ErSO|cas:2407860-35-7|西域试剂

ErSO,99.75%

产品编号：Bellancom-132247| CAS NO：2407860-35-7| 分子式：C₂₂H₁₃F₆NO₃| 分子量：453.33

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货号	价格	库存与货期
Bellancom-132247	￥2900.00	杭州北京（现货）
Bellancom-132247	￥4600.00	杭州北京（现货）
Bellancom-132247	￥8700.00	杭州北京（现货）

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ErSO

产品介绍

ErSO是一种选择性预期折叠蛋白反应 (a-UPR) 激活剂。ErSO 通过 ERα 诱导 a-UPR 产生强而持久的细胞毒性。ErSO 可用于癌症研究。

生物活性

ErSO is a selective anticipatory unfolded protein response (a-UPR) activator. ErSO acts through ERα to elicit strong and sustained cytotoxic activation of the a-UPR. ErSO can be used for the research of cancer.

体外研究

ErSO (1~1000 nM; 24 hours; MCF-7 cells) shows that IC₅₀ value is 20.3 nM in MCF-7 cells and inhibits cell viability.
ErSO (1 μM; 24 hours; TYS cells) rapidly kills ERα-positive breast cancer cells. ErSO is effective against both the breast cancer cell lines expressing wild-type ERα and the ERαY537S and ERαD538G mutations such as human breast cancer cell lines TYS and TDG. ErSO is also effective against tamoxifen- and fulvestrant-resistant breast cancer cell lines containing wild-type ERα. ErSO activity is independent of the presence of estrogen. ErSO induces rapid killing of ERα-positive MCF-7 human breast cancer cells.

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

Cell Viability Assay

Cell Line:	MCF-7 cells
Concentration:	1~1000 nM
Incubation Time:	24 hours
Result:	Showed that IC₅₀ value is 20.3 nM in MCF-7 cells and inhibited cell viability.

体内研究
(In Vivo)

ErSO (10 or 40 mg/kg; p.o.; 21 days) results in elimination of these tumors, with >90% reduction in all cases.
ErSO (0.5~40 mg/kg; p.o.; 3 weeks) is sufficient for a robust response.
ErSO (10 and 40 mg/kg; p.o.; 14 days) induces >10,000-fold regression of TYS-luciferase-expressing breast tumors in all five mice and >100,000-fold regression (to undetectable amounts) within 14 days as shown by bioluminescent imaging of luciferase as compared to vehicle-treated mice.
ErSO (40 mg/kg; i.p.; 14 days) greatly reduces metastatic burden.
ErSO treatment ablates mutant ERα breast cancer cell line xenografts and a PDX mouse model.

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

Animal Model:	Nu/J mice
Dosage:	10 or 40 mg/kg
Administration:	P.o.; 21 days
Result:	Resulted in elimination of these tumors, with >90% reduction in all cases.

Animal Model:	Mice
Dosage:	0.5~40 mg/kg
Administration:	P.o.; 3 weeks
Result:	Sufficient for a robust response.

Animal Model:	Mice
Dosage:	40 mg/kg
Administration:	I.p.; 14 days
Result:	Metastatic burden was greatly reduced

体内研究

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

Animal Model:	Nu/J mice
Dosage:	10 or 40 mg/kg
Administration:	P.o.; 21 days
Result:	Resulted in elimination of these tumors, with >90% reduction in all cases.

Animal Model:	Mice
Dosage:	0.5~40 mg/kg
Administration:	P.o.; 3 weeks
Result:	Sufficient for a robust response.

Animal Model:	Mice
Dosage:	40 mg/kg
Administration:	I.p.; 14 days
Result:	Metastatic burden was greatly reduced

体内研究

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

Animal Model:	Nu/J mice
Dosage:	10 or 40 mg/kg
Administration:	P.o.; 21 days
Result:	Resulted in elimination of these tumors, with >90% reduction in all cases.

Animal Model:	Mice
Dosage:	0.5~40 mg/kg
Administration:	P.o.; 3 weeks
Result:	Sufficient for a robust response.

Animal Model:	Mice
Dosage:	40 mg/kg
Administration:	I.p.; 14 days
Result:	Metastatic burden was greatly reduced

性状

Solid

溶解性数据

In Vitro:

DMSO : 120 mg/mL (264.71 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.2059 mL	11.0295 mL	22.0590 mL
5 mM	0.4412 mL	2.2059 mL	4.4118 mL
10 mM	0.2206 mL	1.1029 mL	2.2059 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: 5.25 mg/mL (11.58 mM); Suspended solution; Need ultrasonic

此方案可获得 5.25 mg/mL (11.58 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 52.5 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
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 3 mg/mL (6.62 mM); Clear solution

此方案可获得 ≥ 3 mg/mL (6.62 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 30.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 3 mg/mL (6.62 mM); Clear solution

此方案可获得 ≥ 3 mg/mL (6.62 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 30.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。