WSB1 Degrader 1

WSB1 Degrader 1 is a poten and orally active WSB1 (WD repeat and SOCS box-containing 1) degrader. WSB1 Degrader 1 has anticancer metastatic effects. In Vitro WSB1 Degrader 1 (compound 4; 0.25-2500 nM; 2-24 hours; H1299-WSB1 cells) treatment indues WSB1 degradation in time-dependent and dose-dependent manners. WSB1 Degrader 1 (compound 4) exhibits potent antimigration efficacy in both KHOS and H460 cell lines with IC 50 values of 39.1 μM and 24.47 μM, respectively. WSB1 Degrader 1 (compound 4) significantly inhibits cancer cell migration under normoxia and hypoxia in KHOS cells. WSB1 Degrader 1 (5 μM) treatment elevates the levels of the RhoGDI2 protein in KHOS cells under hypoxia. The wound-healing of H1299-WSB1 cells is significantly inhibited by treating with WSB1 Degrader 1. WSB1 Degrader 1 can only block the wound-healing capability of wild-type A2780 (A2780-WT) cells but not the A2780-WSB1/KO cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: H1299-WSB1 cells Concentration: 0.25 nM, 2.5 nM, 25 nM, 250 nM, 2500 nM Incubation Time: 2 hours, 4 hours, 6 hours, 8 hours, 12 hours, 24 hours Result: Induced WSB1 degradation in time-dependent and dose-dependent manners. In Vivo WSB1 Degrader 1 (compound 4; 100 mg/kg; p.o.; daily; for 28 days) treatment can effectively inhibit the pulmonary metastasis of cancer cells . In rats, after 100 mg/kg oral dosing or 160 mg/kg intraperitoneal dosing of WSB1 Degrader 1 (compound 4), the two ways of administration are observed with quick absorption (Tmax), but the former dosing displayed a fast clearance (T 1/2 ). Moreover, C max and AUC 0-t values of WSB1 Degrader 1 in oral or intraperitoneal dosing groups showed acceptable blood exposure . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Balb/c (nu/nu) mice bearing highly metastatic 4T1 breast cancer cells . Dosage: 100 mg/kg/day Administration: p.o.; daily; for 28 days Result: Effectively inhibited the pulmonary metastasis of cancer cells. Form:Solid

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