盐酸替拉鲁替x（ONO-4059）

中文名：盐酸替拉鲁替x（ONO-4059）

英文名：tirabrutinib(ONO-4059) hydrochloride

纯度：≥98%

货号：T413925

Cas号：1439901-97-9

存储温度：-20°C储存

运输条件：超低温冰袋运输

产品介绍：

Information

tirabrutinib(ONO-4059) hydrochloride Tirabrutinib Hydrochloride (ONO-4059, GS-4059) is highly potent and selective BTK inhibitor with an IC50 of 2.2 nM.

Targets

BTK 2.2 nM

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 Research(from reference)

Cell lines：DLBCL cell lines TMD8 cells

Concentrations：320 nM

Incubation Time：48 h

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