| Name | LY2334737 |
| Description | LY2334737 is an orally available prodrug of gemcitabine with antineoplastic activity. |
| In vitro | Five cell lines expressing CES2 responded to LY2334737 treatment, which was less cytotoxic to SK-OV-3 CES2 knockdown than to parental cells. CES2-transfected HCT-116 cell drug response correlated with CES2 expression level. Bystander studies showed significantly greater PC-3-GFP growth inhibition by LY2334737 when cocultured with CES2, not mock transfectants [1]. |
| In vivo | Oral treatment of xenograft models with 3.2 mg/kg LY2334737 once daily for 21 days showed significantly greater tumor growth inhibition in CES2 transfectants compared to mock transfectants (P ≤ 0.001) [1]. The MTD was 40 mg LY2334737. Fatigue was the most frequent DLT for LY2334737 monotherapy (4 patients), followed by elevated transaminase levels (2 patients), both observed at the 40-50 mg dose levels. In the combination arm, 2 of 10 patients experienced DLTs at the 40 mg dose level, which included fatigue and elevated liver enzyme levels [2]. Metronomic LY2334737 administration increased blood flow in luciferase-tagged LM2-4 tumor xenografts, measurable via contrast micro-ultrasound, and coincided with a relative increase in tumor bioluminescence [3]. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 45 mg/mL (115.57 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (5.14 mM), Sonication is recommended.
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| Keywords | VirusProtease | Virus Protease | Rhinovirus | orally | NucleosideAntimetabolite | Nucleoside Antimetabolite/Analog | Nucleoside Antimetabolite | LY-2334737 | LY2334737 | LY 2334737 | Inhibitor | inhibit | HRVs | HRV | HEVs | HEV | Gemcitabine | EV-A71 | Enterovirus | antiviral | anticancer | Analog |
| Inhibitors Related | Stavudine | Rifampicin | 5-Fluorouracil | Phenytoin sodium | Uridine | Capecitabine | L-Lysine | L-Lysine hydrochloride | Ofloxacin | Vidarabine | Thymidine | Danthron |
| Related Compound Libraries | Bioactive Compound Library | ReFRAME Related Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Anti-Viral Compound Library | Orally Active Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Cell Cycle Compound Library | Anti-Infection Compound Library | Anti-Cancer Active Compound Library | Anti-Cancer Drug Library |
United States
