Cas No.: | 1351635-67-0 |
Chemical Name: | ONO4059-Analog |
Synonyms: | ON 0459 analog,ON-0459 analog |
SMILES: | O=C1N([C@H]2CCCN(C(C=C)=O)C2)C3=NC=NC(N)=C3N1C4=CC=C(OC5=CC=CC=C5)C=C4 |
Formula: | C25H24N6O3 |
M.Wt: | 456.506 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | The product is the analog of ONO-4059, ONO-4059 is a highly potent and selective Btk inhibitor with an IC50 in the sub-nM range. |
Target: | IC50 value: sub-nM range [2] Target: Btk |
In Vivo: | ONO-4059 (analog) has demonstrated anti-tumour activity in several pre-clinical models.[1] ONO-4059 (analog) potently and dose-dependently reverse clinical arthritis and prevented bone damage in the CIA model.[2] |
In Vitro: | ONO-4059 ( analog ) 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 (analog) shows a favourable safety profile along with promising efficacy in this difficult-to-treat patient population. [1] |
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 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. |