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MTOX1006

Sigma-Aldrich

BCRP/MRP2 Double Knockout Caco-2 Cells

Human male colorectal tissue, adenocarcinoma

Synonym(s):

C2BBe1 Cells BCRP/MRP2 (-/-/-/-,-/-/-/-)

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About This Item

UNSPSC Code:
41106514
NACRES:
NA.81

product name

BCRP/MRP2 Double Knockout Caco-2 Cells, one vial

biological source

human male colorectal tissue (Source disease: adenocarcinoma)

form

liquid

technique(s)

drug transporter assay: suitable
permeability assay: suitable

OMIM accession no.

601107
603756

application(s)

ADME/TOX

storage temp.

−196°C

Gene Information

human ... ABCC2(1244) , ABCG2(9429)

General description

The C2BBe1 cells, a subclone of Caco-2 cells, correspond to ATCC CRL-2102. The BCRP and MRP2 knockout C2BBe1 cells are adenocarcinoma, epithelial cells from a human caucasian male (aged 72 years) with functional double knockout of the ABCG2 and ABCC2 (BCRP/MRP2) efflux transporters.

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

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 juntions which is necessary for efflux ratio analysis. Other benefits include:

  • A functional double knockout of the BCRP gene and MRP2 gene eliminates the reliance on chemical inhibitors to determine if a compound is an MDR1 substrate
  • The vial format enables the BCRP and MRP2 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

ADME/Tox Cell Lines License

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.

Kit Components Also Available Separately

Product No.
Description
SDS
  • MTOX1006BCRP/MRP2 Double Knockout Caco-2 Cells, one vial 1 vialSDS

Storage Class Code

10 - Combustible liquids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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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
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
M J Briske-Anderson et al.
Proceedings of the Society for Experimental Biology and Medicine. Society for Experimental Biology and Medicine (New York, N.Y.), 214(3), 248-257 (1997-03-01)
The Caco-2 cell line is used by many investigators as a model of the intestinal epithelium to study nutrient uptake and transport. Our goal was to create an awareness of inherent variabilities in the Caco-2 cell line which may influence
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