| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
Erteberel targets the estrogen receptor beta (ERβ) with high affinity and selectivity. It exhibits a Ki of 0.19 nM and an EC50 of 0.66 nM for ERβ, with 32-fold selectivity over ERα. The compound binds to ERβ and activates estrogen-responsive gene transcription through this receptor subtype, promoting apoptosis in susceptible cell types such as glioblastoma cells.
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| ln Vitro |
In vitro, Erteberel treatment (0.25-10 μM, 72 hours) significantly inhibited GBM cell proliferation but had no effect on normal astrocytes [2]. Erteberel induces apoptosis in GBM cells. Erteberel affects several processes linked to the cell cycle, DNA damage response, and apoptosis [2]. Erteberel (0-1000 μM) sensitizes GBM cells to a number of chemotherapeutic medications that are licensed by the FDA, such as temozolomide, lomustine, and cisplatin [2].
In vitro, Erteberel promotes apoptosis of glioblastoma (GBM) cells through ERβ-mediated signaling. The compound shows potent binding affinity for both ER subtypes in competitive binding assays using ³H-estradiol and recombinant full-length human estrogen receptors. It activates ERβ-dependent gene transcription and induces cell death in GBM cell lines. |
| ln Vivo |
Erteberel treatment (5 mg/Kg body weight/day, oral, for 28 days) significantly slowed tumor growth and increased GBM tumor cell apoptosis in an orthotopic model [2]. In the GL26 syngeneic glioma model, ERTEBEL (5 mg/Kg body weight/day, oral, 40–50 days) treatment increases the overall survival of tumor-bearing mice [2].
In vivo, Erteberel (5 mg/kg/day, oral, 28 days) significantly reduces tumor growth and promotes apoptosis of GBM tumors in an orthotopic mouse model. The compound demonstrates efficacy in preclinical cancer models by activating ERβ-mediated pathways that suppress tumor progression and induce programmed cell death. |
| Enzyme Assay |
For receptor binding assays, recombinant full-length human ERα and ERβ are incubated with ³H-estradiol and varying concentrations of Erteberel. Non-specific binding is determined using excess unlabeled estradiol. After incubation, bound and free radioligand are separated using charcoal-dextran or filtration methods, and radioactivity is counted to determine Ki values.
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| Cell Assay |
Cell Viability Assay[2]
Cell Types: U87, U251, T98G and normal astrocytes Tested Concentrations: 0.25, 0.5, 1, 2, 4, 6, 8 and 10 μM Incubation Duration: 72 hrs (hours) Experimental Results: Erteberel treatment Dramatically diminished viability was studied in various GBM cell lines in a dose-dependent manner. In contrast, the viability of normal astrocytes was not affected at the tested doses, indicating that Erteberel has tumor cell-specific activity [2]. Cellular assays utilize glioblastoma cell lines or other cells expressing endogenous or transfected ERβ. Cells are treated with Erteberel (typically 0.001-10 μM) for 24-72 hours. Cell viability is measured using MTT or CellTiter-Glo assays. Apoptosis is assessed by Annexin V/PI flow cytometry, caspase-3/7 activity assays, or TUNEL staining. ERβ target gene expression is confirmed by qPCR or Western blot. |
| Animal Protocol |
Animal/Disease Models: Athymic mice (5-7 weeks) vaccinated with OVCAR-3 cells [2]
Doses: 5 mg/kg body weight Route of Administration: Orally, one time/day for 28 days Experimental Results: Immunohistochemical analysis demonstrated that Erteberel Treatment Dramatically diminished the number of proliferation marker Ki-67-positive cells and increased the number of TUNEL-positive apoptotic cells [2]. In vivo studies are performed using orthotopic GBM mouse models. Erteberel is administered orally at 5 mg/kg/day for 28 days. Tumor growth is monitored by bioluminescence imaging or MRI. At study termination, tumors are harvested for histopathological analysis including H&E staining, Ki-67 immunohistochemistry for proliferation, and TUNEL staining for apoptosis. |
| ADME/Pharmacokinetics |
Erteberel (molecular weight 282.33) is orally bioavailable with favorable pharmacokinetic properties. It is soluble in DMSO and ethanol but insoluble in water. For in vivo administration, the compound can be formulated as a homogeneous suspension in CMC-Na or as a clear solution in DMSO/PEG300/Tween 80/ddH2O.
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| Toxicity/Toxicokinetics |
Preclinical toxicity studies have indicated that Erteberel is well-tolerated at therapeutic doses. The compound's selectivity for ERβ over ERα reduces the risk of classical estrogen-associated toxicities such as uterine proliferation and breast epithelial stimulation. No significant adverse effects have been reported at the doses used in preclinical efficacy studies.
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| References |
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| Additional Infomation |
Erteberel is an estrogen receptor beta agonist that has been used in trials investigating the treatment of benign prostatic hyperplasia.
Erteberel (LY500307) is a selective ERβ agonist that was in Phase 2 clinical development. Its mechanism involves activation of ERβ, which acts as a tumor suppressor in various cancer types including glioblastoma, prostate, and breast cancer. By selectively activating ERβ, the compound induces apoptosis and inhibits proliferation without the side effects associated with ERα activation. Clinical trials have explored its potential in glioblastoma and other indications. |
| Molecular Formula |
C18H18O3
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|---|---|
| Molecular Weight |
282.333725452423
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| Exact Mass |
282.125
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| CAS # |
533884-09-2
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| Related CAS # |
(-)-Erteberel; 533884-08-1; rel-Erteberel
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| PubChem CID |
10286159
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| Appearance |
Off-white to light brown solid powder
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| Density |
1.268
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| Boiling Point |
485.2±45.0 °C at 760 mmHg
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| Flash Point |
247.3±28.7 °C
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| Vapour Pressure |
0.0±1.3 mmHg at 25°C
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| Index of Refraction |
1.639
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| LogP |
3.84
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
21
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| Complexity |
364
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| Defined Atom Stereocenter Count |
3
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| SMILES |
C1C[C@H]2[C@@H](C1)C3=C(C=CC(=C3)O)O[C@H]2C4=CC=C(C=C4)O
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| InChi Key |
XIESSJVMWNJCGZ-VKJFTORMSA-N
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| InChi Code |
InChI=1S/C18H18O3/c19-12-6-4-11(5-7-12)18-15-3-1-2-14(15)16-10-13(20)8-9-17(16)21-18/h4-10,14-15,18-20H,1-3H2/t14-,15+,18+/m1/s1
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| Chemical Name |
(3aS,4R,9bR)-4-(4-hydroxyphenyl)-1,2,3,3a,4,9b-hexahydrocyclopenta[c]chromen-8-ol
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| Synonyms |
LY500307; LY-500307; LY 500307
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ≥ 30 mg/mL (~106.26 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.85 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), Clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (8.85 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), Clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 3: ≥ 2.5 mg/mL (8.85 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), Clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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