WSB1 Degrader 1 is a potent and orally active WSB1 (WD repeat and SOCS box-containing 1) degrader, exerting anticancer metastatic effects[1].
体内研究
WSB1 Degrader 1 treatment (100 mg/kg; pO.; daily; for 28 days) effectively inhibits pulmonary metastasis of cancer cells[1].
In rats, following oral dosing of 100 mg/kg or intraperitoneal dosing of 160 mg/kg of WSB1 Degrader 1, both routes of administration show rapid absorption (Tmax), but the former exhibits rapid clearance (T1/2). Additionally, Cmax and AUC0-t values of WSB1 Degrader 1 in oral or intraperitoneal dosing groups indicate acceptable blood exposure[1].
体外研究
WSB1 Degrader 1 treatment (0.25-2500 nM; 2-24 hours; H1299-WSB1 cells) induces WSB1 degradation in both time-dependent and dose-dependent manners[1].
WSB1 Degrader 1 demonstrates potent antimigration efficacy in both KHOS and H460 cell lines, with IC50 values of 39.1 μM and 24.47 μM, respectively[1].
WSB1 Degrader 1 significantly inhibits cancer cell migration under both normoxia and hypoxia conditions in KHOS cells. Treatment with WSB1 Degrader 1 (5 μM) elevates the levels of the RhoGDI2 protein in KHOS cells under hypoxia[1].
WSB1 Degrader 1 significantly inhibits the wound-healing capability of H1299-WSB1 cells. However, WSB1 Degrader 1 only blocks wound healing in wild-type A2780 (A2780-WT) cells and not in A2780-WSB1/KO cells[1].
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