PCI-32765 Racemate_936563-87-0_DataSheet_MedChemExpress

Product Name:

PCI-32765 Racemate CAS No.:

936563-87-0Cat. No.:

HY-10997A

Product Data Sheet

MWt:

440.50Formula:

C25H24N6O2Purity :>98%

Solubility:

DMSO

y Mechanisms:

Biological Activity:

PCI 32765(Ibrutinib)racemate is a potent and highly selective Btk inhibitor with IC50of 05nM Pathways:Protein Tyrosine Kinase/RTK; Target:Btk PCI-32765(Ibrutinib) racemate is a potent and highly selective Btk inhibitor with IC50 of 0.5 nM, modestly potent to Bmx, CSK, FGR, BRK, HCK, less potent to EGFR, Yes, ErbB2, JAK3, etc.

IC50 value: 0.3 nM [1]

Target: Btk in vitro: 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 PLC γ, and phosphorylation of further downstream kinase, ERK with IC50 of 11 nM, 29 nM and 13 nM, respectively [1]. Ibrutinib exhibits a significant dose-dependent and time-dependent induction of cytotoxicity in chronic lymphocytic leukemia (CLL)References:

[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, 107(29), 13075-13080.p p y y y p y ()cells. In addition, Ibrutinib induces cell death depending on caspase pathway activation and antagonizes the ability of CLL cells to proliferate after TLR sign...

[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, 117(23),

6287-6296.[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, 13(4), R115.[4]. Ponader S, et al. The Bruton tyrosine kinase inhibitor PCI-32765 thwarts chronic lymphocytic leukemia cell survival and tissue homing in vitro and in vivo. Blood. 2012, 119(5), 1182-1189....

Caution: Not fully tested. For research purposes only

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