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Ko 143

Catalog No. TQ0186   CAS 461054-93-3

Ko 143 is a selective inhibitor of ATP-binding cassette sub-family G member 2 (ABCG2; BCRP).

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Ko 143 Chemical Structure
Ko 143, CAS 461054-93-3
Pack Size Availability Price/USD Quantity
2 mg In stock $ 39.00
5 mg In stock $ 64.00
10 mg In stock $ 113.00
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1 mL * 10 mM (in DMSO) In stock $ 66.00
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Purity: 98.91%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Ko 143 is a selective inhibitor of ATP-binding cassette sub-family G member 2 (ABCG2; BCRP).
Targets&IC50 ABCG2:26 nM (EC50)
In vitro In HEK G2 cells and mouse G2 cells, Ko143 (10 nM) significantly decreases the IC50 of MTX. Ko143 (1-100 μM) metabolite does not inhibit the function of ABC transporters [1]. Reversal of drug resistance in SKF 104864A-selected mouse MEF3.8/T6400 cells and human IGROV1/T8 cells by Ko143 [2]. Ko143 inhibits BCRP-mediated transport of ZD 4522 in Madin-Darby Canine Kidney (MDCK) 2-BCRP421CC (wild type) cells and MDCK2-BCRP421AA (mutant type) cells [3].
In vivo Ko143 (10 mg/kg, p.o.) increases the oral availability of SKF 104864A in mice [2].
Cell Research Cells are plated at 400 or 1000/well in 96-well plates the night before the addition of drugs. A concentration series of the drug is applied along one plate axis and left for the duration of the assay. Plates are harvested after 4-5 days while untreated wells are still subconfluent. Relative cell proliferation is quantified with CyQuant or Sybr Green I fluorescent nucleic acid stains. Assays with human cell lines are performed in the presence of 0.1 μm PSC833 to inhibit confounding P-gp activity [2].
Animal Research Oral toxicity of FTC analogs in mice is tested by mixing 50 mg/mL stocks in DMSO 1:1 with Tween 80 (polyoxyethylene sorbitan mono-oleate) and diluting with 5% w/v glucose such that the final volume administered by oral gavage is 10 μL/g of body weight. Pairs of mice are administered oral doses of 50 mg/kg Ko132, Ko134, Ko143, or vehicle under light methoxyflurane anesthesia. Final tests of 50 mg/kg Ko134 or Ko143 are performed on additional pairs of unanesthetized animals to observe any behavioral effects. Further, another pair of mice receive a higher dose of 100 mg/kg Ko134. For i.p. toxicity tests, the FTC analog stocks in DMSO are dispersed in at least 10 volumes of sterile corn oil such that the injected volume is 5 μL/g of body weight. After pilot tests at lower doses show no adverse effects, mice (4 per group) are administered vehicle or 10 mg/kg i.p. of Ko132, Ko134, or Ko143. The mice are observed continuously during the first hour after administration and then at increasing intervals for 2 weeks, after which they are sacrificed for histological examination of major organs and structures [2].
Molecular Weight 469.57
Formula C26H35N3O5
CAS No. 461054-93-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: Insoluble

DMSO: 90 mg/mL (191.66 mM), sonification is recommended.

TargetMolReferences and Literature

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.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library Anti-Cancer Compound Library Bioactive Compounds Library Max Ion Channel Inhibitor Library Bioactive Compound Library

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Keywords

Ko 143 461054-93-3 Membrane transporter/Ion channel ABC BCRP Breast cancer resistance protein ABCG2 Ko-143 Inhibitor Ko143 inhibit inhibitor

 

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