Gemcitabine triphosphate  (Synonyms: dFdCTP)

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 K_i 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^[1][2][3][4].

Gemcitabine triphosphate inhibits replicative DNA polymerases α and ε with K_i 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.

Gemcitabine triphosphate (dFdCTP), the active form generated via consecutive weekly administration for 11 weeks, exerts antitumor effects in female BALB/cAJcl-nu/nu mice bearing pancreatic cancer cells (SUIT-2 orthotopic xenograft model), resulting in a median survival time of 89 days and a survival rate of 40% at the end of the experiment^[2].
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.

503.14

C₉H₁₄F₂N₃O₁₃P₃

110988-86-8

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

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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]