PCI 29732

PCI 29732 is a potent, orally active, reversible BTK inhibitor with Kiapp values of 8.2, 4.6, and 2.5 nM for BTK, Lck and Lyn, respectively. PCI 29732 shows only modest inhibitory activity against Itk, another Tec family kinase. PCI 29732 inhibits the function of ABCG2 by competitively binding to the ATP-binding site of ABCG2[1][2].

Product Specifications

CAS Number

[330786-25-9]

UNSPSC

12352005

Hazard Statement

H302-H315-H319-H335

Target

BCRP; Btk

Type

Reference compound

Related Pathways

Membrane Transporter/Ion Channel; Protein Tyrosine Kinase/RTK

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/PCI-29732.html

Purity

99.86

Solubility

DMSO : ≥ 53 mg/mL|Ethanol : 10 mg/mL (ultrasonic)

Smiles

NC1=NC=NC2=C1C(C3=CC=C(OC4=CC=CC=C4)C=C3)=NN2C5CCCC5

Molecular Formula

C22H21N5O

Molecular Weight

371.44

Precautions

P261-P264-P270-P271-P280-P302+P352-P304+P340-P305+P351+P338-P330-P362+P364-P403+P233-P405-P501

References & Citations

[1]Pan Z, et al. Discovery of selective irreversible inhibitors for Bruton's tyrosine kinase. ChemMedChem. 2007 Jan;2 (1) :58-61.|[2]Ge C, et al. PCI29732, a Bruton's Tyrosine Kinase Inhibitor, Enhanced the Efficacy of Conventional Chemotherapeutic Agents in ABCG2-Overexpressing Cancer Cells. Cell Physiol Biochem. 2018;48 (6) :2302-2317.|[3]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;107 (29) :13075-13080.