Gemcitabine elaidate (CP-4126) is a lipophilic prodrug of Gemcitabine. It undergoes conversion to Gemcitabine by esterases prior to phosphorylation. Gemcitabine elaidate demonstrates anti-tumor activity [1][2].
体内研究
Gemcitabine elaidate (25-120 mg/kg; i.p. every 3 days for 5 doses) uppresses the growth of solid tumor xenografts derived from non-small cell lung cancer (EKVX), non-classifiable sarcoma (MHMX), fibrous histiocytoma (TAX II-1), malignant melanoma (THX), prostate cancer (CRL-1435), and pancreatic cancer (PANC-1) [1].
Gemcitabine elaidate (10-20 mg/kg; pO. every 3 days for 5 doses) xhibits acceptable toxicity and significant antitumor efficacy in mice bearing the Co6044 colon cancer xenograft [1].
Gemcitabine elaidate (pO. once daily for 5 doses) demonstrates favorable toxicity and antitumor efficacy, although the 15 mg/kg dose is highly toxic in the human colon cancer xenograft Co6044 [1].
体外研究
Gemcitabine elaidate (0.2 nM-1 mM; 72 h) inhibits the growth of both gemcitabine-sensitive and resistant cells. The IC50 values are 0.0033, 16.0, 0.0042, 13.0, 0.0015, 0.03, 0.0025, 91, 0.0040, 0.0077, 0.028, and 0.088 μM for L1210/L5, L4A6, BCLO, Bara-C, C26-A, C26-G, A2780, AG6000, THX, LOX, MOLT4, and MOLT4/C8 cells, respectively [1].
Gemcitabine elaidate (0.5 nM-1 μM; 72 h) induces S phase accumulation and dose-dependent cell death in A549 and WiDR cells [2].
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