Reagents and instruments for immunology, cell biology and molecular biology.

Gemcitabine (hydrochloride) [122111-03-9]

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Cat# HY-B0003-500mg

Size : 500mg

Brand : MedChemExpress

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Description

Gemcitabine Hydrochloride (LY 188011 Hydrochloride) is a pyrimidine nucleoside analog antimetabolite and an antineoplastic agent. Gemcitabine Hydrochloride inhibits DNA synthesis and repair, resulting in autophagyand apoptosis^[1]^[2].

IC₅₀ & Target

DNA synthesis^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
A2780	IC₅₀	1.25 μM Compound: GEM	Cytotoxicity against human A2780 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human A2780 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 33992863]
A2780	IC₅₀	1.38 μM Compound: GEM	Cytotoxicity against human A2780 cells assessed as reduction in cell viability incubated for 72 hrs in hypoxic condition by MTT assay Cytotoxicity against human A2780 cells assessed as reduction in cell viability incubated for 72 hrs in hypoxic condition by MTT assay	[PMID: 33992863]
A549	IC₅₀	14.65 μM Compound: GEM	Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs in hypoxic condition by MTT assay Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs in hypoxic condition by MTT assay	[PMID: 33992863]
A549	IC₅₀	2.31 μM Compound: GEM	Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 33992863]
C2D cell line	IC₅₀	11.9 nM Compound: Gemzar	Inhibitory concentration to inhibit growth of C2D prostate cancer cell line by using MTT assay Inhibitory concentration to inhibit growth of C2D prostate cancer cell line by using MTT assay	[PMID: 14971910]
C2G cell line	IC₅₀	3.7 nM Compound: Gemzar	Inhibitory concentration to inhibit growth of C2G prostate cancer cell line by using MTT assay Inhibitory concentration to inhibit growth of C2G prostate cancer cell line by using MTT assay	[PMID: 14971910]
L02	IC₅₀	11.87 μM Compound: GEM	Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 33992863]
L02	IC₅₀	4.51 μM Compound: GEM	Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 72 hrs in hypoxic condition by MTT assay Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 72 hrs in hypoxic condition by MTT assay	[PMID: 33992863]
MCF7	IC₅₀	6.35 μM Compound: GEM	Cytotoxicity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 33992863]
NCI-H460	IC₅₀	2.13 nM Compound: Gemcitabine HCl	Cytotoxicity against human NCI-H460 cells by MTT assay Cytotoxicity against human NCI-H460 cells by MTT assay	[PMID: 19345581]
NCI-H460	IC₅₀	2.13 μM Compound: GemcitabineHCl	Cytotoxicity against human NCI-H460 cells after 3 days by MTT assay Cytotoxicity against human NCI-H460 cells after 3 days by MTT assay	[PMID: 20356655]
TRAMP-C1A	IC₅₀	9 nM Compound: Gemzar	Inhibitory concentration to inhibit growth of C1A prostate cancer cell line by using MTT assay Inhibitory concentration to inhibit growth of C1A prostate cancer cell line by using MTT assay	[PMID: 14971910]
TRAMP-C2H	IC₅₀	4.7 nM Compound: Gemzar	Inhibitory concentration to inhibit growth of C2H prostate cancer cell line by using MTT assay Inhibitory concentration to inhibit growth of C2H prostate cancer cell line by using MTT assay	[PMID: 14971910]
Vero C1008	CC₅₀	23.22 μM Compound: Gemcitabine Hydrochloride	CC50 determination at MOI 0.004 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in Vero E6 cells CC50 determination at MOI 0.004 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in Vero E6 cells	10.1101/2020.03.25.008482
Vero C1008	CC₅₀	23.22 μM Compound: Gemcitabine Hydrochloride	CC50 determination at MOI 0.01 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in Vero E6 cells CC50 determination at MOI 0.01 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in Vero E6 cells	10.1101/2020.03.25.008482

In Vitro

Gemcitabine Hydrochloride (purchased from MedChem Express, 0.003-1 μM; 3 days) kills both mouse and human senescent cells effectively and potently^[4].
Gemcitabine Hydrochloride 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.

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 Hydrochloride 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-Kras^G12D/+; LSL-Trp53^R172H; Pdx-1-Cre mice with either Gemcitabine (50 mg/kg, i.p.) or the combination DMAPT/Gemcitabine Hydrochloride 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

299.66

Formula

C₉H₁₂ClF₂N₃O₄

CAS No.

122111-03-9

Appearance

Solid

Color

White to off-white

SMILES

O[C@H]1C(F)(F)[C@H](N2C(N=C(N)C=C2)=O)O[C@@H]1CO.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture and light)

Solvent & Solubility

In Vitro:

DMSO : 62.5 mg/mL (208.57 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 25 mg/mL (83.43 mM; Need ultrasonic)

DMF : 2.5 mg/mL (8.34 mM; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.3371 mL	16.6856 mL	33.3712 mL
5 mM	0.6674 mL	3.3371 mL	6.6742 mL
10 mM	0.3337 mL	1.6686 mL	3.3371 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, 1 year; -20°C, 6 months (sealed storage, away from moisture and light). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

* 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.

Select the appropriate dissolution method based on your experimental animal and administration route.

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: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (6.94 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO 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 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (6.94 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (6.94 mM); Clear solution

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 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn 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: PBS
Solubility: 25 mg/mL (83.43 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

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).

Purity & Documentation

Purity: 99.93%

Data Sheet (280 KB) SDS (418 KB)

COA (252 KB) LCMS (472 KB) Elemental Analysis Report (110 KB)

Handling Instructions (2659 KB)

References

[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]. Lou M, et al. Physical interaction between human ribonucleotide reductase large subunit and thioredoxin increases colorectal cancer malignancy. J Biol Chem. 2017 Jun 2;292(22):9136-9149. [Content Brief]

[4]. 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]

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