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。
生物活性 | Gemcitabine elaidate (CP-4126) hydrochloride is lipophilic pro-drug of Gemcitabine. Gemcitabine elaidate hydrochloride is converted to Gemcitabine by esterases in order to be phosphorylated. Gemcitabine elaidate hydrochloride exhibits anti-tumor activity[1][2]. |
体外研究 (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[1]. Gemcitabine elaidate (0.5 nM-1 μM; 72 h) hydrochloride increases S phase accumulation and dose-dependent cell kill in A549 and WiDR cells[2].
Cell Cycle Analysis[2] Cell Line: | A549 and WiDR cells | Concentration: | 0.0005, 0.001, 0.005, 0.01, 0.05, 0.1, 0.5, 1.0 μM | Incubation Time: | 72 h | Result: | Induced a G2/M and S phase accumulation. |
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体内研究 (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)[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[1]. 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[1].
Animal Model: | Female BALB/c nude (nu/nu) mice (5-8 weeks; 20-27 g) were bearing tumor of EKVX, H-146, MHMX, TAX II-1, OHS, THX, MA-11, CRL-1435, PANC-1 and MiaPaCa-2, respectively[1] | Dosage: | 25-120 mg/kg | Administration: | I.p. every 3 days for 5 doses | Result: | Inhibited the growth of EKVX, MHMX, TAX II-1, THX, CRL-1435 and PANC-1, with T/C values of 7%, 1%, 30%, 7%, 9%, and 12%, respectively. |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Powder | -20°C | 3 years | | 4°C | 2 years | In solvent | -80°C | 6 months | | -20°C | 1 month |
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溶解性数据 | In Vitro: DMSO : 100 mg/mL(177.27 mM;Need ultrasonic) 配制储备液 1 mM | 1.7727 mL | 8.8635 mL | 17.7270 mL | 5 mM | 0.3545 mL | 1.7727 mL | 3.5454 mL | 10 mM | 0.1773 mL | 0.8864 mL | 1.7727 mL |
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