Informationtirabrutinib(ONO-4059) hydrochloride Tirabrutinib Hydrochloride (ONO-4059, GS-4059) is highly potent and selective BTK inhibitor with an IC50 of 2.2 nM.TargetsBTK 2.2 nMIn vitroONO-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 vivoONO-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 Research(from reference)Cell lines：DLBCL cell lines TMD8 cells Concentrations：320 nM Incubation Time：48 h. Specification: 10mM in DMSO Molecular Formula: C25H22N6O3.HCl Molecular Weight: 490.94 PubChem CID: 71571562 Isomeric SMILES: CC#CC(=O)N1CC[C@H](C1)N2C3=NC=NC(=C3N(C2=O)C4=CC=C(C=C4)OC5=CC=CC=C5)N.Cl
- UPC:
- 51131620
- Condition:
- New
- Availability:
- 8-12 weeks
- Weight:
- 0.85 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- T421616-1ml
- CAS:
- 1439901-97-9
- Product Size:
- 1ml
