1. Cell Cycle/DNA Damage
    Autophagy
  2. DNA/RNA Synthesis
    Nucleoside Antimetabolite/Analog
    Autophagy
  3. Gemcitabine

Gemcitabine (Synonyms: LY 188011)

Cat. No.: HY-17026 Purity: 99.92%
Handling Instructions

Gemcitabine (LY 188011) is a DNA synthesis inhibitor which 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.

For research use only. We do not sell to patients.

Gemcitabine Chemical Structure

Gemcitabine Chemical Structure

CAS No. : 95058-81-4

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Customer Review

Based on 21 publication(s) in Google Scholar

Other Forms of Gemcitabine:

Top Publications Citing Use of Products

    Gemcitabine purchased from MCE. Usage Cited in: Chem Biol Interact. 2018 Jun 25;290:44-51.

    U2OS and MG-63 cells are treated with Gemcitabine, Licoricidin, or Gemcitabine+Licoricidin for 24 h, followed by the determination of active caspse-3 protein level using western blot. Cells without treatment are used as Control.

    Gemcitabine purchased from MCE. Usage Cited in: J Biol Chem. 2017 Jun 2;292(22):9136-9149.

    The plate clone formation of SW480 and SW620 cells with Gemcitabine (8 nM in SW480 and 16 nM in SW620) and/or PX-12 (4 μM in SW480 and 8 μM in SW620).

    Gemcitabine purchased from MCE. Usage Cited in: Naunyn Schmiedebergs Arch Pharmacol. 2019 Jan 25.

    The expression level of p-JAK2, p-STAT3, Bcl-XL, and Mcl-1 in PANC-1 cells is detected by western blot analysis and is all down-regulated in the treatment groups.
    • Biological Activity

    • Protocol

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    • References

    • Customer Review

    Description

    Gemcitabine (LY 188011) is a DNA synthesis inhibitor which 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.

    IC50 & Target

    DNA synthesis[1]

    In Vitro

    MTS assay demonstrates that Gemcitabine at 15 nM, indole-3-carbinol (I3C) at 50 μM and the combination does not affect hTERT-HPNE cell viability. However, treatment with Gemcitabine at 15 nM, I3C at 50 μM and the combination results in 31%, 19% and 72% cell death of BxPC-3 cells, respectively[1].

    In Vivo

    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 increased the median survival time by more than 30 days compared to the placebo group (254.5 [P=0.015] or 255 days [P=0.018] vs. 217.5 days, respectively)[2]. 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[3].

    Clinical Trial
    Molecular Weight

    263.20

    Formula

    C₉H₁₁F₂N₃O₄

    CAS No.

    95058-81-4

    SMILES

    O=C1N(C=CC(N)=N1)[[email protected]]2C(F)([[email protected]@H]([[email protected]](O2)CO)O)F

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    4°C, protect from light

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 103.3 mg/mL (392.48 mM)

    Ethanol : 3.33 mg/mL (12.65 mM; Need ultrasonic)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.7994 mL 18.9970 mL 37.9939 mL
    5 mM 0.7599 mL 3.7994 mL 7.5988 mL
    10 mM 0.3799 mL 1.8997 mL 3.7994 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.58 mg/mL (9.80 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.58 mg/mL (9.80 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.58 mg/mL (9.80 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
    Cell Assay
    [1]

    Cells (the human pancreatic cell lines, Mia PaCa-2, BxPC-3, AsPC-1, PANC-1, PL-45, and normal pancreatic ductal epithelial cells, hTERT-HPNE cells) are seeded into 96-well plates (3000 cells/well) in triplicate. After overnight incubation, the medium is changed and cells are treated with I3C and/or NBMPR for 24 h. The medium is changed again and cells are cultured in medium containing different concentrations of Gemcitabine in the presence or absence of the same concentrations of I3C and/or NBMPR for 48 h. The cells are then subjected to CellTiter 96 AQueous One Solution Cell Proliferation Assay (MTS) as per the manufacturer's instructions. Absorbance at 490 nm is measured 2 h after the addition of 20 μL of MTS reagent/well[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [2][3]

    Mice[2]
    At 1 month of age, LSL-KrasG12D/+; LSL-Trp53R172H; Pdx-1-Cre mice are randomized into treatment groups (placebo, DMAPT, Gemcitabine, DMAPT/Gemcitabine). Placebo (vehicle=hydroxylpropyl methylcellulose, 0.2% Tween 80 [HPMT]) and DMAPT (40 mg/kg body weight in HPMT) are administered by oral gastric lavage once daily. Gemcitabine (50 mg/kg body weight in PBS) is administered by intraperitoneal injection twice weekly. Mouse weight is monitored weekly. Treatment is continued until mice show signs of lethargy, abdominal distension or weight loss at which time they are sacrificed. Successful excision-recombination events are confirmed in the pancreata of mice by detecting the presence of a single LoxP site.
    Rats[3]
    The study is conducted in 80 female Wistar rats, with an initial weight of approximately 250 g. Animals are identified by ear mark and divided into groups as follows. Forty rats are divided into five groups of eight: four groups had lung delivery of Gemcitabine via endotracheal spray at doses of 2, 4, 6, and 8 mg/kg, respectively (groups LD2, LD4, LD6, LD8), and one group receive a spray administration of the 0.9% saline vehicle solution (group LDv). The remaining 40 rats are divided into five groups of eight: four groups have oral delivery of Gemcitabine via gavage at doses of 2, 4, 6, and 8 mg/kg, respectively (groups OD2, OD4, OD6, OD8), and one group receive an identical volume of 0.9% saline via gavage (group ODv). The protocol includes nine sessions separated by 1-week intervals. Between sessions, the animals are kept under standard laboratory conditions and housed by groups of four animals in each cage with litter and free access to pellet food and tap water. Cages are placed in a closed chamber connected to an aspiration system.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References

    Purity: 99.92%

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