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ONO-4059 (analog)

Names

[ CAS No. ]:
1351635-67-0

[ Name ]:
ONO-4059 (analog)

[Synonym ]:
9-[(3S)-1-Acryloyl-3-piperidinyl]-6-amino-7-(4-phenoxyphenyl)-7,9-dihydro-8H-purin-8-one
8H-Purin-8-one, 6-amino-7,9-dihydro-9-[(3S)-1-(1-oxo-2-propen-1-yl)-3-piperidinyl]-7-(4-phenoxyphenyl)-
ONO-4059
ONO4059 analog
ONO-4059 (analog)

Biological Activity

[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. IC50 value: sub-nM range [2]Target: Btkin 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]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]

[Related Catalog]:

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> Btk
Research Areas >> Cancer

[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.


[Related Small Molecules]

Acalabrutinib | GDC-0853 | Evobrutinib | AVL-292 | (±)-Zanubrutinib | ONO-4059 | BMX-IN-1 | GDC-0834 | SNS-062 | RN486 | LFM-A13 | Vecabrutinib | CGI-1746 | BMS-986195 | CNX-774

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Boiling Point ]:
714.0±70.0 °C at 760 mmHg

[ Molecular Formula ]:
C25H24N6O3

[ Molecular Weight ]:
456.496

[ Flash Point ]:
385.6±35.7 °C

[ Exact Mass ]:
456.190979

[ LogP ]:
1.82

[ Vapour Pressure ]:
0.0±2.3 mmHg at 25°C

[ Index of Refraction ]:
1.677

[ Storage condition ]:
-20℃

Safety Information

[ Hazard Codes ]:
N

Related Compounds