LY2334737
LY2334737 Basic information
- Product Name:
- LY2334737
- Synonyms:
-
- LY2334737
- 2'-Deoxy-2',2'-difluoro-N-(1-oxo-2-propylpentyl)cytidine
- LY 2334737;LY-2334737;LY2334737
- Cytidine, 2'-deoxy-2',2'-difluoro-N-(1-oxo-2-propylpentyl)-
- anticancer,HEV,Gemcitabine,HEVs,HRVs,LY 2334737,EV-A71,Rhinovirus,inhibit,Nucleoside Antimetabolite/Analog,Enterovirus,HRV,orally,LY2334737,LY-2334737,antiviral,Inhibitor
- N-{1-[(2R,4R,5R)-3,3-difluoro-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-2-oxo-1,2-dihydropyrimidin-4-yl}-2-propylpentanamide
- CAS:
- 892128-60-8
- MF:
- C17H25F2N3O5
- MW:
- 389.39
- Mol File:
- 892128-60-8.mol
LY2334737 Chemical Properties
- Density
- 1.41±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- Soluble in DMSO
- form
- Powder
- pka
- 9.66±0.20(Predicted)
- color
- White to off-white
LY2334737 Usage And Synthesis
Biological Activity
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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