Gemcitabine (LY 188011) est un pyrimidine nucléoside analogue antimétabolite et un agent antinéoplasique. Gemcitabine inhibe la synthèse de l'ADN et la réparation, entraînant l'autophagie et l'apoptose. Gemcitabine inhibe la croissance des cellules de BxPC-3, de Mia Paca-2, de PANC-1, de PL-45 et de AsPC-1 avec des IC50 de 37,6 nM, 42,9 nM, 92,7 nM, 89,3 nM et 131,4 nM, respectivement.
Gemcitabin (LY 188011) ist ein pyrimidine nucleoside-Antimetabolit und ein antineoplastisches Mittel. Gemcitabin hemmt die DNA synthesis und -Reparatur, was zu autophagy und apoptosis führt. Gemcitabin hemmt das Wachstum von BxPC-3-, Mia Paca-2-, PANC-1-, PL-45- und AsPC-1-Zellen mit IC50s von 37,6 nM, 42,9 nM, 92,7 nM, 89,3 nM bzw. 131,4 nM.
Gemcitabine (LY 188011) is a pyrimidine nucleoside analog antimetabolite and an antineoplastic agent. Gemcitabine inhibits DNA synthesis and repair, resulting in autophagyand apoptosis.
For research use only. We do not sell to patients.
Gemcitabine Chemical Structure
CAS No. : 95058-81-4
This product is a controlled substance and not for sale in your territory.
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.
Gemcitabine purchased from MedChemExpress. Usage Cited in:
Chem Biol Interact. 2018 Jun 25;290:44-51.
[Abstract]
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 MedChemExpress. Usage Cited in:
J Biol Chem. 2017 Jun 2;292(22):9136-9149.
[Abstract]
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).
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Description
Gemcitabine (LY 188011) is a pyrimidine nucleoside analog antimetabolite and an antineoplastic agent. Gemcitabine inhibits DNA synthesis and repair, resulting in autophagyand apoptosis[1][2].
IC50 & Target
DNA synthesis[1]
In Vitro
Gemcitabine (purchased from MedChem Express, 0.003-1 μM; 3 days) kills both mouse and human senescent cells effectively and potently[4].
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[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Gemcitabine Related Antibodies
Cell Viability Assay[4]
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.
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[2].
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)[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
Molecular Weight
263.20
Formula
C9H11F2N3O4
CAS No.
95058-81-4
Appearance
Solid
Color
White to off-white
SMILES
NC(C=CN1[C@H]2C(F)(F)[C@H](O)[C@@H](CO)O2)=NC1=O
Shipping
Room temperature in continental US; may vary elsewhere.
DMSO : 250 mg/mL (949.85 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Ethanol : 12.5 mg/mL (47.49 mM; Need ultrasonic)
H2O : 6.25 mg/mL (23.75 mM; ultrasonic and warming and heat to 60°C)
Preparing Stock Solutions
ConcentrationSolventMass
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
View the Complete Stock Solution Preparation Table
*Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles. Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
*
Note: If you choose water as the stock solution, please dilute it to the working solution,
then filter and sterilize it with a 0.22 μm filter before use.
For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day. The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Protocol 1
Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline
This protocol yields a clear solution of ≥ 2.58 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (25.8 mg/mL) to 900 μLCorn oil, and mix evenly.
Protocol 4
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 5
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (20.8 mg/mL) to 900 μLCorn oil, and mix evenly.
For the following dissolution methods, please prepare the working solution directly.
It is recommended to prepare fresh solutions and use them promptly within a short period of time. The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution.
If precipitation or phase separation occurs during preparation,
heat and/or sonication can be used to aid dissolution.
Protocol 1
Add each solvent one by one: 0.5%HPMC 1%Tween80
Solubility: 20 mg/mL (75.99 mM); Clear solution; Need ultrasonic
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
Dosage
mg/kg
Animal weight (per animal)
g
Dosing volume (per animal)
μL
Number of animals
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO+
%
+
%
Tween-80
+
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO,
. All of co-solvents are available by MedChemExpress (MCE).
, Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration:
mg/mL
Method for preparing stock solution:
mg
drug dissolved in
μL
DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take
μL DMSO stock solution, add
μL .
μL , mix evenly, next add
μL Tween 80, mix evenly, then add
μL Saline.
Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution
If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
[1]. Wang H, et al. Enhanced efficacy of Gemcitabine by indole-3-carbinol in pancreatic cell lines: the role of human equilibrativenucleoside transporter 1. Anticancer Res. 2011 Oct;31(10):3171-80.
[Content Brief]
[2]. Gagnadoux F, et al. Safety of pulmonary administration of gemcitabine in rats. J Aerosol Med. 2005 Summer;18(2):198-206
[Content Brief]
[3]. Yip-Schneider MT, et al. Dimethylaminoparthenolide and Gemcitabine: a survival study using a genetically engineered mouse model of pancreatic cancer. BMC Cancer. 2013 Apr 17;13:194.
[Content Brief]
[4]. Yusheng Cai, et al. Elimination of senescent cells by β-galactosidase-targeted prodrug attenuates inflammation and restores physical function in aged mice. Cell Res. 2020 Jul;30(7):574-589.
[Content Brief]
[1]. Wang H, et al. Enhanced efficacy of Gemcitabine by indole-3-carbinol in pancreatic cell lines: the role of human equilibrativenucleoside transporter 1. Anticancer Res. 2011 Oct;31(10):3171-80.
[2]. Gagnadoux F, et al. Safety of pulmonary administration of gemcitabine in rats. J Aerosol Med. 2005 Summer;18(2):198-206
[3]. Yip-Schneider MT, et al. Dimethylaminoparthenolide and Gemcitabine: a survival study using a genetically engineered mouse model of pancreatic cancer. BMC Cancer. 2013 Apr 17;13:194.
[4]. Yusheng Cai, et al. Elimination of senescent cells by β-galactosidase-targeted prodrug attenuates inflammation and restores physical function in aged mice. Cell Res. 2020 Jul;30(7):574-589.
Complete Stock Solution Preparation Table
*Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles. Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Optional Solvent
ConcentrationSolventMass
1 mg
5 mg
10 mg
25 mg
H2O / Ethanol / DMSO
1 mM
3.7994 mL
18.9970 mL
37.9939 mL
94.9848 mL
5 mM
0.7599 mL
3.7994 mL
7.5988 mL
18.9970 mL
10 mM
0.3799 mL
1.8997 mL
3.7994 mL
9.4985 mL
15 mM
0.2533 mL
1.2665 mL
2.5329 mL
6.3323 mL
20 mM
0.1900 mL
0.9498 mL
1.8997 mL
4.7492 mL
Ethanol / DMSO
25 mM
0.1520 mL
0.7599 mL
1.5198 mL
3.7994 mL
30 mM
0.1266 mL
0.6332 mL
1.2665 mL
3.1662 mL
40 mM
0.0950 mL
0.4749 mL
0.9498 mL
2.3746 mL
DMSO
50 mM
0.0760 mL
0.3799 mL
0.7599 mL
1.8997 mL
60 mM
0.0633 mL
0.3166 mL
0.6332 mL
1.5831 mL
80 mM
0.0475 mL
0.2375 mL
0.4749 mL
1.1873 mL
100 mM
0.0380 mL
0.1900 mL
0.3799 mL
0.9498 mL
*
Note: If you choose water as the stock solution, please dilute it to the working solution,
then filter and sterilize it with a 0.22 μm filter before use.
Gemcitabine Related Classifications
Help & FAQs
Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.