Ko143

Catalog No.S7043

For research use only.

KO143 is a potent and relatively selective ATP-binding cassette sub-family G member 2 (ABCG2/BCRP) inhibitor. KO143 decreases the ATPase activity of ABCG2 with IC50 of 9.7 nM.

Ko143 Chemical Structure

CAS No. 461054-93-3

Selleck's Ko143 has been cited by 1 Publication

Purity & Quality Control

Choose Selective BCRP Inhibitors

Biological Activity

Description KO143 is a potent and relatively selective ATP-binding cassette sub-family G member 2 (ABCG2/BCRP) inhibitor. KO143 decreases the ATPase activity of ABCG2 with IC50 of 9.7 nM.
Targets
BCRP [1]
(Cell-free assay)
9.7 nM
In vitro

Ko143, a nontoxic analog of fungal toxin fumitremorgin C, is a potent inhibitor of ABCG2. Ko143 has an effect on the transport activity of both ABCB1 and ABCC1. Furthermore, Ko143 is found to be unstable in rat plasma. These findings indicate that Ko143 lacks specificity for ABCG2.[1]

In vivo

[11C]Ko143 is extensively metabolized in vivo and unidentified radiolabeled metabolites are found in all investigated tissues. [11C]Ko143 and possibly its radiolabeled metabolites are transported by Abcb1a and not by Abcg2 at the mouse blood-brain barrier. [11C]Ko143-derived radioactivity undergoes both hepatobiliary and urinary excretion, with Abcg2 playing a possible role in mediating the transport of radiolabeled metabolites of [11C]Ko143 from the kidney into urine.[2]

Protocol (from reference)

Cell Research:

[1]

  • Cell lines: HEK-293 cells, HEK PC cells, MCF-7 cells
  • Concentrations: 1 μM
  • Incubation Time: 0 - 45 min
  • Method:

    Cells are seeded at a density of 2.5×105 cells/ml media per well in a 24-well plate. A time-course assay is performed to determine the time at which a stable level of [3H]Ko143 is reached, as follows: media containing [3H]Ko143 is added to each well and subsequently aspirated at specific time points between 0 and 45 minutes. Three wells receive nonradioactive media to account for background signal, whereas another three are reserved for cell counts to standardize.

Animal Research:

[2]

  • Animal Models: female wild-type, Abcg2(-/-), Abcb1a/b(-/-) and Abcb1a/b(-/-)Abcg2(-/-) mice with a FVB genetic background
  • Dosages: 10 mg/kg
  • Administration: IV

Solubility (25°C)

In vitro

DMSO 94 mg/mL
(200.18 mM)
Ethanol 94 mg/mL
(200.18 mM)
Water Insoluble

Chemical Information

Molecular Weight 469.57
Formula

C26H35N3O5

CAS No. 461054-93-3
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(C)CC1C2=C(CC3N1C(=O)C(NC3=O)CCC(=O)OC(C)(C)C)C4=C(N2)C=C(C=C4)OC

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy Ko143 | Ko143 supplier | purchase Ko143 | Ko143 cost | Ko143 manufacturer | order Ko143 | Ko143 distributor