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首页-小分子抑制剂&激动剂-Tyrosine Kinase-BTK-Orelabrutinib
Orelabrutinib

Chemical Structure : Orelabrutinib

CAS No.: 1655504-04-3

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Orelabrutinib (ICP-022, ICP022)

货号: PC-23189Not For Human Use, Lab Use Only.

Orelabrutinib (ICP-022) is a potent, selective, orally active, and irreversible Bruton's tyrosine kinase (BTK) inhibitor with IC50 of 1.6 nM.

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5 mg ￥1380 In stock
10 mg ￥2180 In stock
25 mg ￥3880 In stock
50 mg ￥5980 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Orelabrutinib (ICP-022) is a potent, selective, orally active, and irreversible Bruton's tyrosine kinase (BTK) inhibitor with IC50 of 1.6 nM.
Orelabrutinib (ICP-022) displays high selectivity at 1 μM against a panel of 456 kinases, only targets BTK with >90% inhibition lacking inhibition on many additional kinases, including EGFR, TEC, and bone marrow tyrosine kinase.
Orelabrutinib (ICP-022) inhibited B cell lymphoma cell proliferation in vitro (TMD8 cell, IC50=0.08 uM).
Orelabrutinib (ICP-022) lacked inhibition on cellular ITK compared with ibrutinib.
Orelabrutinib (ICP-022) preserved rituximab-mediated cytotoxicity, the combination of orelabrutinib and rituximab treatment enhanced NK-cell-mediated ADCC.
Orelabrutinib (ICP-022) combined with rituximab effectively inhibited tumor growth in animal models.

物理化学性质&存储条件

分子量 427.50
分子式 C26H25N3O3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

6-(1-Acryloylpiperidin-4-yl)-2-(4-phenoxyphenyl)nicotinamide

参考文献

1. Yu H, et al. Mol Ther Oncolytics. 2021 Apr 3;21:158-170.

2. Wu JJ, et al. Invest New Drugs. 2022 Jun;40(3):650-659.

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