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MTOX1001P24

Sigma-Aldrich

MDR1 Knockout Caco-2 Cells

human cervix, Epithelial

Synonym(s):

MDR1 Knockout C2BBe1 Cells

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About This Item

UNSPSC Code:
41106514
NACRES:
NA.81

product name

MDR1 Knockout Caco-2 Cells, one assay ready, 24 well plate

biological source

human colon

form

liquid

morphology

Epthelial

technique(s)

drug transporter assay: suitable
permeability assay: suitable

application(s)

ADME/TOX

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General description

The C2BBe1 cells, a subclone of Caco-2 cells, correspond to ATCC CRL-2102. The MDR1 knockout C2BBe1 cells are adenocarcinoma, epithelial cells from a human caucasian male (aged 72 years) with functional knockout of the ABCB1 (MDR1) efflux transporter.

The three week production lead time begins on the Monday following a purchase, in the third week the cells are shipped overnight for receipt on Tuesday or Wednesday. As a biologic product that′s shipped at room temperature the cells must be processed immediately upon receipt.

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 knockout of the MDR1 gene eliminates the reliance on chemical inhibitors to determine if a compound is an MDR1 substrate
  • The 24 well Transwell format enables the MDR1 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

Storage Class Code

13 - Non Combustible Solids

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
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
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
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
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Articles

Drug transport assays in a 96-well system: reproducibility and correlation to human absorption

Application note on Drug transport assays in a 96-well system using Millicell-96 System from Millipore.

Caco-2 Intestinal Drug Transporter Models for More Predictive 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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