HZ-A-018

Chemical Structure : HZ-A-018

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货号: 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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生物&药学活性

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.

物理化学性质&存储条件

分子量	464.53
分子式	C27H24N6O2
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
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Solubility	10 mM in DMSO
Chemical Name/SMILES	(S)-4-(8-amino-3-(1-(but-2-ynoyl)pyrrolidin-2-yl)imidazo[1,5-a]pyrazin-1-yl)-N-phenylbenzamide

参考文献

1. Liu D, et al. Front Pharmacol. 2023 Mar 22;14:1142127.

2. Wu G, et al. iScience. 2026 Jul 17;29(8):116809.

HZ-A-018

生物&药学活性

物理化学性质&存储条件

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HZ-A-018

生物&药学活性

物理化学性质&存储条件

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