WSB1 Degrader 1|cas:2306039-66-5|西域试剂

WSB1 Degrader 1,99.93%

产品编号：Bellancom-141482| CAS NO：2306039-66-5| 分子式：C₂₁H₂₂N₂O₂| 分子量：334.41

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-141482	￥3000.00	杭州北京（现货）
Bellancom-141482	￥4800.00	杭州北京（现货）
Bellancom-141482	￥9500.00	杭州北京（现货）
Bellancom-141482	￥14500.00	杭州北京（现货）
Bellancom-141482	￥22500.00	杭州北京（现货）

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WSB1 Degrader 1

产品介绍

WSB1 Degrader 1 是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。

生物活性

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.

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis

Cell 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.

体内研究
(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.

西域 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.

体内研究

西域 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.

体内研究

西域 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.

性状

Solid

溶解性数据

In Vitro:

DMSO : 25 mg/mL (74.76 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.9903 mL	14.9517 mL	29.9034 mL
5 mM	0.5981 mL	2.9903 mL	5.9807 mL
10 mM	0.2990 mL	1.4952 mL	2.9903 mL

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。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 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，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制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

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); Clear solution

此方案可获得 ≥ 2.08 mg/mL (6.22 mM，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；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液