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编 号:F611173
分子式:C24H31F3N4S
分子量:464.59
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生物活性:
ZZW-115 is a potent NUPR1 inhibitor, with a Kd of 2.1 μM. ZZW-115 induces tumor cell death by necroptosis and apoptosis. Anticancer activity.

体内研究:
ZZW-115 (0.5-5 mg/kg; injection; daily for 30 days) inhibits the growth of pancreatic xenografted tumors.ZZW-115 (5 mg/kg for 30 days; immunocompetent C57BL/6 mice were orthotopically implanted with Panc02 cells) treatment shows the tumor size is almost unmeasurable in some cases.Animal Model:NMRI-Foxn1nu/Foxn1nu mice (nude mice) xenografted with MiaPaCa-2 cells
Dosage:5, 2.5, 1.0, or 0.5 mg/kg
Administration:Injection, daily for 30 days
Result:When the mice were injected with 5 mg/kg ZZW-115, the tumors stopped growing a few days after treatment and their size decreased progressively, almost disappearing at the end of the treatment.

体外研究:
ZZW-115 (0.1-33 μM; 72 hours) is efficient in killing cancer cells, with an IC50 in the range of 0.84 μM (ANOR) to 4.93 μM (HN14).ZZW-115 (0-100 μM; 24-72 hours) is efficient to kill these tumor cells with an IC50 in the range of 0.42 μM (Hep2G cells) to 7.75 μM (SaOS-2 cells).ZZW-115 induces pancreatic cell death by necrosis and apoptosis. ZZW-115 treatment induces a decrease in ATP production and induces a ROS overproduction.LDH release is significantly higher in ZZW-115-treated cells (MiaPaCa-2, 02-063, LIPC, Foie8b, and HN14 cells) than in control cells in a concentration-dependent manner. Similarly, caspase 3/7 activity is also greater in ZZW-115-treated cells. These experiments demonstrated that ZZW-115 exerted both pronecrotic and proapoptotic effects.
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