| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| Other Sizes |
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| ln Vitro |
In MCF7, MD-134, HCC1500, and CAMA cells, GNE-274 (0.1 nM-1000 nM; 4 hours) is unable to cause an increase in ER turnover[1]. In E2-stimulated ER+ breast cancer cell lines, GNE-274 (1-1000 nM; 7-10 days) is more powerful than fulvestrant, 4-OHT, AZD9496, and GDC-0810 in its ability to decrease cellular proliferation[1]. In the transposaseaccessible chromatin sequencing (ATAC-seq) test, GNE-274 dramatically modifies chromatin accessibility at 594 locations and increases chromatin accessibility at ER-DNA binding sites. However, GDC-0927 has a far smaller effect on chromatin accessibility[1].
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: MCF7, MB-134, HCC1500, EFM-19 , CAMA-1, T-47D cells Tested Concentrations: 1 nM; 10 nM; 100 nM; 1000 nM Incubation Duration: 7-10 days Experimental Results: demonstrated IC50 values approximately ranging from 5nM to 20 nM in different cells. |
| References |
[1]. Jane Guan, et al. Therapeutic Ligands Antagonize Estrogen Receptor Function by Impairing Its Mobility. Cell. 2019 Aug 8;178(4):949-963.e18.
[2]. Jane Guan, et al. Abstract NG05: Not all “SERDs” are equal: Context-independent ER degradation and full ER antagonism define the next generation of ER therapeutics. Cancer research. |
| Molecular Formula |
C29H31NO4
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|---|---|
| Molecular Weight |
457.56
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| CAS # |
2369048-69-9
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| Related CAS # |
(R)-GNE-274
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| SMILES |
[C@@H]1(C2=CC=C(OCC3CN(CCC)C3)C=C2)OC2=CC=C(O)C=C2C(C)=C1C1=CC=CC(O)=C1
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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: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| 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: 200 mg/mL (437.10 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 1.75 mg/mL (3.82 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 17.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to 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: 1.75 mg/mL (3.82 mM) 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; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 17.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1855 mL | 10.9275 mL | 21.8551 mL | |
| 5 mM | 0.4371 mL | 2.1855 mL | 4.3710 mL | |
| 10 mM | 0.2186 mL | 1.0928 mL | 2.1855 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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