Gemcitabine triphosphate trisodium
Based on 1 Customer Validation
Gemcitabine triphosphate (dFdCTP) trisodium is the active metabolite of Gemcitabine (HY-17026). The mechanism of Gemcitabine triphosphate trisodium cell-killing is its competition with cytidine triphosphate during DNA replication, which results in the inhibition of chain elongation. Gemcitabine triphosphate trisodium shows a Ki of 11.2 μM against DNA polymerase α and 14.4 μM against DNA polymerase ε. Gemcitabine triphosphate trisodium partially inhibits dCMP deaminase and acts as a substrate for DNA synthesis to incorporate into cellular DNA and RNA. Gemcitabine triphosphate trisodium disrupts DNA and RNA synthesis, arrests cell cycle in G0/G1 and S phases, triggers apoptosis, reduces tumor cell proliferation. Gemcitabine triphosphate trisodium can be used for the research of pancreatic cancer and non-small cell lung cancer.
For research use only. We do not sell to patients.
- Purity: 99.34%
- Formula: C9H11F2N3Na3O13P3
- Molecular Weight:569.08
-
Storage:
-80°C
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
- Purity & Documentation
- References
-
Help & FAQs
All DNA/RNA Synthesis Isoforms
More
Biological Activity
|
DNA Polymerase |
Gemcitabine triphosphate trisodium 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) trisodium 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) trisodium 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) trisodium 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) trisodium 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.
-
Cell Line:H460 and BxPC-3 cells
-
Concentration:0.1 μM, 0.2 μM, 0.5 μM, 1 μM, 2 μM, 5 μM, 10 μM
-
Incubation Time:48 h
-
Result:Reduced cell viability in a dose-dependent manner.
-
Cell Line:H460 and BxPC-3 cells
-
Concentration:1.8 μM
-
Incubation Time:24 h
-
Result:Increased the percentage of cells in the S phase in both H460 and BxPC-3 cells, indicating S-phase arrest.
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
-
Appearance Liquid
-
Molecular Weight 569.08
-
Formula C9H11F2N3Na3O13P3
-
Color Colorless to light yellow
-
SMILES
NC(C=CN1[C@H]2C(F)(F)[C@H](O)[C@@H](COP(OP(OP(O)(O[Na])=O)(O[Na])=O)(O[Na])=O)O2)=NC1=O
-
Synonyms
dFdCTP trisodium
-
Structure Classification
-
Initial Source
-
Shipping
Shipping with dry ice.
-
Storage
-80°C
Purity & Documentation
-
Data Sheet (279 KB)
-
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
-
Handling Instructions (2659 KB)
References
[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
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Gemcitabine triphosphate trisodium Related Classifications
HY-17026E Related Classifications
Powered by Bioz