中文名:奥拉布替尼(ICP-022)
英文名:Orelabrutinib (ICP-022)
纯度:Moligand™,≥98%
货号:O414422
Cas号:1655504-04-3
存储温度:-20°C储存
运输条件:超低温运输
产品介绍:
Information
Orelabrutinib (ICP-022) Orelabrutinib (ICP-022) is a potent, orally active and irreversible inhibitor of Bruton's tyrosine kinase (BTK) . Orelabrutinib has potential antineoplastic activity.
Targets
BTK
In vitro
Orelabrutinib potently inhibits BTK enzymatic activity with an IC50 value of 1.6 nM. In KINOMEscan assay conducted in parallel at 1 μM against a panel of 456 kinases, orelabrutinib only targets BTK with > 90% inhibition while ibrutinib inhibits additional many other kinases including EGFR, TEC and BMX, demonstrating orelabrutinib\'s superior kinase selectivity.
In vivo
Orelabrutinib has a favorable PK profile with an ideal T1/2 (~1.5-4 h) and good oral bioavailability (~20-80%) as well as prolonged BTK target occupancy in preclinical PK/PD studies. The superior selectivity translates into improved safety profile and large safety window in the GLP toxicology studies in rats and dogs.
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