| 中文名称: | WSB1 Degrader 1 | ||||
|---|---|---|---|---|---|
| 英文名称: | WSB1 Degrader 1 | ||||
| 别名: | EX-A5123 | ||||
| CAS No: | 2306039-66-5 | 分子式: | C21H22N2O2 | 分子量: | 334.41 |
| CAS No: | 2306039-66-5 | ||||
| 分子式: | C21H22N2O2 | ||||
| 分子量: | 334.41 | ||||
| MDL: | MFCD34368539 | ||||
包装规格：
1mg 5mg 10mg 25mg 50mg 100mg in glass bottle
产品简介：
一种有效的具有口服活性的 WSB1 (WD repeat and SOCS box-containing 1) 降解剂。WSB1 Degrader 1 具有抗癌转移作用。
溶解性：
DMSO :25 mg/mL (74.76 mM; 超声助溶)
储备液保存：
-80°C, 6 months
-20°C, 1 month
-20°C, 1 month
体内实验：
1、请依序添加每种溶剂：10% DMSO→40% PEG300→5% Tween-80→45% Saline
Solubility: ≥ 2.08 mg/mL (6.22 mM); 澄清溶液
此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。
＜1mg/ml表示微溶或不溶。
普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
Solubility: ≥ 2.08 mg/mL (6.22 mM); 澄清溶液
此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。
＜1mg/ml表示微溶或不溶。
普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
体外研究：
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 IC50 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.
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.
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.
体内研究：
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 (T1/2). Moreover, Cmax and AUC0-t values of WSB1 Degrader 1 in oral or intraperitoneal dosing groups showed acceptable blood exposure.
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.
保存条件：
-20°C
注意事项：
1、为了您的安全和健康，请穿实验服并戴一次性手套操作。
2、以上信息仅做参考交流之用。
2、以上信息仅做参考交流之用。
UN码：
HazardClass：
危害声明：
安全说明：
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参考文献 & 客户发表文献
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入 输出 )
