Product Introduction
Bioactivity


英文名: Capecitabine

描述: Capecitabine (Capecitibine) 是一种可口服的前药，可由胸苷磷酸化酶催化转变为其活性代谢物 Fluorouracil。

细胞实验: HepG2 and either LS174T WT or LS174T-c2 cells are seeded, respectively, in the top and bottom chambers of 8-well strip membranes in 96-well plates. The exponentially growing cells are exposed to increasing concentrations of capecitabine. The medium is supplemented with 750 ng/mL ZB4 MoAB or 100 ng/mL BR17 MoAB when the latter are used in the experiments. After 72 hours of continuous exposure, LS174T viability is assessed using the classic colorimetric MTT test.(Only for Reference)

体外活性: 作用于高肝转移裸鼠时,Capecitabine对肿瘤生长和转移复发的人肝细胞癌均有抑制作用,这是因为血小板驱动的内皮细胞生长因子在肿瘤中高表达.与5-FU,UFT及其中间代谢物5'-DFUR相比,Capecitabine对人类移植瘤更具有广泛的抗癌活谱性,这与肿瘤dThdPase水平相关.

体内活性: Capecitabine以Fas依赖性地方式诱导凋亡,且对胸苷磷酸化酶-转染的LS174T-c2 细胞的毒性强7倍、凋亡更明显。培养在与HepG2细胞相同的板中时,LS174TWT和 LS174T-c2细胞对Capecitabine敏感性的较强,Capecitabine与LS174TWT单独培养时的IC50为890 μM,与HepG2一起培养的IC50为630 μM。此外, LS174T-C2亚型培养在和HepG2相同的板中时, IC50从330±4降至89±6 μM。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: 5% DMSO+95% Saline : 1.8 mg/mL (5 mM)
Ethanol : 35.9 mg/mL (100 mM)
DMSO : 35.9 mg/mL (100 mM)


关键字: inhibit | Nucleoside Antimetabolite/Analog | Capecitabine | Inhibitor | Apoptosis | DNA/RNA Synthesis

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