| Identification | Back Directory | [Name]
2-Pyridinamine, 5,6-bis(4-methoxy-3-methylphenyl)- | [CAS]
2306039-66-5 | [Synonyms]
WSB1 Degrader 1
2-Pyridinamine, 5,6-bis(4-methoxy-3-methylphenyl)- | [Molecular Formula]
C21H22N2O2 | [MDL Number]
MFCD34368539 | [MOL File]
2306039-66-5.mol | [Molecular Weight]
334.41 |
| Chemical Properties | Back Directory | [Boiling point ]
456.9±45.0 °C(Predicted) | [density ]
1.129±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 25 mg/mL (74.76 mM; Need ultrasonic) | [form ]
Solid | [pka]
6.50±0.41(Predicted) | [color ]
Off-white to light yellow |
| Hazard Information | Back Directory | [Uses]
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]. | [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]. | [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[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]. | Animal Model: | Balb/c (nu/nu) mice bearing highly metastatic 4T1 breast cancer cells[1]. | | Dosage: | 100 mg/kg/day
| | Administration: | p.o.; daily; for 28 days | | Result: | Effectively inhibited the pulmonary metastasis of cancer cells. |
| [storage]
Store at -20°C | [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. |
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