LY2334737
Based on 2 publication(s) in Google Scholar
LY2334737 is an nucleoside analog and is an orally active proagent of Gemcitabine. LY2334737 exhibits inhibitory activity against enterovirus A71 (EV-A71) infection. LY2334737 has antiviral and anticancer effects.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.55%
- No. CAS: 892128-60-8
- Fòrmula: C17H25F2N3O5
- Peso molecular:389.39
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) LY2334737
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Actividad biológica
Enterovirus A71 (EV-A71)[2]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CCRF-CEM | IC50 |
161 μM
Compound: 1, LY2334737
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Cytostatic activity against human dCK-deficient CEM cells after 3 days by coulter counter analysis
Cytostatic activity against human dCK-deficient CEM cells after 3 days by coulter counter analysis
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[PMID: 24341356] |
| CCRF-CEM | IC50 |
5.2 μM
Compound: 1, LY2334737
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Cytostatic activity against human CEM cells after 3 days by coulter counter analysis
Cytostatic activity against human CEM cells after 3 days by coulter counter analysis
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[PMID: 24341356] |
| HeLa | IC50 |
0.76 μM
Compound: 1, LY2334737
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Cytostatic activity against human HeLa cells after 4 days by coulter counter analysis
Cytostatic activity against human HeLa cells after 4 days by coulter counter analysis
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[PMID: 24341356] |
| L1210 | IC50 |
1.1 μM
Compound: 1, LY2334737
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Cytostatic activity against mouse L1210 cells after 2 days by coulter counter analysis
Cytostatic activity against mouse L1210 cells after 2 days by coulter counter analysis
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[PMID: 24341356] |
| MCF7 | IC50 |
0.55 μM
Compound: 1, LY2334737
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Cytostatic activity against human MCF7 cells after 2 days by coulter counter analysis
Cytostatic activity against human MCF7 cells after 2 days by coulter counter analysis
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[PMID: 24341356] |
Five cell lines that express CES2 responded to LY2334737 treatment. LY2334737 is less cytotoxic to a SK-OV-3 CES2 knockdown than parental cells. The drug response of CES2-transfected HCT-116 cells correlated with CES2 expression level. Bystander studies show statistically greater PC-3-GFP growth inhibition by LY2334737 when cells are cocultured with CES2 and not mock transfectants[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Metronomic LY2334737 administration causes increased blood flow in luciferase-tagged LM2-4 tumor xenografts, and this effect, readily measured using contrast micro-ultrasound, coincided with a relative increase in tumor bioluminescence[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 892128-60-8
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Appearance Solid
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Peso molecular 389.39
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Fòrmula C17H25F2N3O5
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Color White to off-white
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SMILES
OC[C@@H]1[C@H](C(F)(F)[C@H](N2C(N=C(C=C2)NC(C(CCC)CCC)=O)=O)O1)O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
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Sci Rep
Drug repurposing of pyrimidine analogs as potent antiviral compounds against human enterovirus A71 infection with potential clinical applications. [Abstract]2020 May 18;10(1):8159. PMID: 32424333 -
ACS Infect Dis
Targeting the Rift Valley Fever Virus Polymerase: Resistance Mechanisms and Structural Insights. [Abstract]2025 Oct 30. PMID: 41166549
Solvente y solubilidad
DMSO : ≥ 100 mg/mL (256.81 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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: ≥ 2.5 mg/mL (6.42 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (6.42 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
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.
Pureza y Documentación
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Ficha de datos (274 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
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- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Pratt SE, et al. Human carboxylesterase-2 hydrolyzes the prodrug of gemcitabine (LY2334737) and confers prodrug sensitivity to cancer cells. Clin Cancer Res. 2013 Mar 1;19(5):1159-68. [Content Brief]
[2]. Jialei Sun, et al. Drug Repurposing of Pyrimidine Analogs as Potent Antiviral Compounds Against Human Enterovirus A71 Infection With Potential Clinical Applications. Sci Rep. 2020 May 18;10(1):8159. [Content Brief]
[3]. Francia G, et al. Low-dose metronomic oral dosing of a prodrug of gemcitabine (LY2334737) causes antitumor effects in the absence of inhibition of systemic vasculogenesis. Mol Cancer Ther. 2012 Mar;11(3):680-9. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.5681 mL | 12.8406 mL | 25.6812 mL | 64.2030 mL |
| 5 mM | 0.5136 mL | 2.5681 mL | 5.1362 mL | 12.8406 mL | |
| 10 mM | 0.2568 mL | 1.2841 mL | 2.5681 mL | 6.4203 mL | |
| 15 mM | 0.1712 mL | 0.8560 mL | 1.7121 mL | 4.2802 mL | |
| 20 mM | 0.1284 mL | 0.6420 mL | 1.2841 mL | 3.2101 mL | |
| 25 mM | 0.1027 mL | 0.5136 mL | 1.0272 mL | 2.5681 mL | |
| 30 mM | 0.0856 mL | 0.4280 mL | 0.8560 mL | 2.1401 mL | |
| 40 mM | 0.0642 mL | 0.3210 mL | 0.6420 mL | 1.6051 mL | |
| 50 mM | 0.0514 mL | 0.2568 mL | 0.5136 mL | 1.2841 mL | |
| 60 mM | 0.0428 mL | 0.2140 mL | 0.4280 mL | 1.0700 mL | |
| 80 mM | 0.0321 mL | 0.1605 mL | 0.3210 mL | 0.8025 mL | |
| 100 mM | 0.0257 mL | 0.1284 mL | 0.2568 mL | 0.6420 mL |
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