Gemcitabine

SKU: orb1223542

Description

A synthetic pyrimidine nucleoside prodrug that works by ihibiting the enzyme ribonucleotide reductase (RNR) and blocking the creation of new DNA; a chemotherapy agent for treatment of a number of types of cancer.Chemotherapeutic Agents Approved(In Vitro):Gemcitabine (purchased from MedChem Express, 0.003-1 μM; 3 days) kills both mouse and human senescent cells effectively and potently.Gemcitabine inhibits the growth of BxPC-3, Mia Paca-2, PANC-1, PL-45 and AsPC-1 cells with IC50s of 37.6, 42.9, 92.7, 89.3 and 131.4 nM, respectively.(In Vivo):Gemcitabine can be administered via endotracheal spray in rats without marked toxicity with a maximum tolerated dose of 4 mg/kg once a week for 9 weeks. The toxicity of Gemcitabine is lower via lung than oral administration at dosages of 2, 4, and 6 mg/kg.Treatment of the LSL-KrasG12D/+; LSL-Trp53R172H; Pdx-1-Cre mice with either Gemcitabine (50 mg/kg, i.p.) or the combination DMAPT/Gemcitabine significantly increases the median survival time by more than 30 days compared to the placebo group (254.5 or 255 days vs. 217.5 days, respectively).

Key Properties

• CAS Number: 95058-81-4
• MW: 263.1982
• Purity: >98% (HPLC)
• Formula: C₉H₁₁F₂N₃O₄
• SMILES: C1=CN(C(=O)N=C1N)[C@H]2C([C@@H]([C@H](O2)CO)O)(F)F
• Target: Nucleoside Antimetabolite/Analog
• Solubility: 10 mM in DMSO

Bioactivity

• In Vitro:
  Cell Viability Assay Cell line: Non-senescent and replication-induced senescent new born dermal fibroblasts (NBFs). Concentration: 0.003, 0.01, 0.03, 0.1, 0.3, 1 μM Incubation time: 3 days. Result: Killed replication-induced senescent NBFs for 3 days with 11.0% cell viability.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

LY 188011 | NSC 613327 | LY188011 | LY-188011

Quick Database Links

Gene Symbol

Nucleoside Antimetabolite/Analog