LY2334737|cas 892128-60-8|DC Chemicals

LY2334737|cas 892128-60-8|DC Chemicals

LY2334737 is an orally available prodrug of gemcitabine which is a nucleoside analog used as chemotherapy.

Product Name: LY2334737|Cat No. DC9304|cas: 892128-60-8|Other names: LY 2334737,LY-2334737,LY2334737| Molecule formular: C17H25F2N3O5Molecule Weight: 389.39

LY2334737 is an orally available prodrug of gemcitabine which is a nucleoside analog used as chemotherapy.
IC50 Value:
in vitro:  Five cell lines that express CES2 responded to LY2334737treatment. LY2334737 was 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 showed statistically greater PC-3-GFP growth inhibition by LY2334737 when cells were cocultured with CES2 and not mock transfectants.
in vivo: Oral treatment of xenograft models with 3.2 mg/kg LY2334737 once a day for 21 days showed greater tumor growth inhibition of CES2 transfectant than the mock transfectant (P ≤ 0.001). The MTD was 40 mg LY2334737. Fatigue was the most frequent DLT for LY2334737monotherapy (4 patients) followed by elevated transaminase levels (2 patients), both observed at the 40- to 50-mg dose levels. Among the 10 patients in the combination arm, 2 had DLTs at the 40-mg dose level. These were fatigue and elevated liver enzyme levels. Metronomic LY2334737 administration caused 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.