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Ibrutinib

Chemical Structure : Ibrutinib

CAS No.: 936563-96-1

Ibrutinib (PCI-32765, PCI32765, PCI 32765)

Catalog No.: PC-42772Not For Human Use, Lab Use Only.

Ibrutinib (PCI-32765, PCI32765) is a potent and highly selective, covalent BTK inhibitor with IC50 of 0.5 nM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Ibrutinib (PCI-32765, PCI32765) is a potent and highly selective, covalent BTK inhibitor with IC50 of 0.5 nM.
Ibrutinib modestly potent to Bmx, CSK, FGR, BRK, HCK, less potent to EGFR, Yes, ErbB2, JAK3, etc.
Ibrutinib (PCI-32765) selectively inhibits B-cell signaling and activation. It inhibits autophosphorylation of Btk (IC50=11 nM), phosphorylation of Btk's physiological substrate PLCγ (IC50=29 nM).
Ibrutinib (PCI-32765) inhibits BCR-activated primary B cell proliferation (IC50=8 nM).
Following FcγR stimulation, Ibrutinib (PCI-32765) inhibits TNFα, IL-1β and IL-6 production in primary monocytes (IC50=2.6, 0.5, 3.9 nM, respectively).
Ibrutinib (PCI-32765) (3.125-50 mg/kg, p.o.) reduces the level of circulating autoantibodies and completely suppresses disease in mice with collagen-induced arthritis.
Ibrutinib (PCI-32765) (0.1 μM) inhibits activation-induced proliferation of CLL cells, induces selective cytotoxicity in B cells compared with T cells, but alters activation induced T-cell cytokine production.

Physicochemical Properties

M.Wt 440.4971
Formula C25H24N6O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: ≥ 52 mg/mL

Chemical Name/SMILES

2-Propen-1-one, 1-[(3R)-3-[4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl]-1-piperidinyl]-

References

1. Honigberg LA, et al. Proc Natl Acad Sci U S A. 2010 Jul 20;107(29):13075-80.

2. Herman SE, et al. Blood. 2014 May 22;123(21):3286-95.

3. Kohrt HE, et al. Blood. 2014 Mar 20;123(12):1957-60.

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