ZLY025 is a potent and orally active CCNK molecular glue degrader with an DC50 of 42.7 nM. ZLY025 exhibits broad-spectrum antiproliferative activity against various tumor cells with IC50 values ranging from 0.08 to 2.45 μM. ZLY025 can induce cells apoptosis and G1 phase arrest. ZLY025 can be used for the research of cancer, such as lung cancer [1].
In Vivo, ZLY025 (10-40 mg/kg; i.g.; once daily for 17 days; ) inhibits tumor growth in BALB/c nude mice bearing A549 xenografts[1]. ZLY025 (200 mg/kg, i.g., once daily for 14 days) shows extremely low subacute toxicity in ICR mice[1].
In Vitro, ZLY025 exhibits broad-spectrum antiproliferative activity against various tumor cell lines including lung cancer, breast cancer, liver cancer, and leukemia, with IC50 values ranging from 0.08 to 2.45 μM[1]. ZLY025 (125-500 nM; 24 h) induces A549 cells apoptosis and G1 phase arrest[1]. ZLY025 (30-1000 nM; 8-24 h) reduces expression of CCNK, CDK12, p-CTD, and BRCA1 in A549 cells[1].
References:
[1]. Liu Y, et al. Discovery of Highly Potent and Orally Available CCNK Molecular Glue Degraders as Broad-Spectrum Antitumor Agents. J Med Chem. 2025;68(21):22689-22714.
In Vivo, ZLY025 (10-40 mg/kg; i.g.; once daily for 17 days; ) inhibits tumor growth in BALB/c nude mice bearing A549 xenografts[1]. ZLY025 (200 mg/kg, i.g., once daily for 14 days) shows extremely low subacute toxicity in ICR mice[1].
In Vitro, ZLY025 exhibits broad-spectrum antiproliferative activity against various tumor cell lines including lung cancer, breast cancer, liver cancer, and leukemia, with IC50 values ranging from 0.08 to 2.45 μM[1]. ZLY025 (125-500 nM; 24 h) induces A549 cells apoptosis and G1 phase arrest[1]. ZLY025 (30-1000 nM; 8-24 h) reduces expression of CCNK, CDK12, p-CTD, and BRCA1 in A549 cells[1].
References:
[1]. Liu Y, et al. Discovery of Highly Potent and Orally Available CCNK Molecular Glue Degraders as Broad-Spectrum Antitumor Agents. J Med Chem. 2025;68(21):22689-22714.