LY2334737 is an oral prodrug of gemcitabine, the clinically efficacious anticancer agent .
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 .
 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.
|Storage||Store at -20°C|
|Solubility||Soluble in DMSO|
|Shipping Condition||Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request|
|General tips||For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.|