LY117018 TFA
Based on 1 Customer Validation
LY117018 TFA, a Raloxifene analog, is a selective estrogen receptor modulator. LY117018 TFA exerts antiproliferative effects on breast cancer cell lines.
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- Purity: 99.18%
- CAS No.: 2390041-98-0
- 화학식: C29H26F3NO6S
- 분자량:573.58
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보관:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Biological Activity
LY117018 (0.01-1000 nM; 24 hours) at lower concentrations (0.01-10 nM) caused an E2-like increase in p53 levels when compared to its effects on cells grown in the stripped medium. At a higher concentration of LY117018 (1 μM), the level of p53 appeared to decline. Treatment with 1 μM LY117018 resulted in a predominantly hypophosphorylated pRb. At lower concentrations, LY117018 did not block E2-induced pRb phosphorylation[1].
LY117018 (1 μM; 96 hours) inhibits MCF-7 cells proliferation with an IC50 of 1 μM[2].
LY117018 suppresses oxidative stress-induced endothelial cell apoptosis through activation of ERK1/2 signaling pathway[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2390041-98-0
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Appearance Solid
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분자량 573.58
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화학식 C29H26F3NO6S
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Color Light yellow to green yellow
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SMILES
FC(F)(C(O)=O)F.O=C(C1=CC=C(C=C1)OCCN2CCCC2)C3=C(SC4=CC(O)=CC=C43)C5=CC=C(C=C5)O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
용액&용해도
DMSO : 100 mg/mL (174.34 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 5 mg/mL (8.72 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 5 mg/mL (8.72 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (277 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Dinda S, et al. Effects of LY117018 (a SERM analog of raloxifene) on tumor suppressor proteins and proliferation of breast cancer cells.Horm Mol Biol Clin Investig. 2010 Aug 1;2(1):211-7. [Content Brief]
[2]. Baumann KH, et al. Effects of celecoxib and ly117018 combination on human breast cancer cells in vitro.Breast Cancer (Auckl). 2009 Apr 7;3:23-34. [Content Brief]
[3]. Yu J, et al.Raloxifene analogue LY117018 suppresses oxidative stress-induced endothelial cell apoptosis through activation of ERK1/2 signaling pathway.Eur J Pharmacol. 2008 Jul 28;589(1-3):32-6. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.7434 mL | 8.7172 mL | 17.4344 mL | 43.5859 mL |
| 5 mM | 0.3487 mL | 1.7434 mL | 3.4869 mL | 8.7172 mL | |
| 10 mM | 0.1743 mL | 0.8717 mL | 1.7434 mL | 4.3586 mL | |
| 15 mM | 0.1162 mL | 0.5811 mL | 1.1623 mL | 2.9057 mL | |
| 20 mM | 0.0872 mL | 0.4359 mL | 0.8717 mL | 2.1793 mL | |
| 25 mM | 0.0697 mL | 0.3487 mL | 0.6974 mL | 1.7434 mL | |
| 30 mM | 0.0581 mL | 0.2906 mL | 0.5811 mL | 1.4529 mL | |
| 40 mM | 0.0436 mL | 0.2179 mL | 0.4359 mL | 1.0896 mL | |
| 50 mM | 0.0349 mL | 0.1743 mL | 0.3487 mL | 0.8717 mL | |
| 60 mM | 0.0291 mL | 0.1453 mL | 0.2906 mL | 0.7264 mL | |
| 80 mM | 0.0218 mL | 0.1090 mL | 0.2179 mL | 0.5448 mL | |
| 100 mM | 0.0174 mL | 0.0872 mL | 0.1743 mL | 0.4359 mL |