Product Name:
ONO-4059CAS No.:
1351635-67-0
Product Data Sheet
Cat. No.:
HY-18951MWt:
456.50Formula:
C25H24N6O3Purity :
>98%
Solubility:Mechanisms:
Biological Activity:
Pathways:Protein Tyrosine Kinase/RTK; Target:Btk
20 mg/ml in DMSO
g y ONO-4059 is a highly potent and selective Btk inhibitor with an IC50 in the sub-nM range.
IC50 value: sub-nM range [2]
Target: Btk in vitro: ONO-4059 is a selective, once-daily, oral inhibitor of BTK, which has been shown to play a role in the survival and proliferation of malignant B-cells. ONO-4059 shows a favourable safety
profile along with promising efficacy in this difficult-to-treat patient population. [1]in vivo: ONO-4059 has demonstrated anti-tumour activity in several pre-clinical models.[1] ONO-4059 potently and dose-dependently reverse clinical arthritis and prevented bone damage in the CIA References:
[1]. Simon Rule,A Phase I Study Of The Oral Btk Inhibitor ONO-4059 In Patients With
Relapsed/Refractory B-Cell Lymphoma. November 15, 2013; Blood: 122 (21)[2]. Toshio Yoshizawa, et al. Development of a Bruton's Tyrosine Kinase (Btk) Inhibitor, ONO-4059:Efficacy in a Collagen Induced Arthritis (CIA) Model Indicates Potential Treatment for Rheumatoid p y p y p g model.[2]...
y g ()
Arthritis (RA). Washington, DC November 9-14, 2012.[3]. Yamamoto, et al. Preparation of purinone derivatives as selective Btk inhibitors. From PCT Int.
Appl. (2011), WO 2011152351 A1 20111208.Caution: Not fully tested. For research purposes only
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