Ko 143

Ko 143 is a potent and selective ATP-binding cassette subfamily G member 2 (ABCG2/BCRP) inhibitor. Ko 143 displays >200-fold selectivity over P-gp and MRP-1 transporters[1][2].

Product Specifications

CAS Number

[461054-93-3]

UNSPSC

12352005

Hazard Statement

H315, H319, H335

Target

BCRP

Type

Reference compound

Related Pathways

Membrane Transporter/Ion Channel

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/Ko-143.html

Purity

99.97

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C1N2[C@]([H])(C3=C(C[C@]2(C(N[C@H]1CCC(OC(C)(C)C)=O)=O)[H])C4=CC=C(OC)C=C4N3)CC(C)C

Molecular Formula

C26H35N3O5

Molecular Weight

469.57

Precautions

H315, H319, H335

References & Citations

[1]Weidner LD, et al. The Inhibitor Ko143 Is Not Specific for ABCG2. J Pharmacol Exp Ther. 2015 Sep;354 (3) :384-93.|[2]JD Allen et al. Potent and Specific Inhibition of the Breast Cancer Resistance Protein Multidrug Transporter in Vitro and in Mouse Intestine by a Novel Analogue of Fumitremorgin C. Mol. Cancer Ther. 2002, 1, 417-425.|[3]Wen JH, et al. Effect of Ursolic Acid on Breast Cancer Resistance Protein-mediated Transport of ZD 4522 In Vivo and Vitro. Chin Med Sci J. 2015 Dec;30 (4) :218-25.|[4]Hou J, et al. Quantitative determination and pharmacokinetic study of the novel anti-Parkinson's disease candidate drug FLZ in rat brain by high performance liquid chromatography-tandem mass spectrometry. J Pharm Biomed Anal. 2012 Jul;66:232-9.|[5]Liu K, et al. Metabolism of KO143, an ABCG2 inhibitor. Drug Metab Pharmacokinet. 2017 Aug;32 (4) :193-200.