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PRODUCT INFORMATION Erteberel Item No. 22130 OH CAS Registry No.: 533884-09-2 Formal Name: (3aS,4R,9bR)-1,2,3,3a,4,9b-hexahydro-4-(4- H hydroxyphenyl)-cyclopenta[c][1]benzopyran-8-ol Synonym: LY500307 O MF: C18H18O3 H FW: 282.3 Purity: ≥98% UV/Vis.: λmax: 225 nm Supplied as: A crystalline solid Storage: -20°C OH Stability: ≥2 years Information represents the product specifications. Batch specific analytical results are provided on each certificate of analysis. Laboratory Procedures Erteberel is supplied as a crystalline solid. A stock solution may be made by dissolving the erteberel in the solvent of choice. Erteberel is soluble in organic solvents such as ethanol, DMSO, and dimethyl formamide, which should be purged with an inert gas. The solubility of erteberel in these solvents is approximately 30 mg/ml. Description Erteberel is a potent and selective agonist of estrogen receptor β (ERβ; Ki = 1.54 nM; 1 + EC50 = 3.61 nM). Erteberel reduces the viability of patient-derived, ERβ primary glioblastoma (GBM) cells, 2 significantly reducing in vitro colony formation and inducing apoptosis. It induces G2/M arrest and sensitizes GBM cells to the chemotherapeutic agents cisplatin (Item No. 13119), lomustine, and temozolomide (Item No. 14163) in vitro. Treatment with erteberel reduces GBM progression in and increases survival of orthotopic and syngeneic GBM mouse models. Erteberel also induces dose-dependent reduction in prostate weight with no effect on levels of circulating testosterone (Item Nos. 15645 | ISO60154) or dihydrotestosterone (Item No. 15874) in a rat model of benign prostatic hyperplasia (BPH).1 Formulations containing erteberel have been tested in phase II clinical trials for treatment of BPH in healthy men.3 References 1. Norman, B.H., Dodge, J.A., Richardson, T.I., et al. Benzopyrans are selective estrogen receptor beta agonists with novel activity in models of benign prostatic hyperplasia. J. Med. Chem. 49(21), 6155-6157 (2006). 2. Sareddy, G.R., Li, X., Liu, J., et al. Selective estrogen receptor β agonist LY500307 as a novel therapeutic agent for glioblastoma. Sci. Rep. 6:24185, (2016). 3. Roehrborn, C.G., Spann, M.E., Myers, S.L., et al. Estrogen receptor beta agonist LY500307 fails to improve symptoms in men with enlarged prostate secondary to benign prostatic hypertrophy. Prostate Cancer Prostatic Dis. 18(1), 43-48 (2015). WARNING CAYMAN CHEMICAL THIS PRODUCT IS FOR RESEARCH ONLY - NOT FOR HUMAN OR VETERINARY DIAGNOSTIC OR THERAPEUTIC USE. 1180 EAST ELLSWORTH RD SAFETY DATA ANN ARBOR, MI 48108 · USA This material should be considered hazardous until further information becomes available. Do not ingest, inhale, get in eyes, on skin, or on clothing. Wash thoroughly after handling. Before use, the user must review the complete Safety Data Sheet, which has been sent via email to your institution. PHONE: [800] 364-9897 WARRANTY AND LIMITATION OF REMEDY [734] 971-3335 Buyer agrees to purchase the material subject to Cayman’s Terms and Conditions. Complete Terms and Conditions including Warranty and Limitation of Liability information can be found on our website. FAX: [734] 971-3640 [email protected] Copyright Cayman Chemical Company, 11/14/2017 WWW.CAYMANCHEM.COM.

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Erteberel (LY500307) Product Data Sheet
Product Name: Erteberel (LY500307) Revision Date: 01/10/2021 Product Data Sheet Erteberel (LY500307) Cat. No.: B1518 CAS No.: 533884-09-2 Formula: C18H18O3 M.Wt: 282.33 Synonyms: Target: Endocrinology and Hormones Pathway: Estrogen/progestogen Receptor Storage: Store at -20°C Solvent & Solubility insoluble in H2O; ≥14.1 mg/mL in DMSO; ≥48.3 mg/mL in EtOH Mass Solvent 1mg 5mg 10mg Preparing Concentration In Vitro Stock Solutions 1 mM 3.5420 mL 17.7098 mL 35.4195 mL 5 mM 0.7084 mL 3.5420 mL 7.0839 mL 10 mM 0.3542 mL 1.7710 mL 3.5420 mL Please refer to the solubility information to select the appropriate solvent. Biological Activity Shortsummary ERβ agonist, potent and selective IC₅₀ & Target Cell Viability Assay Cell Line: Human prostate cancer cell line (PC-3 cells) Preparation method： The solubility of this compound in DMSO is >10 mM. General tips for obtaining In Vitro a higher concentration: Please warm the tube at 37°C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months. Reacting conditions: N/A 1 | www.apexbt.com Applications: Erteberel showed potent and selective binding affinity for ERβ with EC50 value of 0.66 nM [1]. Animal experiment Animal models: Male and female rat fertility and rat and rabbit embryo-fetal development model Dosage form: 0.03 to 10 mg/kg/day for rats, or 1 to 25 mg/kg/day for rabbits, oral gavage, for 2 or 10 weeks Applications: There were no-observed adverse effect levels following LY500307 In Vivo administration of 1 mg/kg/day for male rat fertility, 0.3 mg/kg/day for female rat fertility and embryo-fetal development, and 25 mg/kg/day for rabbit embryo-fetal development [2].
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Supplementary Information
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US 20200187851A1TE INI (19 ) United States (12 ) Patent Application Publication ( 10) Pub . No .: US 2020/0187851 A1 Offenbacher et al. (43 ) Pub . Date : Jun . 18 , 2020 ( 54 ) PERIODONTAL DISEASE STRATIFICATION (52 ) U.S. CI. AND USES THEREOF CPC A61B 5/4552 (2013.01 ) ; G16H 20/10 ( 71) Applicant: The University of North Carolina at ( 2018.01) ; A61B 5/7275 ( 2013.01) ; A61B Chapel Hill , Chapel Hill , NC (US ) 5/7264 ( 2013.01 ) ( 72 ) Inventors: Steven Offenbacher, Chapel Hill , NC (US ) ; Thiago Morelli , Durham , NC ( 57 ) ABSTRACT (US ) ; Kevin Lee Moss, Graham , NC ( US ) ; James Douglas Beck , Chapel Described herein are methods of classifying periodontal Hill , NC (US ) patients and individual teeth . For example , disclosed is a method of diagnosing periodontal disease and / or risk of ( 21) Appl. No .: 16 /713,874 tooth loss in a subject that involves classifying teeth into one of 7 classes of periodontal disease. The method can include ( 22 ) Filed : Dec. 13 , 2019 the step of performing a dental examination on a patient and Related U.S. Application Data determining a periodontal profile class ( PPC ) . The method can further include the step of determining for each tooth a ( 60 ) Provisional application No.62 / 780,675 , filed on Dec. Tooth Profile Class ( TPC ) . The PPC and TPC can be used 17 , 2018 together to generate a composite risk score for an individual, which is referred to herein as the Index of Periodontal Risk Publication Classification ( IPR ) . In some embodiments , each stage of the disclosed (51 ) Int. Cl. PPC system is characterized by unique single nucleotide A61B 5/00 ( 2006.01 ) polymorphisms (SNPs ) associated with unique pathways , G16H 20/10 ( 2006.01 ) identifying unique druggable targets for each stage .
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Mitochondrial estrogen receptors alter mitochondrial priming and response to endocrine therapy in breast cancer cells. Ozgur Kutuk ( [email protected] ) Başkent University, Adana Dr. Turgut Noyan Medical and Research Center https://orcid.org/0000-0001- 9854-7220 Bahriye Karakas Sabanci University Yeliz Aka Baskent University Asli Giray Alanya Alaaddin Keykubat University Huveyda Basaga Sabanci University Ufuk Acikbas Baskent University Ozgur Gul Bilgi University Sehime Gulsun Temel Uludag University Article Keywords: breast cancer, BH3, Estrogen receptor, mitochondrial estrogen signaling Posted Date: February 5th, 2021 DOI: https://doi.org/10.21203/rs.3.rs-139821/v1 License: This work is licensed under a Creative Commons Attribution 4.0 International License. Read Full License Page 1/29 Abstract Breast cancer is the most common cancer with a high rate of mortality and morbidity among women worldwide. Estrogen receptor status is an important prognostic factor and endocrine therapy is the choice of rst-line treatment in ER-positive breast cancer. However, most tumors develop resistance to endocrine therapy. Here we demonstrate that BH3 proling technology, in particular dynamic BH3 proling can predict the response to endocrine therapy agents as well as development of acquired resistance in breast cancer cells independent of estrogen receptor status. Immunouorescence analysis and subcellular fractionation experiments revealed distinct ER-α and ER-β subcellular localization patterns in breast cancer cells, including mitochondrial localization of both receptor subtypes. shRNA-mediated depletion of ER-β in breast cancer cells led to resistance to endocrine therapy agents and selective reconstitution of ER-β in mitochondria restored sensitivity. Notably, mitochondria-targeted ER-α did not restore sensitivity, even conferred further resistance to endocrine therapy agents.
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Mitochondrial Estrogen Receptors Alter Mitochondrial Priming and Response to Endocrine Therapy in Breast Cancer Cells
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Inhibitor United States China Toll Free: +1 877 796-6397 Toll Free: 400-668-6834 Fax: +1 832 582-8590 Fax: 021-68591981 E-mail: [email protected] E-mail: [email protected] Europe Japan Tel: +49-89-46148500 Tel: + 81 3-5632-9610 Fax: +49-89-461485022 Fax: + 81 3-5632-9619 E-mail: [email protected] E-mail: [email protected] Protein Tyrosine Kinase PI3K/Akt/mTOR MAPK Inhibitors Cytoskeletal Signaling Selleck Chemicals supplies over 3,000 Apoptosis + inhibitors used in the study of cell 3000 Epigenetics Cell Cycle Inhibitors signaling pathways. Ubiquitin Signaling DNA Damage Stem Others Cells Neuronal Signaling Product Citations Selleck products have been cited in more than 12000 studies from various SCI journals. (Cell, Nature, Science: 61 studies) Compound Libraries Bioactive Compound Library 2659 compounds Nature. 2017, 541(7638):481-487. Nature. 2015, 521(7552):357-61. Science. 2016, 354(6315). Nature. 2017, 10.1038/nature21064. Nature. 2015, 521(7552):316-21. Science. 2016, 353(6302):929-32. Kinase Inhibitor Library Nature. 2016, 540(7631):119-123. Nature. 2015, 520(7549):683-7. Science. 2016, 352(6283):353-8. 430 inhibitors Nature. 2016, 539(7629):437-442. Nature. 2015, 520(7547):368-72. Science. 2016, 352(6282):189-96. Nature. 2016, 539(7628):304-308. Nature. 2015, 519(7543):370-3. Science. 2016, 351(6277):aad3680. FDA-approved Drug Library 1443 compounds Nature. 2016, 539(7627):54-58. Nature. 2015, 518(7538):254-7. Science. 2013, 341(6146):651-4. Nature. 2016, 538(7626):477-482. Nature. 2015, 517(7536):583-8.
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Potency Price List
Potency List Published 06.02.2021 # of Actives Turnaround Time (in business days) Tested Standard Rush* Super Rush 1-3 See Table Below See Table Below See Table Below Potency 4-8 1 day/active 0.5 day/active Call for TAT 9+ Call for TAT Call for TAT Call for TAT 1-3 Add 1 Day to Table Below Add 1 Day to Table Below Add 1 Day to Table Below Potency (Cream/Gel/Ointment) 4-8 10 5 Call for TAT 9+ Call for TAT Call for TAT Call for TAT Standard Rush Super Rush Active Days Price Days Price Days Price Notes 2-Methoxyestradiol 3 $210 1 $315 0 $420 Client to provide starting material or pay for standard 4-Aminophenol 3 $160 1 $240 0 $320 4-Aminopyridine 3 $160 1 $240 0 $320 5-Aminosalicylic Acid 3 $160 1 $240 0 $320 5-Fluorouracil 3 $260 1 $390 0 $520 5- Hydroxytryptophan 3 $160 1 $240 0 $320 5-Methyltetrahydrofolate 3 $210 1 $315 0 $420 Client to provide starting material or pay for standard 7-Keto DHEA 3 $160 1 $240 0 $320 7-Hydroxymitragynine 3 $210 1 $315 0 $420 Client to provide starting material or pay for standard 13C - Urea 3 $710 1 $1,065 0 $1,420 Client to provide starting material or pay for standard 6,6 D2-Glucose 3 $210 1 $315 0 $420 Acebutolol 3 $160 1 $240 0 $320 Acepromazine 3 $160 1 $240 0 $320 Acepromazine Maleate 3 $160 1 $240 0 $320 Acetaminophen 3 $160 1 $240 0 $320 Acetate 3 $160 1 $240 0 $320 Acetazolamide 3 $160 1 $240 0 $320 Acetic Acid 3 $160 1 $240 0 $320 Acetohydroxamic Acid 3 $210 1 $315 0 $420 Acetyl Glucosamine 3 $160 1 $240 0 $320 Acetyl Hexapeptide 3 $210 1 $315 0 $420 Client to provide starting material or pay for standard Acetylcholine Chloride 3 $210 1 $315 0 $420 Client to provide starting material or pay for standard Acetylcysteine 3 $160 1 $240 0 $320 Drug list may not include consumables such as columns, standards, and special handling requests.
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Androgen Receptor
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GSK3B Regulates Epithelial-Mesenchymal Transition and Cancer Stem Cell Properties and Is a Novel Drug Target for Triple-Negative Breast Cancer
The Texas Medical Center Library DigitalCommons@TMC The University of Texas MD Anderson Cancer Center UTHealth Graduate School of The University of Texas MD Anderson Cancer Biomedical Sciences Dissertations and Theses Center UTHealth Graduate School of (Open Access) Biomedical Sciences 8-2017 GSK3B regulates epithelial-mesenchymal transition and cancer stem cell properties and is a novel drug target for triple-negative breast cancer Geraldine Vidhya Raja Follow this and additional works at: https://digitalcommons.library.tmc.edu/utgsbs_dissertations Part of the Life Sciences Commons, and the Medicine and Health Sciences Commons Recommended Citation Raja, Geraldine Vidhya, "GSK3B regulates epithelial-mesenchymal transition and cancer stem cell properties and is a novel drug target for triple-negative breast cancer" (2017). The University of Texas MD Anderson Cancer Center UTHealth Graduate School of Biomedical Sciences Dissertations and Theses (Open Access). 806. https://digitalcommons.library.tmc.edu/utgsbs_dissertations/806 This Dissertation (PhD) is brought to you for free and open access by the The University of Texas MD Anderson Cancer Center UTHealth Graduate School of Biomedical Sciences at DigitalCommons@TMC. It has been accepted for inclusion in The University of Texas MD Anderson Cancer Center UTHealth Graduate School of Biomedical Sciences Dissertations and Theses (Open Access) by an authorized administrator of DigitalCommons@TMC. For more information, please contact [email protected]. GSK3β REGULATES EPITHELIAL-MESENCHYMAL TRANSITION AND CANCER STEM CELL PROPERTIES AND IS A NOVEL DRUG TARGET FOR TRIPLE-NEGATIVE BREAST CANCER. by Geraldine Vidhya Raja, MS. APPROVED: ______________________________ Sendurai Mani, Ph.D. Advisory Professor ______________________________ Joya Chandra, Ph.D. ______________________________ Jonathan Kurie, MD.
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