biological source
human male colorectal tissue (Source Disease: colon adenocarcinoma)
Quality Level
form
liquid
technique(s)
drug transporter assay: suitable
permeability assay: suitable
application(s)
ADME/TOX
storage temp.
−196°C
Gene Information
human ... ABCC3(8714)
General description
The C2BBe1 cells, a subclone of Caco-2 cells, correspond to ATCC CRL-2102. The MRP3 knockout C2BBe1 cells are adenocarcinoma, epithelial cells from a human caucasian male (aged 72 years) with functional knockout of the ABCC3 (MRP3) efflux transporter.
Application
The following posters and articles demonstrate how Caco-2 cells can be used for cell based assays:
Transporter Function in Caco-2 Cells with Targeted P-Glycoprotein, MRP2 and BCRP Gene Knockout Using Zinc Finger Nucleases
Comparison of Function and Relative Transporter Protein Concentrations in Caco-2 Cells with Single and Double Knockouts of the ABCB1, ABCG2, and ABCC2 Genes
Caco-2 Transporter Knockout Cell Based Assays
Transporter Function in Caco-2 Cells with Targeted P-Glycoprotein, MRP2 and BCRP Gene Knockout Using Zinc Finger Nucleases
Comparison of Function and Relative Transporter Protein Concentrations in Caco-2 Cells with Single and Double Knockouts of the ABCB1, ABCG2, and ABCC2 Genes
Caco-2 Transporter Knockout Cell Based Assays
Features and Benefits
The Caco-2 subclone C2BBe1 cells are ideal for transporter analysis as they express multiple transporters, are human derived, and grow in a homogenous monolayer that forms tight junctions necessary for efflux ratio analysis. Other benefits include:
- A functional knockout of the MRP3 gene eliminates the reliance on chemical inhibitors to determine if a compound is an MRP3 substrate
- The vial format enables the MRP3 knockout cells to be included in standard drug transporter protocols
- Human assay with no interference from animal inhibitors
- Overcome the limitations of RNAi and knockdown cell lines that arise from remaining transporter functionality
Legal Information
Disclaimer
RESEARCH USE ONLY. This product is regulated in France when intended to be used for scientific purposes, including for import and export activities (Article L 1211-1 paragraph 2 of the Public Health Code). The purchaser (i.e. enduser) is required to obtain an import authorization from the France Ministry of Research referred in the Article L1245-5-1 II. of Public Health Code. By ordering this product, you are confirming that you have obtained the proper import authorization.
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Regulatory Information
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Find documentation for the products that you have recently purchased in the Document Library.
P Artursson
Journal of pharmaceutical sciences, 79(6), 476-482 (1990-06-01)
A human intestinal cell line, Caco-2, was used as a model to study the passive diffusion of drugs across intestinal epithelium. The cells formed continuous monolayers when grown on permeable filters of polycarbonate. After 10 days in culture, the monolayers
V Pade et al.
Journal of pharmaceutical sciences, 87(12), 1604-1607 (1999-04-03)
The objective of this investigation was to establish a relationship between drug permeability and solubility in vitro and the extent of drug absorption in humans. We selected drugs with varying permeabilities and solubilities with the aim of establishing a relationship
S Yee
Pharmaceutical research, 14(6), 763-766 (1997-06-01)
To evaluate and optimize the use of Caco-2 cell monolayers to predict the in vivo absorption of a broad range of compounds in man. Caco-2 cells are derived from human adenocarcinoma colon cells and spontaneously differentiate when grown on porous
X Wu et al.
Pharmaceutical research, 17(2), 209-215 (2000-04-06)
The purpose of this study was to elucidate the mechanisms by which an HMG-CoA reductase inhibitor, atorvastatin (an organic acid with a pKa of 4.46), was transported in the secretory and absorptive directions across Caco-2 cell monolayers. Caco-2 cells were
Kathleen E Sampson et al.
Drug metabolism and disposition: the biological fate of chemicals, 43(2), 199-207 (2014-11-13)
Membrane transporters P-glycoprotein [P-gp; multidrug resistance 1 (MDR1)], multidrug resistance-associated protein (MRP) 2, and breast cancer resistance protein (BCRP) affect drug absorption and disposition and can also mediate drug-drug interactions leading to safety/toxicity concerns in the clinic. Challenges arise with
Articles
We presents an article on The Role of Intestinal Efflux Transporters In Drug Absorption.
Utilize these Caco-2 cell based assay tools for screening small molecule drug compounds prior to clinical studies and submission to regulatory agencies.
Our team of scientists has experience in all areas of research including Life Science, Material Science, Chemical Synthesis, Chromatography, Analytical and many others.
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