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LY2334737
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
LY2334737图片
CAS NO:892128-60-8
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
2mg电议
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
LY2334737 是一种核苷类似物,是吉西他滨的口服活性前药。
Cas No.892128-60-8
别名2'-脱氧-2',2'-二氟-N-(1-氧代-2-丙基戊基)胞苷
化学名N-[1-[(2R,4R,5R)-3,3-difluoro-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-2-oxopyrimidin-4-yl]-2-propylpentanamide
Canonical SMILESCCCC(CCC)C(=O)NC1=NC(=O)N(C=C1)C2C(C(C(O2)CO)O)(F)F
分子式C17H25F2N3O5
分子量389.39
溶解度Soluble in DMSO
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.