ErSO

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

ErSO  纯度: 99.75%

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。

ErSO

ErSO Chemical Structure

CAS No. : 2407860-35-7

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5 mg ¥4000 In-stock
10 mg ¥6800 In-stock
25 mg ¥13500 In-stock
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100 mg   询价  

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ErSO 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Anti-Cancer Compound Library
  • Orally Active Compound Library
  • Anti-Breast Cancer Compound Library

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[1].

IC50 & Target

a-UPR[1]

体外研究
(In Vitro)

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[1].
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[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

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[1].
ErSO (0.5~40 mg/kg; p.o.; 3 weeks) is sufficient for a robust response[1].
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[1].
ErSO (40 mg/kg; i.p.; 14 days) greatly reduces metastatic burden[1].
ErSO treatment ablates mutant ERα breast cancer cell line xenografts and a PDX mouse model[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Nu/J mice[1]
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[1]
Dosage: 0.5~40 mg/kg
Administration: P.o.; 3 weeks
Result: Sufficient for a robust response.
Animal Model: Mice[1]
Dosage: 40 mg/kg
Administration: I.p.; 14 days
Result: Metastatic burden was greatly reduced

分子量

453.33

Formula

C22H13F6NO3

CAS 号

2407860-35-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
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。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Boudreau MW, et al. A small-molecule activator of the unfolded protein response eradicates human breast tumors in mice. Sci Transl Med. 2021;13(603):eabf1383.

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