Gemcitabine HCl

PDF

S1149

5~200mg

Brand

Selleckchem

Description

Gemcitabine HCl

Catalog No.S1149

2 Reviews 2 Product Citations

Gemcitabine HCl is a DNA synthesis inhibitor with IC50 of 50 nM, 40 nM, 18 nM and 12 nM in PANC1, MIAPaCa2, BxPC3 and Capan2 cells, respectively.

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Biological Activity

Description	Gemcitabine HCl is a DNA synthesis inhibitor with IC50 of 50 nM, 40 nM, 18 nM and 12 nM in PANC1, MIAPaCa2, BxPC3 and Capan2 cells, respectively.
Targets	PANC1	MIAPaCa2	BxPC3	Capan2 cell lines
IC50	50 nM	40 nM	18 nM	12 nM ^[1]
In vitro	Gemcitabine induced NF-κB activity in BxPC-3, PANC-1, and MIA PaCa-2 cells and decreased the level of the NF-κB inhibitor IκBα in BxPC-3 and PANC-1 cells. Treatment of BxPC-3 cells with low dose Gemcitabine for 48 hours results in a dose-dependent increase in NF-κB binding. In contrast, NF-κB DNA binding is decreased in BxPC-3 cells treated with the higher Gemcitabine doses for 48 h; however, 24-h treatment with these higher doses increases NF-κB binding in BxPC-3 cells ^[2]
In vivo	Intratumoral NF-κB activity is significantly elevated (1.3- to 1.8-fold) in the Gemcitabine-treated mice compared to the PBS-treated mice, suggesting that Gemcitabine also induces NF-κB activation. ^[2]
Features	Gemcitabine has been used to treat pancreatic cancer and has demonstrated effective anti-tumor activity.

Protocol(Only for Reference)

Cell Assay: ^[2]

Cell lines	BxPC-3, MIA PaCa-2, and PANC-1 cells
Concentrations	0.2 μM
Incubation Time	24 hours or 48 hours
Method	BxPC-3, MIA PaCa-2, and PANC-1 cells are seeded in a 96-well plate. After 24 hours, cells are treated with vehicle, DMAPT and/or Gemcitabine for an additional 24 hours or 48 hours. Apoptosis is quantified using the Cell Death Detection ELISA to detect the amount of cytoplasmic histone-associated DNA fragments and expressed relative to vehicle-treated cells.

Animal Study: ^[2]

Animal Models	Athymic nude mice with MIA PaCa-2 cells
Dosages	50 mg/kg or 100 mg/kg
Administration	Administered via i.p.
Solubility	Saline, 20 mg/mL

References

Clinical Trial Information( data from http://clinicaltrials.gov)

NCT Number	Recruitment	Conditions	Sponsor /Collaborators	Start Date	Phases
NCT01956812	Not yet recruiting	Metastatic Pancreatic Cancer\|Pancreatic Cancer	Immunomedics, Inc.	2013-12	Phase 3
NCT01964430	Not yet recruiting	Pancreatic Neoplasms\|Digestive System Neoplasms\|Neoplasms by Site\|Neoplasms\|Endocrine Gland Neoplasms\|Pancreatic Diseases\|Digestive System Diseases\|Endocrine System Diseases\|Gemcitabine\|Antimetabolite	Celgene Corporation	2014-01	Phase 3
NCT01830322	Withdrawn	Metastatic Pancreatic Adenocarcinoma	Cornerstone Pharmaceuticals, Inc.	2014-01	Phase 2
NCT02016417	Not yet recruiting	Nasopharyngeal Carcinoma	Cancer Hospital of Guangxi Medical University	2014-01	Phase 2
NCT01852890	Not yet recruiting	Pancreatic Neoplasms	University of Iowa\|Joseph J. Cullen	2014-02	Phase 1

Chemical Information

Download Gemcitabine HCl SDF

Molecular Weight (MW)	299.66
Formula	C₉H₁₁F₂N₃O₄.HCI
CAS No.	122111-03-9

Storage	3 years -20â„ƒPowder
Storage	6 months-80â„ƒin DMSO
Syonnyms	N/A

Solubility (25°C) *	In vitro	DMSO	<1 mg/mL (<1 mM)
		Water	23 mg/mL (76 mM)
		Ethanol	<1 mg/mL (<1 mM)
	In vivo	Saline,	20 mg/mL
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Name	4-amino-1-((2R,4R,5R)-3,3-difluoro-4-hydroxy-5-(hydroxymethyl)-tetrahydrofuran-2-yl)pyrimidin-2(1H)-one hydrochloride

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Customer Reviews (2)

Click to enlarge	Rating
	Source	Immunol Immunother, 2013, 62, 383–391. Gemcitabine HCl purchased from Selleck
	Method	Xenograft
	Cell Lines	CT26 cells
	Concentrations	50/100 mg/kg
	Incubation Time	30 day
	Results	Injection of GEM (50 mg/kg) suppressed tumor growth significantly when the tumor size was evaluated on day 30 after tumor inoculation.