Tirabrutinib (ONO-4059, GS-4059)

Tirabrutinib (ONO-4059, GS-4059)

$50.00$400.00

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$50.00$400.00

Tirabrutinib (ONO-4059, GS-4059) (CAS No.: 1351636-18-4), a selective and novel inhibitor of BTK with IC50 2.2 nM, Tirabrutinib binds to BTK within B cells, thereby preventing B-cell receptor signaling and impeding B-cell development. >98% Purity.

Synonyms: ONO-4059, GS-4059, BTK inhibitor, Bruton’s tyrosine kinase inhibitor

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Description

APIM050411: Tirabrutinib (ONO-4059, GS-4059) is a selective and novel inhibitor of BTK with IC50 2.2 nM, Tirabrutinib binds to BTK within B cells, thereby preventing B-cell receptor signaling and impeding B-cell development.

CAS No.: 1351636-18-4
IUPAC/Chemical Name: (R)-6-amino-9-(1-(but-2-ynoyl)pyrrolidin-3-yl)-7-(4-phenoxyphenyl)-7,9-dihydro-8H-purin-8-one
Molecular Formula: C25H22N6O3
Molecular Weight: 454.49
Purity: >98% Purity
QC: Achiral and Chiral HPLCs, MS, NMR, and Quantitative Elemental Analysis Report
Solubility: Soluble in DMSO
Storage: Dry, dark and at 0 – 4 C for short term (days to weeks) or -20 C for long term (months to years).
Note: Please contact us for COA, Spectra, and SDS information.

Background Information:

Tirabrutinib (ONO-4059, GS-4059) (CAS No. 1351636-18-4) is an orally administered, small molecule, Bruton’s tyrosine kinase (BTK) inhibitor being developed by Ono Pharmaceutical and its licensee Gilead Sciences for the treatment of autoimmune disorders and haematological malignancies. Tirabrutinib irreversibly and covalently binds to BTK in B cells and inhibits aberrant B cell receptor signalling in B cell-related cancers and autoimmune diseases. In March 2020, oral tirabrutinib was approved in Japan for the treatment of recurrent or refractory primary central nervous system lymphoma. Tirabrutinib is also under regulatory review in Japan for the treatment of Waldenström’s macroglobulinemia and lymphoplasmacytic lymphoma. Clinical development is underway in the USA, Europe and Japan for autoimmune disorders, chronic lymphocytic leukaemia, B cell lymphoma, Sjogren’s syndrome, pemphigus and rheumatoid arthritis. This article summarizes the milestones in the development of tirabrutinib leading to the first approval of tirabrutinib for the treatment of recurrent or refractory primary central nervous system lymphoma in Japan. [1]

Target: BTK

IC50: 2.2 nM

What is the solubility of Tirabrutinib in vitro?
DMSO: > 100 mg/mL

What is the solubility of Tirabrutinib in vivo?
1. DMSO, PEG300, Tween-80, saline
Please add DMSO (10%), PEG300 (40%), Tween-80 (5%), saline (45%) in order, solubility ≥ 2.5 mg/mL.
2. DMSO, 20% SBE-β-CD in saline
Please add 10% DMSO and 90% (20% SBE-β-CD in saline) in order, solubility: ≥ 2.5 mg/mL.
3. DMSO, corn oil
Please add 10% DMSO and 90% corn oil in order, solubility: ≥ 2.5 mg/mL.

Reference:
[1]. Dhillon, S. et al. “Tirabrutinib: First Approval”, Drugs, 2020, 80, 835-840
[2]. Nagane, M. et al. “Phase 1/2 Study of Tirabrutinib (ONO/GS-4059), a Next-Generation Bruton’s Tyrosine Kinase (BTK) Inhibitor, Monotherapy in Patients with Relapsed/Refractory Primary Central Nervous System Lymphoma (PCNSL)”, Blood, 2019, 134, (Supplement_1): 1586
[3]. Yamagami, M. et al. “A multicenter, open-label, uncontrolled, single-arm phase 2 study of tirabrutinib, an oral Bruton’s tyrosine kinase inhibitor, in pemphigus”, J. Dermatol. Sci. 2021, 103, 135-142.
[4]. Okita, Y. et al. “Histological verification of the treatment effect of tirabrutinib for relapsed/refractory primary central nervous system lymphoma”, Exp. Hematol. Oncol. 2021, 10, 870.
[5]. Narita, Y. et al. “Phase I/II study of tirabrutinib, a second-generation Bruton’s tyrosine kinase inhibitor, in relapsed/refractory primary central nervous system lymphoma”, Neuro-Oncol. 2021, 23, 122-133.
[6]. Morschhauser, F. et al. “Phase 1b study of tirabrutinib in combination with idelalisib or entospletinib in previously treated B-cell lymphoma”, Leukemia 2021, 35, 2108-2113.
[7]. Danilov, A. V. et al. “Phase Ib Study of Tirabrutinib in Combination with Idelalisib or Entospletinib in Previously Treated Chronic Lymphocytic Leukemia”, Clin. Cancer Res. 2020, DOI: 10.1158/1078-0432.CCR-19-3504
[8]. Sule, S. A. et al. “Long-term follow-up of patients with mantle cell lymphoma (MCL) treated with the selective Bruton’s tyrosine kinase inhibitor tirabrutinib (GS/ONO-4059)”, Leukemia 2020, 34, 1458-1461
[9]. Yoshizawa, T. et al. “ONO-4059—a Potent and Selective Reversible Bruton’s Tyrosine Kinase (Btk) Inhibitor: Single Agent, Twice Daily (BD) Dosing and Dosing with Food Results in Sustained, High Trough Levels of ONO-4059, Translating into 100% Tumour Remission in a TMD-8 Xenograft Model”, Blood, 2014, 124, 4502
[10]. Dyer, M. et al. “The Bruton’s tyrosine kinase (BTK) inhibitor ONO-4059: Single-agent activity in patients with relapsed and refractory non-GCB-DLBCL.”, J. Clin. Oncol., 2014, DOI: 10.1200/jco.2014.32.15_suppl.8553

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