Chemical Structure
Ibrutinib [936563-96-1]
AG-CR1-3620
Overview
- SupplierAdipoGen Life Sciences
- Product NameIbrutinib [936563-96-1]
- Delivery Days Customer10
- CAS Number936563-96-1
- CertificationResearch Use Only
- Estimated Purity>98%
- Hazard InformationDanger
- Molecular FormulaC25H24N6O2
- Molecular Weight440.5
- Scientific DescriptionChemical. CAS: 936563-96-1. Formula: C25H24N6O2. MW: 440.5. Potent and highly selective Brutons tyrosine kinase (BTK) inhibitor. Orally bioavailable and irreversible inhibitor of BTK (IC50 = 0.5 nM) with antineoplastic activity. Binds to and irreversibly inhibits BTK activity, preventing B cell activation and B cell-mediated signaling. This leads to an inhibition of the growth of malignant B cells that overexpress BTK. Shown to inhibit autophosphorylation of BTK (IC50 = 11nM), phosphorylation of PLCgamma (IC50 = 29nM), a substrate of BTK and phosphorylation of ERK (IC50 = 13nM). - Potent and highly selective Brutons tyrosine kinase (BTK) inhibitor. Orally bioavailable and irreversible inhibitor of BTK (IC50 = 0.5 nM) with antineoplastic activity. Binds to and irreversibly inhibits BTK activity, preventing B cell activation and B cell-mediated signaling. This leads to an inhibition of the growth of malignant B cells that overexpress BTK. Shown to inhibit autophosphorylation of BTK (IC50 = 11nM), phosphorylation of PLCgamma (IC50 = 29nM), a substrate of BTK and phosphorylation of ERK (IC50 = 13nM).
- SMILESNC1=C2C(=NC=N1)N(N=C2C1=CC=C(OC2=CC=CC=C2)C=C1)C1CCCN(C1)C(=O)C=C
- Storage Instruction-20°C,2°C to 8°C
- UNSPSC12352200
References
- The Bruton tyrosine kinase inhibitor PCI-32765 blocks B-cell activation and is efficacious in models of autoimmune disease and B-cell malignancy: L.A. Honigberg, et al.; PNAS 107, 13075 (2010)
- BTK inhibitor ibrutinib is cytotoxic to myeloma and potently enhances bortezomib and lenalidomide activities through NF-kappaB: S.A. Rushworth, et al.; Cell Signal. 25, 106 (2013)
- In vitro, in vivo and ex vivo characterization of ibrutinib: a potent inhibitor of the efflux function of the transporter MRP1: H. Zhang, et al.; Br. J. Pharmacol. 171, 5845 (2014)
- Ibrutinib: a first in class covalent inhibitor of Bruton's tyrosine kinase: M.S. Davids & J.R. Brown; Future Oncol. 10, 957 (2014) (Review)