Ibrutinib

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

Product Specifications

CAS Number

[936563-96-1]

Product Name Alternative

PCI-32765

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Btk; Ligands for Target Protein for PROTAC

Type

Reference compound

Related Pathways

PROTAC; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/PCI-32765.html

Purity

99.97

Solubility

DMSO : 100 mg/mL (ultrasonic)

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

Molecular Formula

C25H24N6O2

Molecular Weight

440.50

Precautions

H302, H315, H319, H335

References & Citations

[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]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.|[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.|[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.