ONO-4059 analog

• CAT Number: I001351
• CAS Number: 1351635-67-0
• Molecular Formula: C₂₅H₂₄N₆O₃
• Molecular Weight: 456.51
• Purity: ≥95%
• Target: BTK
• Solubility: DMSO: ≥ 30 mg/mL
• Storage: Store at -20°C
• IC50: sub-nM range [2]
• IUPAC Name: 6-amino-7-(4-phenoxyphenyl)-9-[(3S)-1-prop-2-enoylpiperidin-3-yl]purin-8-one
• InChI: InChI=1S/C25H24N6O3/c1-2-21(32)29-14-6-7-18(15-29)31-24-22(23(26)27-16-28-24)30(25(31)33)17-10-12-20(13-11-17)34-19-8-4-3-5-9-19/h2-5,8-13,16,18H,1,6-7,14-15H2,(H2,26,27,28)/t18-/m0/s1
• InChIKey: KSUDUUBCXJUFRL-SFHVURJKSA-N
• SMILES: C=CC(=O)N1CCCC(C1)N2C3=NC=NC(=C3N(C2=O)C4=CC=C(C=C4)OC5=CC=CC=C5)N

ONO-WG-307 is an analog of ONO-4059（Cat No.:I001351）, a highly potent and selective oral inhibitor of Bruton’s tyrosine kinase (BTK). It exhibits an inhibitory concentration (IC50) of 23.9 nM, indicating its strong inhibitory activity against BTK. By specifically targeting BTK, ONO-WG-307 interferes with B-cell receptor signaling, which plays a critical role in the development and progression of various B-cell malignancies.

Reference

[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.