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Gemcitabine elaidate

Gemcitabine elaidate
Gemcitabine elaidate (CP-4126), is a lipophilic, unsaturated fatty acid ester derivative of gemcitabine (dFdC), an antimetabolite deoxynucleoside analogue, with potential antineoplastic activity. Upon hydrolysis intracellularly by esterases, the prodrug gemcitabine is converted into the active metabolites difluorodeoxycytidine di- and tri-phosphate (dFdCDP and dFdCTP) by deoxycytidine kinase. dFdCDP inhibits ribonucleotide reductase, thereby decreasing the deoxynucleotide pool available for DNA synthesis; dFdCTP is incorporated into DNA, resulting in DNA strand termination and apoptosis.
Catalog No. T15378Cas No. 210829-30-4

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Gemcitabine elaidate

Catalog No. T15378Alias Gemcitabine 5'-elaidate, Gemcitabine (elaidate), CP-4126, CO-101Cas No. 210829-30-4

Gemcitabine elaidate (CP-4126), is a lipophilic, unsaturated fatty acid ester derivative of gemcitabine (dFdC), an antimetabolite deoxynucleoside analogue, with potential antineoplastic activity. Upon hydrolysis intracellularly by esterases, the prodrug gemcitabine is converted into the active metabolites difluorodeoxycytidine di- and tri-phosphate (dFdCDP and dFdCTP) by deoxycytidine kinase. dFdCDP inhibits ribonucleotide reductase, thereby decreasing the deoxynucleotide pool available for DNA synthesis; dFdCTP is incorporated into DNA, resulting in DNA strand termination and apoptosis.
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2 mg$435 days
5 mg$895 days
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Product Introduction

Bioactivity
Description
Gemcitabine elaidate (CP-4126), is a lipophilic, unsaturated fatty acid ester derivative of gemcitabine (dFdC), an antimetabolite deoxynucleoside analogue, with potential antineoplastic activity. Upon hydrolysis intracellularly by esterases, the prodrug gemcitabine is converted into the active metabolites difluorodeoxycytidine di- and tri-phosphate (dFdCDP and dFdCTP) by deoxycytidine kinase. dFdCDP inhibits ribonucleotide reductase, thereby decreasing the deoxynucleotide pool available for DNA synthesis; dFdCTP is incorporated into DNA, resulting in DNA strand termination and apoptosis.
In vitro
Gemcitabine analog Upon hydrolysis intracellularly by esterases, the prodrug gemcitabine is converted into the active metabolites difluorodeoxycytidine di- and tri-phosphate (dFdCDP and dFdCTP) by deoxycytidine kinase. dFdCDP inhibits ribonucleotide reductase, thereby decreasing the deoxynucleotide pool available for DNA synthesis; dFdCTP is incorporated into DNA, resulting in DNA strand termination and apoptosis. Gemcitabine 5'-elaidic acid ester shows an enhanced cellular uptake and accumulation, resulting in increased conversion to active metabolites, compared to gemcitabine. This formulation of gemcitabine may be less susceptible to deamination and deactivation by deoxycytidine deaminase. Check for active clinical trials or closed clinical trials using this agent.
AliasGemcitabine 5'-elaidate, Gemcitabine (elaidate), CP-4126, CO-101
Chemical Properties
Molecular Weight527.64
FormulaC27H43F2N3O5
Cas No.210829-30-4
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 26 mg/mL (49.28 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.8952 mL9.4762 mL18.9523 mL94.7616 mL
5 mM0.3790 mL1.8952 mL3.7905 mL18.9523 mL
10 mM0.1895 mL0.9476 mL1.8952 mL9.4762 mL
20 mM0.0948 mL0.4738 mL0.9476 mL4.7381 mL

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