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描述 | 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]. |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
2.99mL 0.60mL 0.30mL |
14.95mL 2.99mL 1.50mL |
29.90mL 5.98mL 2.99mL |
CAS号 | 2306039-66-5 |
分子式 | C21H22N2O2 |
分子量 | 334.412 |
别名 | |
运输 | 蓝冰 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Keep in dark place,Inert atmosphere,Room temperature |
溶解方案 |
DMSO: 25 mg/mL(74.76 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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动物实验配方 |