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AJL0780A

Ibrutinib

Pharmaceutical Grade
  • CAS Number 936563-96-1
  • Molecular Formula C25H24N6O2
  • Molecular Weight 440.50
  • Function: Ibrutinib
  • Application: For research use only
  • Negotiable/1 Kg/Bag
    Tel:
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    Summary

      Ibrutinib is a potent and highly selective Brutons tyrosine kinase (Btk) inhibitor with IC50 of 0.5 nM in cell-free assays, modestly potent to Bmx, CSK, FGR, BRK, HCK, less potent to EGFR, Yes, ErbB2, JAK3, etc.

      Ibrutinib shows the potent and irreversible inhibitory effect and selectivity for Btk enzymatic activity. In BCR pathway-activated DOHH2 cell line, Ibrutinib inhibits autophosphorylation of Btk, phosphorylation of Btk's physiological substrate PLCγ, and phosphorylation of further downstream kinase, ERK with IC50 of 11 nM, 29 nM and 13 nM, respectively. Ibrutinib exhibits a significant dose-dependent and time-dependent induction of cytotoxicity in chronic lymphocytic leukemia (CLL) cells. In addition, Ibrutinib induces cell death depending on caspase pathway activation and antagonizes the ability of CLL cells to proliferate after TLR signaling. A recent study shows that Ibrutinib inhibits BCR-activated primary B cell proliferation with IC50 of 8 nM and results in inhibition of TNFα, IL-1β and IL-6 production in primary monocytes with IC50 of 2.6 nM, 0.5 nM and 3.9 nM, respectively.
      In a collagen-induced arthritis model, Ibrutinib significantly reduces clinical arthritis scores reflecting paw swelling and joint inflammation by inhibiting B-cell activation. In a MRL-Fas(lpr) lupus model, Ibrutinib reduces renal disease and autoantibody production. In an adoptive transfer TCL1 mouse model of CLL, Ibrutinib (25 mg/kg/day) causes a transient early lymphocytosis, and delays CLL disease progression.
      Seebio also can supply Ibrutinib Intermedites as below:

      CODE PRODUCT NAME CAS NO. USAGE
      AJL0781A
      (S)-1-Boc-3-hydroxypiperidine 143900-44-1 Ibrutinib
      AJL0782A
      3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine 330786-24-8 Ibrutinib

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    Properties

      Physical and chemical properties

      Molecular Formula:

      C25H24N6O2

      Molecular Weight: 440.5
      CAS No.: 936563-96-1
      Stability:
      3 years -20°C Powder
      6 months -80°C in DMSO
      Molecular Structure:

      Analytical data

      HPLC: ≥99% purity
      NMR: Consistent with structure

    Product Detail