| 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 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 45 mg/mL (115.56 mM)
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| Keywords | anticancer | LY-2334737 | HEV | Gemcitabine | HEVs | HRVs | EV-A71 | Rhinovirus | inhibit | LY 2334737 | Nucleoside Antimetabolite/Analog | Enterovirus | HRV | orally | LY2334737 | antiviral | Inhibitor |
| Inhibitors Related | Stavudine | 5-Fluorouracil | EIDD-1931 | Phenytoin sodium | Anthraquinone | Aspirin | L-Lysine | 2-Phenylethanol | L-Lysine hydrochloride | 5-BrdU | (-)-α-Pinene | 4-Phenylbutyric acid |
| Related Compound Libraries | Bioactive Compound Library | Anti-Cancer Clinical Compound Library | Anti-Viral Compound Library | Drug Repurposing Compound Library | Orally Active Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Anti-Cancer Drug Library | Anti-Cancer Active Compound Library | Nucleotide Compound Library |
United States
