LY2334737

SKU: orb1303216

Description

LY2334737 is an orally administered prodrug of the antimetabolite gemcitabine. It is designed to improve bioavailability and is used in oncology research to study its antitumor effects in both in vitro and in vivo experimental models.

Research Area

Cell Biology, Infectious Disease & Virology, Molecular Biology

Key Properties

• CAS Number: 892128-60-8
• MW: 389.39
• Purity: >99.99% (May vary between batches)
• Formula: C₁₇H₂₅F₂N₃O₅
• SMILES: CCCC(CCC)C(=O)Nc1ccn([C@@H]2O[C@H](CO)[C@@H](O)C2(F)F)c(=O)n1
• Target: Virus Protease,Nucleoside Antimetabolite/Analog
• Solubility: DMSO:45 mg/mL (115.57 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.14 mM)

Bioactivity

• 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) . 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 . 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 .
• 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 .

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

anticancer, antiviral, Analog, Inhibitor, HEVs, HEV, Gemcitabine, HRV, HRVs, Enterovirus, EV-A71, inhibit, LY2334737, LY-2334737, LY 2334737, NucleosideAntimetabolite, Nucleoside Antimetabolite, Nucleoside Antimetabolite/Analog, orally, Rhinovirus, Virus Protease, VirusProtease

Compound Identifiers

PubChem CID

11646777