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MedChemExpressModel LY2334737 -892128-60-8

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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[1][2].
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LY2334737

MCE China:LY2334737

Brand:MedChemExpress (MCE)

Cat. No.HY-13672

CAS:892128-60-8

Purity:98.88%

Storage:Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year

Shipping:Room temperature in continental US; may vary elsewhere.

Description: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.

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].

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].

IC50 & Target:Enterovirus A71 (EV-A71)[2] Cellular Effect Cell Line Type Value Description References

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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.  [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]

Brand introduction:
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