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Chemical Structure
Chemical Structure
Chemical Structure

Ibrutinib [936563-96-1]

Research Use Only
AG-CR1-3620
AdipoGen Life Sciences
CAS Number936563-96-1
Product group Chemicals
Estimated Purity>98%
Molecular Weight440.5
Price on request
Packing Size
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Overview

  • Supplier
    AdipoGen Life Sciences
  • Product Name
    Ibrutinib [936563-96-1]
  • Delivery Days Customer
    10
  • CAS Number
    936563-96-1
  • Certification
    Research Use Only
  • Estimated Purity
    >98%
  • Hazard Information
    Danger
  • Molecular Formula
    C25H24N6O2
  • Molecular Weight
    440.5
  • Scientific Description
    Chemical. 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).
  • SMILES
    NC1=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
  • UNSPSC
    12352200

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)