l General Information |
Product Name | Gemcitabine |
General description | Gemcitabine is a Nucleoside Metabolic Inhibitor with antineoplastic activity. |
Synonym | 4-amino-1-[(2R,4R,5R)-3,3-difluoro-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]pyrimidin-2-one; Gemcitabinum; Gamcitabine; Gemcitabina;dFdC, Gemzar (Lilly), LY-188011, dFdC, dFdCyd |
Purity | ≥99%(HPLC) | CAS Number | 95058-81-4 |
Formula | C9H11F2N3O4 | Molecular Weight | 263.201 |
Suitability | BioReagent, suitable for cell culture, etc. |
l Physical and Chemical Information |
Appearance | White to Off-white solid |
Solubility(25℃) | DMSO | ≥50mg/mL |
Ethanol | Insoluble |
Water | ≥20mg/mL |
l Biological Information |
Biochem/Physiol Actions | Gemcitabine is an antineoplastic anti-metabolite. Anti-metabolites masquerade as purine or pyrimidine - which become the building blocks of DNA. They prevent these substances becoming incorporated in to DNA during the "S" phase (or DNA synthesis phase of the cell cycle), stopping normal development and division. Gemcitabine blocks an enzyme which converts the cytosine nucleotide into the deoxy derivative. In addition, DNA synthesis is further inhibited because Gemcitabine blocks the incorporation of the thymidine nucleotide into the DNA strand. It demonstrates dose-dependent synergistic activity with cisplatin in vitro. In vivo, gemcitabine showed activity in combination with cisplatin against the LX-1 and CALU-6 human lung xenografts, but minimal activity was seen with the NCI-H460 or NCI-H520 xenografts. Gemcitabine was synergistic with cisplatin in the Lewis lung murine xenograft. Sequential exposure to gemcitabine 4 hours before cisplatin produced the greatest interaction. Gemcitabine is a broad-spectrum antimetabolite and deoxycytidine analogue with antineoplastic activity. Upon administration, gemcitabine is converted into the active metabolites difluorodeoxycytidine diphosphate (dFdCDP) and difluorodeoxycytidine triphosphate (dFdCTP) by deoxycytidine kinase. dFdCTP competes with deoxycytidine triphosphate (dCTP) and is incorporated into DNA. This locks DNA polymerase thereby resulting in masked termination during DNA replication. On the other hand, dFdCDP inhibits ribonucleotide reductase, thereby decreasing the deoxynucleotide pool available for DNA synthesis. The reduction in the intracellular concentration of dCTP potentiates the incorporation of dFdCTP into DNA. |
Application | 1. Antiviral Agents 2. Enzyme Inhibitors 3. Radiation-Sensitizing Agents 4. Antimetabolites, Antineoplastic 5. Immunosuppressive Agents |
l Packaging & Storage |
Packaging | 250mg; 1g |
Storage temp. | 0-5℃ |
l Precautions and Disclaimer |
This product is for R&D use only, not for drug, household, or other uses. |
l References |
1. http://www.drugbank.ca 2. https://ncit.nci.nih.gov 3. https://www.ncbi.nlm.nih.gov |
