892128-60-8

Usage

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.

Upstream product

• 95058-81-4 gemcitabine 
• 1254062-21-9 4-amino-1-((6aR,8R,9aR)-9,9-difluoro-2,2,4,4-tetraisopropyltetrahydro-6H-furo[3,2-f] [1,3,5,2,4]trioxadisilocin-8-yl)pyrimidin-2(1H)-one 
• 99-66-1 valproic acid 
• 122111-03-9 gemcitabine hydrochloride 
• 1196664-00-2 C₂₇H₄₁F₂N₃O₉ 

Downstream Products

• 960397-74-4 1-(2,2-difluoro-2-deoxy-β-D-ribofuranosyl)-4-(2-propyl-1-oxopentyl)aminopyrimidin-2-one p-toluenesulfonic acid co-crystal 
• 892128-62-0 1-(2,2-difluoro-2-deoxy-β-D-ribofuranosyl)-4-(2-propyl-1-oxopentyl)aminopyrimidin-2-one benzensulfonic acid co-crystal 
• 95058-81-4 gemcitabine 

Relevant academic research and scientific papers

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The present invention relates to novel crystal forms of an amide prodrug of gemcitabine, compositions thereof and methods for using.

AMIDE PRODRUG OF GEMCITABINE, COMPOSITIONS AND USE THEREOF

The present invention relates to novel amide prodrugs of gemcitabine, compositions thereof and methods for using.