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| Targets |
Yp537 TFA targets the estrogen receptor (ER), specifically blocking the dimerization of human estrogen receptor (hER) monomers. It binds to the SH2-like domain of the receptor, obstructing the process by which sh2-like phosphopeptides couple with hER monomers. By preventing dimerization, Yp537 TFA inhibits the formation of the hER-ERE (estrogen response element) complex, thereby blocking ER-mediated transcriptional activity. It does not prevent the development of the element complex generated by STAT1 serum, indicating selectivity for the ER pathway.
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| ln Vitro |
Yp537 TFA (5-50 μM; 1 hour) eliminates the formation of hER-ERE complexes. and does not prevent the development of the element complex generated by STAT1 serum [1]. By attaching itself to the SH2-like domain, Yp537 TFA obstructs the process that sh2-like phosphopeptides use to couple with hER monomers [1].
In vitro, Yp537 TFA (5-50 microM; 1 hour) abolishes the formation of the hER-ERE complex, indicating that it effectively blocks ER transcriptional activity. By attaching itself to the SH2-like domain, the compound obstructs the process that sh2-like phosphopeptides use to couple with hER monomers. It does not prevent the development of the element complex generated by STAT1 serum, demonstrating specificity for ER. Yp537 TFA is used as a tool to study the mechanism of ER dimerization and to investigate the role of ER signaling in cell proliferation, differentiation, and cancer progression. |
| ln Vivo |
In vivo activity data for Yp537 TFA are not detailed in the provided sources. As an inhibitor of ER dimerization, it has the potential to suppress estrogen-dependent tumor growth in animal models of breast cancer. It could be tested in ovariectomized mouse models with estrogen supplementation and MCF-7 xenografts to evaluate its anti-tumor efficacy. Further studies are required to assess its in vivo bioavailability and therapeutic potential.
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| Enzyme Assay |
For in vitro ER dimerization assays, recombinant human estrogen receptor (hER) protein or cell lysates from ER-expressing cells (e.g., MCF-7) are incubated with Yp537 TFA at concentrations of 1-100 microM for 1 hour at room temperature. The formation of hER dimers is then assessed by chemical cross-linking with a cross-linking reagent (e.g., BS3 or glutaraldehyde) followed by SDS-PAGE and Western blot with ER antibody. The reduction in dimer formation compared to control is quantified by densitometry. For electrophoretic mobility shift assays (EMSA), nuclear extracts from ER-expressing cells are prepared. The extracts are pre-incubated with Yp537 TFA (5-50 microM) for 1 hour, then incubated with a biotinylated or radiolabeled estrogen response element (ERE) probe. The hER-ERE complex is resolved on a native polyacrylamide gel and visualized by chemiluminescence or autoradiography. The reduction in complex formation is quantified.
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| Cell Assay |
For cell-based reporter assays, ER-positive breast cancer cells (e.g., MCF-7) are transiently transfected with an ERE-luciferase reporter construct and a renilla luciferase control. After 24 hours, cells are treated with Yp537 TFA (1-50 microM) in the presence of 1-10 nM estradiol (E2). After an additional 24-48 hours, luciferase activity is measured using a dual-luciferase assay kit. The inhibition of E2-induced reporter activity is calculated. Cytotoxicity is assessed by MTT assay.
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| Animal Protocol |
For in vivo studies, a xenograft mouse model using MCF-7 cells (estrogen-dependent) is commonly used. Mice are ovariectomized and supplemented with estradiol pellets to support tumor growth. Yp537 TFA would be formulated in a suitable vehicle (e.g., PBS or a DMSO-based formulation) and administered via intraperitoneal or subcutaneous injection at doses of 5-50 mg/kg, once daily or on a schedule determined by pilot studies. Tumor volume is measured with calipers twice weekly. At study termination, tumors are excised and analyzed for ER signaling markers (e.g., progesterone receptor expression) by Western blot or immunohistochemistry.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for Yp537 TFA are limited. The compound has a molecular weight of 1584.65, with a molecular formula of C66H105F3N13O24PS. It is soluble in water at approximately 9.09 mg/mL (5.74 mM). For in vivo use, a formulation of DMSO, PEG300, Tween-80, and saline can be used. The compound is a peptide-based inhibitor, and as such, it is likely to have a short half-life in circulation due to proteolytic degradation. Researchers should conduct pilot PK studies to determine its half-life, Cmax, and bioavailability. Yp537 TFA should be stored as a powder at -20degC in a sealed, protected environment (e.g., under nitrogen), away from moisture and light.
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| Toxicity/Toxicokinetics |
Toxicological data for Yp537 TFA are limited. In cell-based assays at concentrations up to 50 microM, no overt cytotoxicity is reported. However, as an ER inhibitor, off-target effects on other steroid hormone receptors or signaling pathways should be considered. Comprehensive toxicology studies have not been published. Standard safety precautions should be followed.
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| References | |
| Additional Infomation |
Yp537 TFA is a research-grade compound and is not approved for clinical use. It is an estrogen receptor (ER) inhibitor that specifically blocks dimerization of the human estrogen receptor, a novel mechanism of action distinct from classical ER antagonists like tamoxifen (which binds to the ligand-binding domain). Yp537 TFA binds to the SH2-like domain, preventing receptor dimerization and subsequent DNA binding. This compound is a valuable tool for dissecting the molecular mechanisms of ER signaling and for developing new therapeutic strategies for ER-positive breast cancer. The related CAS number for the free base (Yp537) is 166664-90-0. Store at -20degC as a powder, protected from light and moisture.
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| Molecular Formula |
C66H105F3N13O24PS
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| Molecular Weight |
1584.65
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| Related CAS # |
Yp537;166664-90-0
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| Appearance |
White to off-white solid powder
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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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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) |
H2O :~9.09 mg/mL (~5.74 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.6311 mL | 3.1553 mL | 6.3105 mL | |
| 5 mM | 0.1262 mL | 0.6311 mL | 1.2621 mL | |
| 10 mM | 0.0631 mL | 0.3155 mL | 0.6311 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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