Home Protein Tyrosine Kinase BTK inhibitor PCI 29732 For research use only.

PCI 29732

PCI 29732 is a selective and irreversible Btk inhibitor with an IC50 of 0.5 nM.

PCI 29732 Chemical Structure

PCI 29732 Chemical Structure

CAS: 330786-25-9

Purity & Quality Control

Batch: S672501 DMSO] 74 mg/mL] false] Ethanol] 4 mg/mL] false] Water] Insoluble] false Purity: 99.91%
99.91

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Signaling Pathway

BTK Signaling Pathways

BTK Signaling Pathway

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Biological Activity

Description PCI 29732 is a selective and irreversible Btk inhibitor with an IC50 of 0.5 nM.
Targets
BTK [1]
(Cell-free assay)		 BLK [1]
(Cell-free assay)		 Bmx [1]
(Cell-free assay)		 EGFR [1]
(Cell-free assay)		 YES [1]
(Cell-free assay)		 Click to View More Targets
0.5 nM 0.5 nM 0.8 nM 5.6 nM 6.5 nM
In vitro
In vitro

PCI-32765 blocks BCR signaling in human peripheral B cells at concentrations that does not affect T cell receptor signaling. In DOHH2 cells, 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). PCI-32765 is more than 1,000-fold selective for inhibition of antigen receptor signaling in B cells over T cells, and that only B-cell inhibition is sustained following short duration treatment[1].
In Vivo
In vivo

In mice with collagen-induced arthritis, orally administered PCI-32765 reduces the level of circulating autoantibodies and completely suppresses disease. PCI-32765 also inhibits autoantibody production and the development of kidney disease in the MRL-Fas(lpr) lupus model. The mean terminal plasma half-life of PCI-32765 following oral dosing in mice is 1.7 to 3.1 h[1].
Animal Research Animal Models Arthritic DBA/1 mice
Dosages 3.125, 12.5, or 50 mg/kg per day
Administration oral

Chemical Information & Solubility

Molecular Weight 371.43 Formula

C22H21N5O
CAS No. 330786-25-9 SDF --
Smiles C1CCC(C1)N2C3=NC=NC(=C3C(=N2)C4=CC=C(C=C4)OC5=CC=CC=C5)N
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 74 mg/mL ( (199.23 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 4 mg/mL

Water : Insoluble


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

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

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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