2379884-70-3
2379884-70-3
Chemical Structure
HZ-A-018
- CAS No.: 2379884-70-3
- Formula:C27H24N6O2
- Molecular Weight:464.52
InChIKey: ULLYUWLWLYIOCF-NRFANRHFSA-N
SMILES: CC#CC(N1CCC[C@H]1C2=NC(C3=CC=C(C=C3)C(NC4=CC=CC=C4)=O)=C5C(N)=NC=CN25)=O
Biological Activity: HZ-A-018 is an orally active BTK inhibitor (IC50 = 4.0 nM) that inhibits BTK phosphorylation and AKT/S6 ribosomal protein phosphorylation by binding to cysteine 481 in the ATP-binding site, induces apoptosis, and decreases RRM2 expression, sensitizing gastric cancer cells to 5-Fluorouracil (5-FU) (HY-90006). HZ-A-018 can be used for research on gastric cancer and relapsed or refractory B-cell malignancies[1][2].
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HZ-A-018 | HZ-A-018 is an orally active BTK inhibitor (IC50 = 4.0 nM) that inhibits BTK phosphorylation and AKT/S6 ribosomal protein phosphorylation by binding to cysteine 481 in the ATP-binding site, induces apoptosis, and decreases RRM2 expression, sensitizing gastric cancer cells to 5-Fluorouracil (5-FU) (HY-90006). HZ-A-018 can be used for research on gastric cancer and relapsed or refractory B-cell malignancies. | |||||||||||||||||||||
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References
- [1]. Liu D, et al. HZ-A-018, a novel inhibitor of Bruton tyrosine kinase, exerts anti-cancer activity and sensitizes 5-FU in gastric cancer cells. Frontiers in pharmacology. 2023;14:1142127.
- [2]. Wu G, et al. Covalent Bruton's tyrosine kinase inhibitor HZ-A-018 in patients with relapsed or refractory B cell malignancies: A multicenter phase I study. iScience. 2026 Aug 21;29(8):116809.
