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In vitro: ONO-4059 covalently binds to BTK, and reversibly blocks BCR signaling and B-cell proliferation and activation. It has greater selectivity for BTK than Lck, Fyn, LynA and ONO/GS-4059 only inhibits anti-IgM-induced B-cell activation in a concentration-dependent manner but not inhibit anti-CD3/CD28-induced activation of T-lymphocytes from human PBMCs. ONO/GS-4059 inhibits cell proliferation in some malignant B-cell lines but also induces classical apoptosis at nanomolar concentration in the activated-B cell (ABC) DLBCL cell line, TMD8.
In vivo: ONO-4059 demonstrates therapeutic efficacy in a mouse CIA model by suppressing generation of inflammatory chemokines and cytokines including IL-6, IL-8, and TNFα by monocytes, and accompanied by regression of cartilage erosion, bone damage, and pannus formation. In pre-clinical models, and in the clinic in both CLL and NHL patients, It exerts its anti-tumour activity, with a favourable safety profile along with promising efficacy over a long duration.
| Cell Experiment | |
|---|---|
| Cell lines | DLBCL cell lines TMD8 cells |
| Preparation method | Cells are treated with idelalisib (420 nM), ONO/GS-4059 (320 nM) or in combination for 48 hours and apoptosis is assessed by FITC Annexin V staining, and measured by flow cytometry. |
| Concentrations | 320 nM |
| Incubation time | 48 h |
| Animal Experiment | |
|---|---|
| Animal models | Male CB17-SCID mice |
| Formulation | 5% (v/v) N-Methyl-2-pyrrolidone (NMP) / 55% (v/v) Polyethylene Glycol 300 (PEG) 300 / 40% (v/v) Water / 1% (w/v) Vitamin E D-α-Tocopherol Polyethylene Glycol 1000 Succinate (TPGS) |
| Dosages | 5 and 10 mg/kg |
| Administration | oral gavage |
| Molecular Weight | 490.94 |
| Formula | C25H22N6O3.HCl |
| CAS Number | 1439901-97-9 |
| Solubility (25°C) | 98 mg/mL in DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[2] Wu J, et al. Oncotarget. Bruton tyrosine kinase inhibitor ONO/GS-4059: from bench to bedside.
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