Ibrutinib [936563-96-1]

Catalog number: HY-10997_100mg
Brand: MedChem Express
Packing: 100 mg
Other sizes: Also available in other sizes.
Price: € 139.00
Expected delivery time: 10 days

Product specifications for - Ibrutinib [936563-96-1]

Product group: Chemicals
Category: Other
CAS No.: 936563-96-1
Purity: >98%
Molecular Formula: C25H24N6O2
Molecular weight: 440.50
Datasheet: Datasheet
  Research Use Only
UNSPSC: 12352200
Scientific information: 
Scientific info: PCI-32765(Ibrutinib) 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 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 PLCgamma, 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) cells. In addition, Ibrutinib induces cell death depending on caspase pathway activation and antagonizes the ability of CLL cells to proliferate after TLR signaling [2]. A recent study shows that Ibrutinib inhibits BCR-activated primary B cell proliferation with IC50 of 8 nM and results in inhibition of TNFalpha, IL-1beta and IL-6 production in primary monocytes with IC50 of 2.6 nM, 0.5 nM and 3.9 nM, respectively [3]. in vivo: 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 [1]. In an adoptive transfer TCL1 mouse model of CLL, Ibrutinib (25 mg/kg/day) causes a transient early lymphocytosis, and delays CLL disease progression [4].
Safety information: 
HCK AS A THERAPEUTIC TARGET IN MYD88 MUTATED DISEASES', Treon, Steven P. Patent. US 20170333436A1. Read more
Methods for evaluating and treating waldenstrom's macroglobulinemia', Steven P. Treon. Patent. US 20160222465 A1. Read more
HCK is a survival determinant transactivated by mutated MYD88, and a direct target of ibrutinib.', Yang G. Blood. 2016 Jun 23;127(25):3237-52. Read more
High expression of Bruton’s tyrosine kinase (BTK) is required for EGFR-induced NF-κB activation and predicts poor prognosis in human glioma', Yue C. J Exp Clin Cancer Res. 2017 Sep 25;36(1):132. Read more
STAT3 mediates C6-ceramide-induced cell death in chronic lymphocytic leukemia', Ushma A Doshi. Signal Transduct Target Ther. 2017 Oct 27;2:17051. Read more