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Gemcitabine elaidate

Catalog No. T15378   CAS 210829-30-4
Synonyms: Gemcitabine 5'-elaidate, Gemcitabine (elaidate), CO-101, CP-4126

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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Gemcitabine elaidate Chemical Structure
Gemcitabine elaidate, CAS 210829-30-4
Pack Size Availability Price/USD Quantity
2 mg 5 days $ 43.00
5 mg 5 days $ 89.00
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Biological Description
Chemical Properties
Storage & Solubility Information
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.
Synonyms Gemcitabine 5'-elaidate, Gemcitabine (elaidate), CO-101, CP-4126
Molecular Weight 527.64
Formula C27H43F2N3O5
CAS No. 210829-30-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 26 mg/mL (49.28 mM)

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Approved Drug Library

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R406 free base Ganetespib Y-27632 AZD5582 TFA ICCB-19 hydrochloride TCS7010 Poziotinib Apitolisib

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Keywords

Gemcitabine elaidate 210829-30-4 Apoptosis Autophagy Cell Cycle/Checkpoint DNA Damage/DNA Repair Nucleoside Antimetabolite/Analog anti-tumor CO101 inhibit CP4126 CP 4126 Gemcitabine 5'-elaidate Gemcitabine (elaidate) CO 101 CO-101 Gemcitabine CP-4126 Inhibitor elaidate inhibitor

 

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