Home Tools

Cart

Ibrutinib

Catalog No. T1835 CAS 936563-96-1

Synonyms: PCI-32765

Ibrutinib (PCI-32765) is an irreversible inhibitor of BTK (IC50: 0.5 nM) that selectively blocks B cell activation.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

Ibrutinib, CAS 936563-96-1

Pack Size	Availability	Price/USD
5 mg	In stock	$ 36.00
10 mg	In stock	$ 46.00
50 mg	In stock	$ 57.00
100 mg	In stock	$ 72.00
200 mg	In stock	$ 93.00
1 mL * 10 mM (in DMSO)	In stock	$ 46.00

Bulk Inquiry

Select Batch

Purity: 99.79%

Purity: 99.76%

Purity: 99.71%

Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Ibrutinib (PCI-32765) is an irreversible inhibitor of BTK (IC50: 0.5 nM) that selectively blocks B cell activation.
Targets&IC50	FGR:2.3 nM (cell free), BLK:0.5 nM (cell free), Brk:3.3 nM (cell free), BTK:0.5 nM (cell free), BMX:0.8 nM (cell free), CSK:2.3 nM (cell free)
In vitro	In DOHH2, a cell line in which the BCR pathway can be activated by stimulation with anti-IgG, Ibrutinib (PCI-32765) 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). Continuous exposure to 10 nM PCI-32765 for 18 h completely prevented up-regulation of the B-cell activation marker CD69. A 1-h pulse exposure to 10 nM PCI-32765 resulted in a similar level of CD69 inhibition in B cells [1]. PCI-32765 inhibited BCR-activated primary B cell proliferation (IC50: 8 nM). Following FcγR stimulation, PCI-32765 inhibited TNFα, IL-1β and IL-6 production in primary monocytes (IC50s: 2.6/0.5/3.9 nM). Following FcεRI stimulation of cultured human mast cells, PCI-32765 inhibited release of histamine, PGD(2), TNF-α, IL-8, and MCP-1 [2]. Treatment of CD40 or BCR activated CLL cells with PCI-32765 results in inhibition of BTK tyrosine phosphorylation and also effectively abrogates downstream survival pathways activated by this kinase including ERK1/2, PI3K, and NF-κB. In addition, PCI-32765 inhibits activation-induced proliferation of CLL cells in vitro and effectively blocks survival signals provided externally to CLL cells from the microenvironment [3].
In vivo	PCI-32765 (3.125, 12.5, or 50 mg/kg per day) markedly inhibited clinical arthritis scores. Partial and nearly complete elimination of clinical signs of the disease occurred after 9 to 11 d of treatment at dosages of 3.125 and 12.5 mg/kg per day, respectively. An oral single dose of PCI-32765 at 3.125 mg/kg per day resulted in partial Btk occupancy in splenocytes, and the maximally efficacious dose (12.5 mg/kg per day) was sufficient to fully occupy Btk for 12 h [1]. PCI-32765 dose-dependently and potently reversed arthritic inflammation in a therapeutic CIA model (ED50: 2.6 mg/kg/day). PCI-32765 also prevented clinical arthritis in CAIA models. In both models, infiltration of monocytes and macrophages into the synovium was completely inhibited [2].
Kinase Assay	In vitro kinase IC50s were measured using 33P filtration binding assay after 1 h incubation of kinase, 33P-ATP, inhibitor, and substrate [0.2 mg/mL poly(EY)(4:1]. Assays were performed at Reaction Biology [1].
Cell Research	CD20+ B and CD3+ T cells were purified by negative selection (RosetteSep, >90% purity) from buffy coat PBMCs and viably frozen in 10% DMSO. Cells were thawed at 37 °C and maintained in growth media (RPMI media containing 10% FCS). B cells were stimulated with goat anti-human IgM F(ab′)2 (10 μg/mL) and T cells were stimulated with anti-CD3/CD28 coated beads at a 1:1 bead/cell ratio. Cells were stained with PE-CD69 and analyzed by flow cytometry, gating on viable lymphocytes. PCI-32765 at concentrations lower than 10 μM did not decrease B- or T-cell viability during the course of the experiment, although PCI-32765 did block the modest survival benefit of anti-IgM stimulation in B cells. For washout experiments, cells were rinsed three times in 10 volumes of growth media, a protocol that was confirmed to completely wash away inhibition of BCR signaling by PCI-29732, a reversible Btk inhibitor [1].
Animal Research	ale DBA/1 mice were immunized with type II collagen plus Freund adjuvant and boosted 21 d later. On a rolling basis, as significant swelling appeared in at least one paw, mice were enrolled and randomized. PCI-32765 or dexamethasone (0.2 mg/kg) was administered orally once per day for 11 d. Arthritis scores (0–5) were assigned to the mice based on the degree and extent of paw swelling. Mouse anti-type II collagen antibody and total IgG levels were measured by ELISA. Female MRL/MpJ-Faslpr mice received PCI-32765 by oral gavage once per day from week 8 through week 20. Proteinuria was monitored weekly. At week 20, serum was collected and analyzed for BUN and mouse anti-dsDNA antibody levels. Kidney histology was scored according to established criteria (26). No drug-induced weight loss was observed at any of the dose levels tested. These studies were carried out at Boulder Biopath according to approved animal care protocols. Results are presented as the mean ± SEM. Statistical significance between groups were evaluated with repeated measures one-way ANOVA or one-way ANOVA using GraphPad Prism with Tukey or Bonferroni multicomparison posttest [1].

Synonyms	PCI-32765
Molecular Weight	440.5
Formula	C25H24N6O2
CAS No.	936563-96-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 82 mg/mL (186.2 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

References and Literature

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. 2. 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. 3. 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.

Citations

1. Guo W, Liang D, Wang P, et al. HIF-PH Encoded by EGLN1 Is a Potential Therapeutic Target for Chronic Lymphocytic Leukemia. Pharmaceuticals. 2022, 15(6): 734 2. Huang F, Liang J, Lin Y, et al.Repurposing of Ibrutinib and Quizartinib as potent inhibitors of necroptosis.Communications Biology.2023, 6(1): 972. 3. Zhang Z, Zhou H, Gu W, et al.CGI1746 targets σ1R to modulate ferroptosis through mitochondria-associated membranes.Nature Chemical Biology.2024: 1-11.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Active Compound Library Anti-Cancer Approved Drug Library FDA-Approved Kinase Inhibitor Library Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Tyrosine Kinase Inhibitor Library Drug Repurposing Compound Library Highly Selective Inhibitor Library Kinase Inhibitor Library EMA Approved Drug Library

Related Products

Related compounds with same targets

Decernotinib Ginsenoside Ra1 GTP-14564 ST271 NVP-AEW541 Paltimatrectinib BMS-911543 Oclacitinib maleate

Dose Conversion

You can also refer to dose conversion for different animals. More

In vivo Formulation Calculator (Clear solution)

Step One: Enter information below

Dosage

mg/kg

Average weight of animals

Dosing volume per animal

Number of animals

Step Two: Enter the in vivo formulation

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

Calculate Reset

Calculation results:

Working concentration: mg/ml;

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

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

Note:

Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Calculator

Molarity Calculator

Dilution Calculator

Reconstitution Calculation

Molecular Weight Calculator

Mass

Concentration

Volume

Molecular Weight

Molarity Calculator allows you to calculate the

Mass of a compound required to prepare a solution of known volume and concentration
Volume of solution required to dissolve a compound of known mass to a desired concentration
Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of a molarity calculation using the molarity calculator
What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
Enter 197.13 into the Molecular Weight (MW) box
Enter 10 into the Concentration box and select the correct unit (millimolar)
Enter 10 into the Volume box and select the correct unit (milliliter)
Press calculate
The answer of 19.713 mg appears in the Mass box

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

Calculator the dilution required to prepare a stock solution

Calculate the dilution required to prepare a stock solution
The dilution calculator is a useful tool which allows you to calculate how to dilute a stock solution of known concentration. Enter C1, C2 & V2 to calculate V1.

See Example

An example of a dilution calculation using the Tocris dilution calculator
What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=50 μM, V2=20 ml and V1 is the unknown:
Enter 10 into the Concentration (start) box and select the correct unit (millimolar)
Enter 50 into the Concentration (final) box and select the correct unit (micromolar)
Enter 20 into the Volume (final) box and select the correct unit (milliliter)
Press calculate
The answer of 100 microliter (0.1 ml) appears in the Volume (start) box

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

Calculate the volume of solvent required to reconstitute your vial.

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial.
Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

Molecule Formula

Molecular Weight g/mol

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

Tip: Chemical formula is case sensitive: C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed n the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

bottom

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Ibrutinib 936563-96-1 Angiogenesis PROTAC Tyrosine Kinase/Adaptors Tyrosine Kinases Src BTK Ligands for Target Protein for PROTAC inhibit PCI 32765 Target Protein-binding Moiety PCI32765 Inhibitor Btk Bruton tyrosine kinase PCI-32765 inhibitor

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.