ErSO
目录号 : GC62443
ErSO activates the anticipatory unfolded protein response (a-UPR) with an IC50 of 20.3 nM in MCF-7 cells. ErSO induces rapid and selective necrosis of ERα-positive breast cancer cell lines in vitro.
Cas No.:2407860-35-7
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
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- Purity: >98.00%
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- Datasheet
ErSO activates the anticipatory unfolded protein response (a-UPR) with an IC50 of 20.3 nM in MCF-7 cells. ErSO induces rapid and selective necrosis of ERα-positive breast cancer cell lines in vitro.
[1] Matthew W Boudreau, et al. Sci Transl Med . 2021 Jul 21;13(603):eabf1383.
| Cas No. | 2407860-35-7 | SDF | |
| 分子式 | C22H13F6NO3 | 分子量 | 453.33 |
| 溶解度 | 储存条件 | Store at -20°C | |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.2059 mL | 11.0295 mL | 22.059 mL |
| 5 mM | 0.4412 mL | 2.2059 mL | 4.4118 mL |
| 10 mM | 0.2206 mL | 1.1029 mL | 2.2059 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
A small-molecule activator of the unfolded protein response eradicates human breast tumors in mice
Sci Transl Med 2021 Jul 21;13(603):eabf1383.PMID:34290053DOI:10.1126/scitranslmed.abf1383.
Metastatic estrogen receptor α (ERα)-positive breast cancer is presently incurable. Seeking to target these drug-resistant cancers, we report the discovery of a compound, called ErSO, that activates the anticipatory unfolded protein response (a-UPR) and induces rapid and selective necrosis of ERα-positive breast cancer cell lines in vitro. We then tested ErSO in vivo in several preclinical orthotopic and metastasis mouse models carrying different xenografts of human breast cancer lines or patient-derived breast tumors. In multiple orthotopic models, ErSO treatment given either orally or intraperitoneally for 14 to 21 days induced tumor regression without recurrence. In a cell line tail vein metastasis model, ErSO was also effective at inducing regression of most lung, bone, and liver metastases. ErSO treatment induced almost complete regression of brain metastases in mice carrying intracranial human breast cancer cell line xenografts. Tumors that did not undergo complete regression and regrew remained sensitive to retreatment with ErSO. ErSO was well tolerated in mice, rats, and dogs at doses above those needed for therapeutic responses and had little or no effect on normal ERα-expressing murine tissues. ErSO mediated its anticancer effects through activation of the a-UPR, suggesting that activation of a tumor protective pathway could induce tumor regression.
Activators of the Anticipatory Unfolded Protein Response with Enhanced Selectivity for Estrogen Receptor Positive Breast Cancer
J Med Chem 2022 Mar 10;65(5):3894-3912.PMID:35080871DOI:10.1021/acs.jmedchem.1c01730.
Approximately 75% of breast cancers are estrogen receptor alpha-positive (ERα+), and targeting ERα directly with ERα antagonists/degraders or indirectly with aromatase inhibitors is a successful therapeutic strategy. However, such treatments are rarely curative and development of resistance is universal. We recently reported ErSO, a compound that induces ERα-dependent cancer cell death through a mechanism distinct from clinically approved ERα drugs, via hyperactivation of the anticipatory unfolded protein response. ErSO has remarkable tumor-eradicative activity in multiple ERα+ tumor models. While ErSO has promise as a new drug, it has effects on ERα-negative (ERα-) cells in certain contexts. Herein, we construct modified versions of ErSO and identify variants with enhanced differential activity between ERα+ and ERα- cells. We report ErSO-DFP, a compound that maintains antitumor efficacy, has enhanced selectivity for ERα+ cancer cells, and is well tolerated in rodents. ErSO-DFP and related compounds represent an intriguing new class for the treatment of ERα+ cancers.
Preparation and Properties of Plant-Oil-Based Epoxy Acrylate-Like Resins for UV-Curable Coatings
Polymers (Basel) 2020 Sep 22;12(9):2165.PMID:32971913DOI:10.3390/polym12092165.
Novel oil-based epoxy acrylate (EA)-like prepolymers were synthesized via the ring-opening reaction of epoxidized plant oils with a new unsaturated carboxyl acid precursor (MAAMA) synthesized by reacting maleic anhydride (MA) with methallyl alcohol (MAA). Since the employed epoxidized oils including epoxidized soybean oil (ESO), epoxidized rubber seed oil (ErSO), and epoxidized wilsoniana seed oil (EWSO) possessed epoxy values of 7.34-4.38%, the obtained epoxy acrylate (EA)-like prepolymers (MMESO, MMERSO, and MMEWSO) indicated a C=C functionality of 7.81-4.40 per triglyceride. Furthermore, effects of the C=C functionality and the addition of hydroxyethyl methacrylate (HEMA) diluent on the ultimate properties of the resulting UV-cured EA-like materials were investigated and compared with those of commercially available acrylated ESO (AESO) resins. As the C=C functionality increased, the storage modulus at 25 °C (E'25), glass transition temperature (Tg), 5% weight-loss temperature (T5), tensile strength and modulus (σ and E), and hardness of the coating for both the pure EA and EA/HEMA resins increased significantly as well. These properties indicated similar trends when comparing the EA materials with 30% of HEMA with those pure EA materials. Specially, although ErSO had a clearly lower epoxy value that ESO, both the UV-cured pure MMERSO and MMERSO/HEMA materials showed much better E'25, Tg, σ, and E than their AESO counterparts, indicating that the MAAMA modification of epoxidized plant oils was much more effective than the modification of acrylic acid to achieve high-performance oil-based epoxy acrylate resins.
Rapid emission angle selection for rotating-shield brachytherapy
Med Phys 2013 May;40(5):051720.PMID:23635268DOI:10.1118/1.4802750.
Purpose: The authors present a rapid emission angle selection (REAS) method that enables the efficient selection of the azimuthal shield angle for rotating shield brachytherapy (RSBT). The REAS method produces a Pareto curve from which a potential RSBT user can select a treatment plan that balances the tradeoff between delivery time and tumor dose conformity. Methods: Two cervical cancer patients were considered as test cases for the REAS method. The RSBT source considered was a Xoft Axxent(TM) electronic brachytherapy source, partially shielded with 0.5 mm of tungsten, which traveled inside a tandem intrauterine applicator. Three anchor RSBT plans were generated for each case using dose-volume optimization, with azimuthal shield emission angles of 90°, 180°, and 270°. The REAS method converts the anchor plans to treatment plans for all possible emission angles by combining neighboring beamlets to form beamlets for larger emission angles. Treatment plans based on exhaustive dose-volume optimization (ERVO) and exhaustive surface optimization (ErSO) were also generated for both cases. Uniform dwell-time scaling was applied to all plans such that that high-risk clinical target volume D90 was maximized without violating the D2cc tolerances of the rectum, bladder, and sigmoid colon. Results: By choosing three azimuthal emission angles out of 32 potential angles, the REAS method performs about 10 times faster than the ERVO method. By setting D90 to 85-100 Gy10, the delivery times used by REAS generated plans are 21.0% and 19.5% less than exhaustive surface optimized plans used by the two clinical cases. By setting the delivery time budget to 5-25 and 10-30 min∕fx, respectively, for two the cases, the D90 contributions for REAS are improved by 5.8% and 5.1% compared to the ErSO plans. The ranges used in this comparison were selected in order to keep both D90 and the delivery time within acceptable limits. Conclusions: The REAS method enables efficient RSBT treatment planning and delivery and provides treatment plans with comparable quality to those generated by exhaustive replanning with dose-volume optimization.
Study on the Lubricating Properties of Castor ( Ricinus communis) and Hydroxylated Rubber ( Hevea brasiliensis) Seed Oil
ACS Omega 2021 Oct 18;6(43):28471-28476.PMID:34746542DOI:10.1021/acsomega.0c05810.
Rubber seed oil (RSO) (Hevea brasiliensis) was extracted from rubber seeds by chemical means. The effect of temperature on the oil yield was investigated. The experiment suggested that the maximum yield of the oil occurs at 60 °C. This is a result of the proximity to the boiling point of n-hexane, which is about 68 °C. Epoxidized and hydroxylated RSOs were further synthesized by performic acid generated in situ by the reaction of formic acid with 30% hydrogen peroxide. The physiochemical properties of the epoxidized rubber seed oil (ErSO) and hydroxylated rubber seed oil (HRSO) were determined. A separate study was also carried out on castor seed oil (CSO). The improved products were characterized with respect to their configuration and properties. Spectroscopic analysis was carried out on the oil base stocks (RSO, CSO, ErSO, and HRSO). All of the experimental findings were compared with one another. The lubricating properties of CSO and HRSO are further studied as a result of their common hydroxyl nature to ascertain their suitability as a lubricant base. Both oils can be categorized as a nondrying oil with saponification values of 179.52 and 255.25 mgKOH/g, respectively, and as such possess advantageous properties for industrial application. When compared to one another, HRSO appears to be a more effective choice as a lubricant base. This is because of its higher viscosity index of 380.65. The outcomes of this study indicate that hydroxylated and epoxidized RSO with high oxirane content can be synthesized concurrently by one-pot multistep reactions.