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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Orelabrutinib (ICP-022)
Dangerous GoodsCAS number：1655504-04-3 molecular formula：C26H25N3O3
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compound introduction
Specs
| Chinese alias | - | ||
| English alias | AC-36680 | ICP022 | ICP-022 | Orelabrutinib | 6-(1-(1-Oxo-2-propen-1-yl)-4-piperidinyl)-2-(4-phenoxyphenyl)-3-pyridinecarboxamide | HY-129390 | F88710 | HY-108451 | NSC826039 | NSC-826039 | ORELABRUTINIB [WHO-DD] | 2-(4-phenoxyphenyl)-6-(1-prop-2-enoylpip | ||
| CAS number | 1655504-04-3 | molecular formula | C26H25N3O3 |
| molecular weight | 427.49 g/mol | Exact mass | - |
| PSA | 85.500 Ų | logp | 4.055 |
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physicochemical properties
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Safety information
pictogram：
GHS07
Signal word：
Warning
Hazard Statement：
H315: 引起皮肤刺激 H319: 引起严重眼睛刺激 H335: 可能引起呼吸道刺激 H302: 吞食有害
Statement of Preventive Measures：
P261: 避免吸入灰尘/烟雾/气体/雾/蒸汽/喷雾 P305+P351+P338: 如进入眼睛：用水小心冲洗几分钟。如戴隐形眼镜并可方便地取出，取出隐形眼镜。继续冲洗。
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