CAS NO: | 461054-93-3 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
500mg | 电议 |
生物活性 | Ko 143 is a potent and selectiveATP-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) | ||||||||||||||||
体外研究 (In Vitro) | Ko143 (10 nM) significantly decreases (2.5-fold) the IC50of 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 EC90concentration 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]. | ||||||||||||||||
体内研究 (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]. | ||||||||||||||||
分子量 | 469.57 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C26H35N3O5 | ||||||||||||||||
CAS 号 | 461054-93-3 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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溶解性数据 | In Vitro: DMSO : 100 mg/mL(212.96 mM;Need ultrasonic) 配制储备液
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以下溶剂前显示的百
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