Chemical Structure : HZ-A-018
CAS No.:
2379884-70-3
HZ-A-018
Catalog No.: PC-27437Not For Human Use, Lab Use Only.
HZ-A-018 is a derivative of ACP-196 and potent, highly selective, covalent BTK inhibitor with IC50 of 4.0 nM, binds irreversibly to cysteine 481 (Cys481), exhibits minimal activity against off-target kinases such as ITK, HCK, SRC, and CSK.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
HZ-A-018 is a derivative of ACP-196 and potent, highly selective, covalent BTK inhibitor with IC50 of 4.0 nM, binds irreversibly to cysteine 481 (Cys481), exhibits minimal activity against off-target kinases such as ITK, HCK, SRC, and CSK.
HZ-A-018 displays stronger anti-proliferation activity in gastric cancer cells (HGC-27 cell, IC50=17.9 uM) than ACP-196 (HGC-27 cell, IC50=35.6 uM) via the substantial suppression of AKT/S6 pathway.
HZ-A-018, but not ACP-196, exerts the synergistic effects in gastric cancer cells when combined with 5-FU both in vitro and in vivo, without exacerbating the adverse effects of 5-FU.
The combination of HZ-A-018 and 5-FU remarkably reduced the expression of RRM2, which played an essential role in proliferation and drug sensitivity in gastric cancer cells.
Physicochemical Properties
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M.Wt
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464.53
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Formula
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C27H24N6O2
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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(S)-4-(8-amino-3-(1-(but-2-ynoyl)pyrrolidin-2-yl)imidazo[1,5-a]pyrazin-1-yl)-N-phenylbenzamide
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References
1. Liu D, et al. Front Pharmacol. 2023 Mar 22;14:1142127.
2. Wu G, et al. iScience. 2026 Jul 17;29(8):116809.
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