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Gemcitabine elaidate

Cat. No. M13701
Gemcitabine elaidate Structure
Synonym:

CP-4126; CO-101; Gemcitabine 5'-elaidate

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Quality Control & Documentation
Biological Activity

Gemcitabine elaidate (CP-4126) is lipophilic pro-drug of Gemcitabine. Gemcitabine elaidate is converted to Gemcitabine by esterases in order to be phosphorylated. Gemcitabine elaidate exhibits anti-tumor activity.

Chemical Information
Molecular Weight 527.64
CAS Number 210829-30-4
Solubility (25°C) DMSO ≥ 26 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Bowen Sun, et al. Adv Sci (Weinh). Wirelessly Activated Nanotherapeutics for In Vivo Programmable Photodynamic-Chemotherapy of Orthotopic Bladder Cancer

[2] D Li, et al. Pancreatology. A phase II, open-label, multicenter study to evaluate the antitumor efficacy of CO-1.01 as second-line therapy for gemcitabine-refractory patients with stage IV pancreatic adenocarcinoma and negative tumor hENT1 expression

[3] Godefridus J Peters. Nucleosides Nucleotides Nucleic Acids. Novel developments in the use of antimetabolites

[4] F E Stuurman, et al. Invest New Drugs. Phase I study of oral CP-4126, a gemcitabine derivative, in patients with advanced solid tumors

[5] Andries M Bergman, et al. Invest New Drugs. 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

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Keywords: Gemcitabine elaidate, CP-4126; CO-101; Gemcitabine 5'-elaidate supplier, inhibitors, activators


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