Ibrutinib

Ibrutinib

• CAS Number: 936563-96-1
• 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