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Chemical Structure : Orelabrutinib
CAS No.: 1655504-04-3
Catalog No.: 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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $138 | In stock | |
| 10 mg | $218 | In stock | |
| 25 mg | $388 | In stock | |
| 50 mg | $598 | In stock | |
| 100 mg | Get quote |
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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.
| M.Wt | 427.50 | |
| Formula | C26H25N3O3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
6-(1-Acryloylpiperidin-4-yl)-2-(4-phenoxyphenyl)nicotinamide |
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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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