Ibrutinib

• UNSPSC Description:

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

• Target Antigen:

  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 Weight:

  440.50

• 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.

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

  4°C (Powder, protect from light)

• Clinical Information:

  Launched

• CAS Number:

  936563-96-1