892128-60-8

Basic information

• Product Name: LY2334737
• Synonyms: LY2334737;2'-Deoxy-2',2'-difluoro-N-(1-oxo-2-propylpentyl)cytidine
• CAS NO: 892128-60-8
• Molecular Formula: C₁₇H₂₅F₂N₃O₅
• Molecular Weight: 389.3943064
• Mol File: 892128-60-8.mol
• Article Data: 5

Chemical Properties

• Appearance: /
• Density: 1.41±0.1 g/cm3(Predicted)
• Solubility: Soluble in DMSO
• PKA: 9.66±0.20(Predicted)
• CAS DataBase Reference: LY2334737(CAS DataBase Reference)
• NIST Chemistry Reference: LY2334737(892128-60-8)
• EPA Substance Registry System: LY2334737(892128-60-8)

Safety Data

• Hazardous Substances Data: 892128-60-8(Hazardous Substances Data)

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

• 99-66-1 valproic acid 
• 1196664-00-2 C₂₇H₄₁F₂N₃O₉ 
• 122111-03-9 gemcitabine hydrochloride 
• 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 
• 95058-81-4 gemcitabine 

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 articles and documents

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