TAS-102

TAS‑102 （CAS号：733030-01-8）为口服核苷类抗肿瘤药，由 Trifluridine（FTD，货号：A8542，CAS号：70-00-8）+ Tipiracil （货号：BA3519，CAS号：183204-74-2）组成。FTD 经磷酸化后以 FTD‑TP 形式大量掺入 DNA，是主要致死机制，可诱导 p53 激活和 G2 期阻滞，并通过抑制 AKT / NF‑κB 下调 VEGF、FGF2，兼具抗增殖与抗血管生成作用。

常用人源肿瘤细胞（如 OSCC HSC2/HSC4、结直肠癌 HCT‑116）中，FTD/TAS‑102 多用 0.1–10 μg/mL（约 0.3–30 μM），处理 24–48 h。可见剂量依赖性增殖抑制与迁移抑制，并可用抗‑BrdU 抗体（3D4/B44）检测 S 期核内 FTD‑DNA 掺入量，与细胞毒性、p‑AKT/p‑p65 降低高度相关。

皮下瘤模型中，常在肿瘤体积约 40–100 mm³ 时分组给药：TAS‑102 100 mg/kg/day 口服灌胃，连续 4 周（对照 0.5% HPMC；可设 5‑FU （货号：A4071，CAS号：51-21-8） 10 mg/kg/day 腹腔注射作为阳性对照）。在 HSC2 裸鼠皮下瘤中，该方案显著抑制肿瘤生长，效果略优于 5‑FU，体重基本稳定；瘤组织内 p‑AKT、p‑p65、VEGF、FGF2、CD31 表达和微血管密度均明显下降，体现其 DNA 掺入 + 抗血管生成的综合生物学功能。

参考文献：

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