Ko143

Catalog No.S7043 Batch:S704301

Technical Data

Formula

C₂₆H₃₅N₃O₅

Molecular Weight

469.57

CAS No.

461054-93-3

Solubility (25°C)*

In vitro

DMSO

94 mg/mL (200.18 mM)

Ethanol

94 mg/mL (200.18 mM)

Water

Insoluble

In vivo (Add solvents to the product individually and in order)

Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	2.35mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 47 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil	0.78mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 15.6 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

* <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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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 Assay:^{^[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 Study:^{^[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

Cell Assay:^{^[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 Study:^{^[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

References

Selleck's Ko143 has been cited by 2 publications

The Modern Day Heracles: Patient-derived Liver Organoids to Model Rare Pediatric Liver Diseases [ DSpace, 2023, 10.33540/2012]	PubMed: none
Heat Shock Protein 90 Triggers Multi-Drug Resistance of Ovarian Cancer via AKT/GSK3β/β-Catenin Signaling [ Front Oncol, 2021, 11:620907]	PubMed: 33738259

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.