Gemcitabine triphosphate
Gemcitabine triphosphate (dFdCTP) is the active metabolite of Gemcitabine (HY-17026). The mechanism of Gemcitabine triphosphate cell-killing is its competition with cytidine triphosphate during DNA replication, which results in the inhibition of chain elongation. Gemcitabine triphosphate shows a Ki of 11.2 μM against DNA polymerase α and 14.4 μM against DNA polymerase ε. Gemcitabine triphosphate partially inhibits dCMP deaminase and acts as a substrate for DNA synthesis to incorporate into cellular DNA and RNA. Gemcitabine triphosphate disrupts DNA and RNA synthesis, arrests cell cycle in G0/G1 and S phases, triggers apoptosis, reduces tumor cell proliferation. Gemcitabine triphosphate can be used for the research of pancreatic cancer and non-small cell lung cancer.
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- CAS. Nr.: 110988-86-8
- Formel: C9H14F2N3O13P3
- Molecular Weight:503.14
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Biologische Aktivität
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DNA Polymerase |
Gemcitabine triphosphate inhibits replicative DNA polymerases α and ε with Ki values of 11.2 μM and 14.4 μM, respectively[1].
Gemcitabine triphosphate (0.01-10 μM; short-term incubation) accumulates to 0.01-10 μM in human colon carcinoma cells, with radiation enhancement ratios plateauing at 1.0 μM Gemcitabine (precursor)[1].
Gemcitabine triphosphate (0.1-10 μM; 48 h) reduces cell viability in H460 human NSCLC cells and BxPC-3 human pancreatic cancer cells in a dose-dependent manner[3].
Gemcitabine triphosphate (1.8 μM; 24 h) arrests the cell cycle in the S phase in H460 human NSCLC cells and BxPC-3 human pancreatic cancer cells[3].
Gemcitabine triphosphate (1.8 μM; 48 h) induce caspase-3/7 activation in H460 human NSCLC cells and BxPC-3 human pancreatic cancer cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:H460 and BxPC-3 cells
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Concentration:0.1 μM, 0.2 μM, 0.5 μM, 1 μM, 2 μM, 5 μM, 10 μM
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Incubation Time:48 h
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Result:Reduced cell viability in a dose-dependent manner.
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Cell Line:H460 and BxPC-3 cells
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Concentration:1.8 μM
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Incubation Time:24 h
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Result:Increased the percentage of cells in the S phase in both H460 and BxPC-3 cells, indicating S-phase arrest.
| Species | Dose | Route | AUC | MRT | Vss |
|---|---|---|---|---|---|
| Mice[3] | 7.5 μmol/Kg | i.v. | 14.89 h | 0.83 h | 5.58 |
Lipid/calcium/phosphate (LCP) nanoparticles loaded with Gemcitabine triphosphate (7.5 μmol/kg; i.v.; every other day for 4 days, followed by daily administration for 3 days) exert potent anti-tumor efficacy in H460 non-small cell lung cancer and BxPC-3 pancreatic cancer xenograft models via caspase-dependent apoptosis, proliferation inhibition and tumor growth arrest[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 110988-86-8
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Molecular Weight 503.14
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Formel C9H14F2N3O13P3
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SMILES
NC(C=CN1[C@H]2C(F)(F)[C@H](O)[C@@H](COP(OP(OP(O)(O)=O)(O)=O)(O)=O)O2)=NC1=O
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Synonyms
dFdCTP
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Structure Classification
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Initial Source
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[1]. Shewach DS, et al. Gemcitabine and radiosensitization in human tumor cells. Invest New Drugs. 1996;14(3):257-263. [Content Brief]
[2]. Matsumoto T, et al. A Liposomal Gemcitabine, FF-10832, Improves Plasma Stability, Tumor Targeting, and Antitumor Efficacy of Gemcitabine in Pancreatic Cancer Xenograft Models. Pharm Res. 2021;38(6):1093-1106. [Content Brief]
[3]. Zhang Y, et al. Systemic delivery of gemcitabine triphosphate via LCP nanoparticles for NSCLC and pancreatic cancer therapy. Biomaterials. 2013;34(13):3447-3458. [Content Brief]
[4]. Rizzuto I, et al. Pharmacological factors affecting accumulation of gemcitabine's active metabolite, gemcitabine triphosphate. Pharmacogenomics. 2017;18(9):911-925. [Content Brief]
Calculators
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