Ko 143


CAS No. : 461054-93-3

461054-93-3
Price and Availability of CAS No. : 461054-93-3
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5mg $80 In-stock
10mg $140 In-stock
25mg $280 In-stock
50mg $500 In-stock
100mg $900 In-stock
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Cat. No. : HY-10010
M.Wt: 469.57
Formula: C26H35N3O5
Purity: >98 %
Solubility: DMSO : 100 mg/mL (212.96 mM; Need ultrasonic)
Introduction of 461054-93-3 :

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]. IC50 & Target: EC90: 26 nM (BCRP) In Vitro: Ko143 (10 nM) significantly decreases (2.5-fold) the IC50 of MTX for HEK G2 cells and mouse G2 cells. 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 FTC analogue Ko143. Ko143 is applied at zero, one, or eight times the EC90 concentration of 25 nM[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]. Ko143 significantly affects the pharmacokinetics of ZD 4522 in rats[3].

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