LY2334737 |
| رقم الكتالوجGC17522 |
LY2334737 هو نظير نيوكليوزيد وهو دواء مساعد فعال عن طريق الفم من جيمسيتابين
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 892128-60-8
Sample solution is provided at 25 µL, 10mM.
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LY2334737 is an oral prodrug of gemcitabine, the clinically efficacious anticancer agent [1].
LY2334737 has been shown the hydrolytic activity by carboxylesterase 2 (CES2). The Michaelis-Menten kinetic parameters are exhibited to be : Km of 43μM and Vmax of 40nmol/min/mg protein. In addition, LY2334737 has been found to be cytotoxic to cells in the NCl-60 panel with the EC50 values of 0.512±0.016μM, 0.402±0.018μM and 0.034±0.002μM for PC-GFP alone, HCT-116 mock transfectant and HCT-116 CES2 transfectant cell lines, respectively. Apart from these, the study result has been noted that parental SK-OV-3 cells were approximately 4-fold more sensitive to LY2334737 cytotoxicity than the SK-OV-3 knockdown with the EC50 values of 1.1μM and 4.5μM, respectively [1].
References:
[1] Pratt SE1, Durland-Busbice S, Shepard RL, Heinz-Taheny K, Iversen PW, Dantzig AH. 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.
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