2-Pyridinamine, 5,6-bis(4-methoxy-3-methylphenyl)-
- CAS No.
- 2306039-66-5
- Chemical Name:
- 2-Pyridinamine, 5,6-bis(4-methoxy-3-methylphenyl)-
- Synonyms
- WSB1 Degrader 1;5,6-Bis(4-methoxy-3-methylphenyl)pyridin-2-amine;2-Pyridinamine, 5,6-bis(4-methoxy-3-methylphenyl)-;E3 ligating enzyme,oral,inhibit,anticancer,Ubiquitin conjugating enzyme,Ubiquitin activating enzyme,E2 conjugating enzyme,Inhibitor,E1 activating enzyme,E1/E2/E3 Enzyme,WSB1 Degrader 1,metastasis,Ubiquitin ligase,WSB-1 Degrader 1,RhoGDI2,WSB1
- CBNumber:
- CB29280425
- Molecular Formula:
- C21H22N2O2
- Molecular Weight:
- 334.41
- MDL Number:
- MFCD34368539
- MOL File:
- 2306039-66-5.mol
2-Pyridinamine, 5,6-bis(4-methoxy-3-methylphenyl)- Chemical Properties,Uses,Production
Biological Activity
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[1]. 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[1].WSB1 Degrader 1 (compound 4) exhibits 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 (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[1].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[1]. WSB1 Degrader 1 (compound 4; 100 mg/kg; p.o.; daily; for 28 days) treatment can effectively inhibit the pulmonary metastasis of cancer cells[1].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 (T1/2). Moreover, Cmax and AUC0-t values of WSB1 Degrader 1 in oral or intraperitoneal dosing groups showed acceptable blood exposure[1].
References
[1]. Jinxin Che, et al. Discovery of 5,6-Bis(4-methoxy-3-methylphenyl)pyridin-2-amine as a WSB1 Degrader to Inhibit Cancer Cell Metastasis. J Med Chem. 2021 Jun 1.
2-Pyridinamine, 5,6-bis(4-methoxy-3-methylphenyl)- Preparation Products And Raw materials
Raw materials
Preparation Products
2-Pyridinamine, 5,6-bis(4-methoxy-3-methylphenyl)- Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
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| TargetMol Chemicals Inc. | +1-781-999-5354 | support@targetmol.com | United States | 19973 | 58 |
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