| Identification | Back Directory | [Name]
CP-4126 (LVT derivative of Gemcitabine) | [CAS]
210829-30-4 | [Synonyms]
CP 4126
CS-1569
GeMcitabine elaidate
GeMcitabine 5'-elaidate
Gemcitabine elaidate(CP-4126
CO-101:CP-4126:Gemcitabineelaidate
CP-4126 (LVT derivative of Gemcitabine)
CO-101; CP-4126; GEMCITABINE 5'-ELAIDATE
Cytidine, 2'-deoxy-2',2'-difluoro-, 5'-(9E)-9-octadecenoate
CO-101; CO101; CO 101; CP-4126; CP4126; CP 4126; GEMCITABINE ELAIDATE | [Molecular Formula]
C27H43F2N3O5 | [MDL Number]
MFCD15145214 | [MOL File]
210829-30-4.mol | [Molecular Weight]
527.64 |
| Chemical Properties | Back Directory | [Boiling point ]
631.4±65.0 °C(Predicted) | [density ]
1.20±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
Ethanol:PBS (pH 7.2) (1:2):0.33(Max Conc. mg/mL);0.63(Max Conc. mM)
DMSO:28.0(Max Conc. mg/mL);53.07(Max Conc. mM)
DMF:30.0(Max Conc. mg/mL);56.86(Max Conc. mM)
Ethanol:30.0(Max Conc. mg/mL);56.86(Max Conc. mM) | [form ]
A crystalline solid | [pka]
11.48±0.70(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
Gemcitabine elaidate (CP-4126) is lipophilic pro-agent of Gemcitabine. Gemcitabine elaidate is converted to Gemcitabine by esterases in order to be phosphorylated. Gemcitabine elaidate exhibits anti-tumor activity[1][2]. | [Definition]
ChEBI: Gemcitabine elaidate is a pyrimidine 2'-deoxyribonucleoside. | [in vivo]
Gemcitabine elaidate (25-120 mg/kg; i.p. every 3 days for 5 doses) 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) 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) 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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| [storage]
Store at -20°C | [References]
[1] Bergman AM, et, al. Antiproliferative activity, mechanism of action and oral antitumor activity of CP-4126, a fatty acid derivative of gemcitabine, in in vitro and in vivo tumor models. Invest New Drugs. 2011 Jun;29(3):456-66. DOI:10.1007/s10637-009-9377-7
[2] Adema AD, et, al. Cell cycle effects of fatty acid derivatives of cytarabine, CP-4055, and of gemcitabine, CP-4126, as basis for the interaction with oxaliplatin and docetaxel. Int J Oncol. 2010 Jan;36(1):285-94. PMID:19956857 |
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