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Gemcitabine elaidate hydrochloride

CAS No. :

MCE 站：Gemcitabine elaidate hydrochloride

产品活性：Gemcitabine elaidate (CP-4126) hydrochloride 是 Gemcitabine 的亲脂性前药。Gemcitabine elaidate hydrochloride 通过酯酶转化为 Gemcitabine 以被磷酸化。Gemcitabine elaidate hydrochloride 具有抗肿瘤活性。

研究领域：Cell Cycle/DNA Damage  |  Autophagy  |  Apoptosis

作用靶点：Nucleoside Antimetabolite/Analog  |  Autophagy  |  Apoptosis

In Vitro: Gemcitabine elaidate (0.2 nM-1 mM; 72 h) hydrochloride inhibits the growth of gemcitabine sensitive ａnd resistant cells, with IC₅₀s of 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.
Gemcitabine elaidate (0.5 nM-1 μM; 72 h) hydrochloride increases S phase accumulation ａnd dose-dependent cell kill in A549 ａnd WiDR cells.

In Vivo: Gemcitabine elaidate (25-120 mg/kg; i.p. every 3 days for 5 doses) hydrochloride inhibits the solid tumor xenografts growth of non-small cell lung cancer (EKVX), non-classifiable sarcoma (MHMX), fibrous histiocytoma (TAX II-1), malignant melanoma (THX), prostate cancer (CRL-1435), pancreatic cancer (PANC-1).
Gemcitabine elaidate (10-20 mg/kg; p.o. every 3 days for 5 doses) hydrochloride shows acceptable toxicity ａnd significant antitumor activity in the colon cancer xenograft Co6044 bearing mice.
Gemcitabine elaidate (p.o. once daily for 5 doses) hydrochloride shows a favorable toxicity ａnd antitumor activity, while the dose of 15 mg/kg is highly toxic in the human colon cancer xenograft Co6044.

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