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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
| Canonical Smiles | CC1=C(C=CC(=C1)C2=C(N=C(C=C2)N)C3=CC(=C(C=C3)OC)C)OC |
|---|---|
| IUPAC Name | 5,6-bis(4-methoxy-3-methylphenyl)pyridin-2-amine |
| InChIKey | AUHCLHXXUVPUBD-UHFFFAOYSA-N |
| INCHI | 1S/C21H22N2O2/c1-13-11-15(5-8-18(13)24-3)17-7-10-20(22)23-21(17)16-6-9-19(25-4)14(2)12-16/h5-12H,1-4H3,(H2,22,23) |
| PubChem CID | 149706874 |
| Molecular Weight | 334.41 |
Comprehensive hazard, handling, storage, and regulatory compliance document.
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View spec sheet →| Solubility | DMSO : 25 mg/mL (74.76 mM; Need ultrasonic) |
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