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[CAS NO. 892128-60-8] LY2334737
| Ships within | Stock | Price | Qty | Total |
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| Catalog: | HY-13672 |
| Brand: | MCE |
| CAS: | 892128-60-8 |
Overview
| MDL | MFCD25976631 |
|---|---|
| Molecular Weight | 389.39 |
| Molecular Formula | C17H25F2N3O5 |
| 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 |
1 Publications Citing Use of MCE
Summary
LY2334737 is an nucleoside analog and is an orally active prodrug of Gemcitabine. LY2334737 exhibits inhibitory activity against enterovirus A71 (EV-A71) infection . LY2334737 has antiviral and anticancer effects [1] [2] .
IC50 & Target
Enterovirus A71 (EV-A71) [2]
In Vitro
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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Oral treatment of xenograft models with 3.2 mg/kg LY2334737 once a day for 21 days shows greater tumor growth inhibition of CES2 transfectant than the mock transfectant
[1]
.
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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT01648764 | Eli Lilly and Company |
Malignant Solid Tumor|Solid Tumor|Metastatic Tumor
|
September 2008 | Phase 1 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : ≥ 100 mg/mL ( 256.81 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.5681 mL | 12.8406 mL | 25.6812 mL |
| 5 mM | 0.5136 mL | 2.5681 mL | 5.1362 mL |
| 10 mM | 0.2568 mL | 1.2841 mL | 2.5681 mL |
References
- [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.
- [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.
- [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.
Synonyms
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