SSRN

2023 Aug 15.
Oncotarget

LP-284, a small molecule acylfulvene, exerts potent antitumor activity in preclinical non-Hodgkin's lymphoma models and in cells deficient in DNA damage repair. [Abstract]

2023 Jun 12:14:597-611. PMID: 37306526
bioRxiv

2023 Feb 24.
Research Square Print

August 25th, 2022
Patent

US20220202794A1.
Patent

US20200199683A1
University of Pennsylvania

2020 Feb.
bioRxiv

2019 Nov.
Charles University

2019 Jun.
Patent

US20190040013A1.
Patent

US20170333436A1.
Patent

US20170128439A1.
Oncotarget

Ibrutinib targets mutant-EGFR kinase with a distinct binding conformation. [Abstract]

2016 Oct 25;7(43):69760-69769. PMID: 27626175

Ibrutinib purchased from MedChemExpress. Usage Cited in: Oncotarget. 2016 Oct 25;7(43):69760-69769. [Abstract]

Ibrutinib and WZ4002 inhibitory effects on EGFRY1068 auto-phosphorylation in the H1975 cell line at different time points by removal of drug after 4 h pretreatment
Patent

US20160222465A1.

Ibrutinib purchased from MedChemExpress. Usage Cited in: Patent. US20160222465A1.

Impact of Ibrutinib on p-AKT, ERK and BTK expression following SDF-1a stimulation of plenti-GFP vector, CXCR4^WT and CXCR4^S338X expressing BCWM.1 cells.
Oncotarget

Ibrutinib selectively and irreversibly targets EGFR (L858R, Del19) mutant but is moderately resistant to EGFR (T790M) mutant NSCLC Cells. [Abstract]

2015 Oct 13;6(31):31313-22. PMID: 26375053

Ibrutinib purchased from MedChemExpress. Usage Cited in: Oncotarget. 2015 Oct 13;6(31):31313-22. [Abstract]

Effect of Ibrutinib on EGFR wt/mutant NSCLCs. Ibrutinib effects on wt EGFR and mutant EGFR- mediated signaling pathways. The results demonstrate that Ibrutinib potently inhibits both EGFR wt/mutant auto-phosphorylation at Y1068.

Ibrutinib purchased from MedChemExpress. Usage Cited in: Oncotarget. 2015 Oct 13;6(31):31313-22. [Abstract]

Effect of Ibrutinib, WZ4002, AZD9291 and CO1686 on EGFR phosphorylation of tyrosines 1068 and 1173 in EGFR-dependent cancer cell lines.
The Pennsylvania State University

2015 Jul.

Ibrutinib purchased from MedChemExpress. Usage Cited in: The Pennsylvania State University. 2015 Jul.

JVM-3 cells are treated with BTK inhibitor, Ibrutinib for 6 hours and Western blotting is performed to determine protein levels.

Solvant et solubilité

In Vitro:

DMSO : 100 mg/mL (227.01 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.2701 mL

11.3507 mL

22.7015 mL

5 mM

0.4540 mL

2.2701 mL

4.5403 mL

10 mM

0.2270 mL

1.1351 mL

2.2701 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.75 mg/mL (6.24 mM); Clear solution

Protocol 2

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (5.68 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 3

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 2.5 mg/mL (5.68 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 4

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.68 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 0.5% Methyl cellulose/0.5% Tween-80 in Saline water

Solubility: 3.33 mg/mL (7.56 mM); Suspension solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protocole

Cell Assay^[3]

Primary human B cells are isolated from peripheral blood mononuclear cell using human Miltenyl human B cell Isolation Kit II. In 0.2 mL RPMI plus 10% FBS, 100,000 B cells are treated with Ibrutinib (PCI-32765) (0.3 nM-10 μM) in triplicate wells or vehicle control in 0.1% DMSO final concentration for 30 minutes at 37°C, 5% CO₂, then cells are stimulated with 10 μg/mL anti-IgM F(ab')₂, 5 μg/mL anti-CD3/CD28 as a negative control or 0.5 μg/mL PMA (Phorbal 12-myristate 13-acetate) as a positive control. B cells are stimulated for 72 hours at 37°C, 5% CO₂. Proliferation is measured with Cell Titer Glo reagent and measured on a luminometer.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[3]

Male DBA1/1OlaHsd mice are injected on days 0 and 21 with Freunds' Complete Adjuvant containing bovine type II collagen. On days 21 to 35, mice are randomized into treatment groups when the average clinical score of each animal is 1.5 (in a scale of 5). Ibrutinib (PCI-32765) treatment (1.56-12.5 mg/kg, p.o.) is initiated following enrollment and continues for 18 days. Clinical scores are given to each mouse daily for each paw. Clinical score assessment is made using the following criteria: 0=normal; 1=one hind paw or fore paw joint affected or minimal diffuse erythema and swelling; 2=two hind or fore paw joints affected or mild diffuse erythema and swelling; 3=three hind or fore paw joints affected or moderate diffuse erythema and swelling; 4=marked diffuse erythema and swelling or four digit joints affected; 5=severe diffuse erythema and severe swelling of entire paw, unable to flex digits.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (285 KB)
SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Honigberg LA, et al. The Bruton tyrosine kinase inhibitor PCI-32765 blocks B-cell activation and is efficacious in models of autoimmune disease and B-cell malignancy. Proc Natl Acad Sci U S A. 2010 Jul 20;107(29):13075-80. [Content Brief]

[2]. Herman SE, et al. Bruton tyrosine kinase represents a promising therapeutic target for treatment of chronic lymphocytic leukemia and is effectively targeted by PCI-32765. Blood. 2011 Jun 9;117(23):6287-96. [Content Brief]

[3]. Chang BY, et al. The Bruton tyrosine kinase inhibitor PCI-32765 ameliorates autoimmune arthritis by inhibition of multiple effector cells. Arthritis Res Ther. 2011 Jul 13;13(4):R115. [Content Brief]

[4]. Sun Y, et al. PROTAC-induced BTK degradation as a novel therapy for mutated BTK C481S induced ibrutinib-resistant B-cell malignancies. Cell Res. 2018 Jul;28(7):779-781. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.2701 mL	11.3507 mL	22.7015 mL	56.7537 mL
	5 mM	0.4540 mL	2.2701 mL	4.5403 mL	11.3507 mL
	10 mM	0.2270 mL	1.1351 mL	2.2701 mL	5.6754 mL
	15 mM	0.1513 mL	0.7567 mL	1.5134 mL	3.7836 mL
	20 mM	0.1135 mL	0.5675 mL	1.1351 mL	2.8377 mL
	25 mM	0.0908 mL	0.4540 mL	0.9081 mL	2.2701 mL
	30 mM	0.0757 mL	0.3784 mL	0.7567 mL	1.8918 mL
	40 mM	0.0568 mL	0.2838 mL	0.5675 mL	1.4188 mL
	50 mM	0.0454 mL	0.2270 mL	0.4540 mL	1.1351 mL
	60 mM	0.0378 mL	0.1892 mL	0.3784 mL	0.9459 mL
	80 mM	0.0284 mL	0.1419 mL	0.2838 mL	0.7094 mL
	100 mM	0.0227 mL	0.1135 mL	0.2270 mL	0.5675 mL

Keywords

Ibrutinib

136 Cited Publications

100 mg Obtenir un devis

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Ibrutinib

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Publications Citing Use of MedChemExpress (MCE) Ibrutinib

Activité biologique

Chemical Information

Publications (136)

Solvant et solubilité

Protocole

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Ibrutinib Related Classifications

HY-10997 Related Classifications